Search Result
Results for "
rat models
" in MedChemExpress (MCE) Product Catalog:
8
Biochemical Assay Reagents
19
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-B0712B
-
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Ro 13-9904
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Antibiotic
GSK-3
Bacterial
Aurora Kinase
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Infection
Inflammation/Immunology
Cancer
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Ceftriaxone sodium salt (Ro 13-9904) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium salt is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium salt is an inhibitor of Aurora B. Ceftriaxone sodium salt has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium salt can be used in the study of bacterial infections and meningitis .
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- HY-B0712
-
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Ro 13-9904 free acid
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Bacterial
Antibiotic
GSK-3
Aurora Kinase
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Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
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- HY-119580
-
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Others
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Inflammation/Immunology
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Leucocyanidin is an active anti-ulcerogenic ingredient was extracted from Litchi Chinensis. Leucocyanidin demonstrates a significant protective effect against Aspirin-induced erosions in rat models .
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- HY-B0712A
-
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Ro 13-9904 sodium hydrate
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Bacterial
Antibiotic
GSK-3
Aurora Kinase
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Infection
Cancer
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Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium hydrate is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis .
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- HY-15451
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MDA 19
2 Publications Verification
BZO-HEXOXIZID
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Cannabinoid Receptor
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Neurological Disease
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MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity .
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- HY-145512
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NLT
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Dopamine Receptor
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Neurological Disease
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N-(α-Linolenoyl) tyrosine (NLT) is a dopaminergic agonist capable of crossing the blood-brain barrier. N-(α-Linolenoyl) tyrosine increases the level, turnover rate and release amount of dopamine in the striatum. N-(α-Linolenoyl) tyrosine modulates rotational behavior in a rat model with unilateral striatal injury and alleviates excessive blinking symptoms in models induced by dopamine-depleting agents. N-(α-Linolenoyl) tyrosine can be used for research on Parkinson's disease and idiopathic blepharospasm .
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- HY-W041988
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Bacterial
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Infection
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Fmoc-Glu-OMe is a glutamic acid derivative. Fmoc-Glu-OMe exhibits significant antibacterial activity and excellent gelation properties in silver nitrate (AgNO3) solution. Fmoc-Glu-OMe promotes wound healing in rat models and eliminates bacteria in MRSA-infected rat wound models. Fmoc-Glu-OMe can be used in studies related to wound infections and MRSA-infected wounds .
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- HY-B1258
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Aminomethylbenzoic acid; α-Amino-p-toluic acid
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Amino Acid Derivatives
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Cancer
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4-(Aminomethyl)benzoic acid is a competitive inhibitor of PepT1 and has antifibrinolytic activity .
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- HY-W008270
-
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γ-Crotonolactone
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Endogenous Metabolite
Bacterial
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Infection
Neurological Disease
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2(5H)-Furanone (γ-Crotonolactone) is an endogenous metabolite. 2(5H)-Furanone mimics N-acyl homoserine lactone signals, occupies the binding site of LuxR homologs, and interferes with quorum sensing-mediated gene regulation. 2(5H)-Furanone inhibits quorum sensing mediated by AHLs with different acyl chain lengths. 2(5H)-Furanone inhibits biofilm formation of environmental Aeromonas hydrophila strains on polystyrene plates. 2(5H)-Furanone suppresses spike-and-wave discharges in a rat model of generalized absence seizures and exhibits selective activity against absence seizures. 2(5H)-Furanone can be used in studies related to bacteria infections and generalized absence seizures.
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- HY-101481
-
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COX
Apoptosis
MEK
ERK
PPAR
AMPK
NF-κB
Interleukin Related
TNF Receptor
STAT
Wnt
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Neurological Disease
Inflammation/Immunology
Cancer
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Flurbiprofen axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent with anti-inflammatory and analgesic effects. Flurbiprofen axetil inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. Flurbiprofen axetil can promote neuroprotection after focal cerebral ischemia in rats by partially activating PPAR-γ. Flurbiprofen axetil alleviates cerebral ischemia/reperfusion injury by reducing inflammation in a transient global cerebral ischemia/reperfusion rat model. Flurbiprofen axetil can alleviate inflammatory responses and cognitive function in a mild cognitive impairment (MCI) SD rat model through the AMPKα/NF-κB signaling pathway .
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- HY-11095
-
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mGluR
CaSR
PI3K
Akt
mTOR
Autophagy
Apoptosis
Bcl-2 Family
Caspase
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Cardiovascular Disease
Neurological Disease
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NPS 2390 is an allosteric antagonist of calcium-sensing receptor (CaSR) and mGluR1/5. NPS 2390 inhibits the PI3K/Akt/mTOR signaling pathway, reduces hypoxia-induced intracellular calcium elevation, decreases the expression of autophagy (autophagy) proteins, regulates the expression of phenotypic marker proteins, and inhibits the proliferation of pulmonary artery smooth muscle cells. NPS 2390 attenuates the endogenous apoptosis (apoptosis) pathway, increases the expression level of Bcl-2, downregulates the expression levels of Bax, cytochrome c and caspase-3, alleviates cerebral edema and improves neurological function in rat models. NPS 2390 can be used in studies related to hypoxic pulmonary hypertension, traumatic brain injury, stroke and pain .
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- HY-N3710
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Kumujian G; O-Methylpicrasidine I
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JAK
Apoptosis
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Neurological Disease
Cancer
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Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain .
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- HY-132814
-
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ATH-1017
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c-Met/HGFR
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Neurological Disease
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Fosgonimeton (ATH-1017) is a hepatocyte growth factor receptor (c-Met/HGFR) agonist. Fosgonimeton has neuroprotective effects in both LPS (HY-D1056) -induced neuroinflammation and Aβ-induced AD models .
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- HY-17375
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Progesterone Receptor
Androgen Receptor
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Endocrinology
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Allylestrenol is an orally active synthetic anti-androgen sexualsteroid. Allylestrenol can prevent miscarriage in vivo. Allylestrenol significantly affects testosterone progesterone level in rat model. Allylestrenol can reduce ventral prostate weight in rat model .
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- HY-P990302
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nAChR
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Neurological Disease
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Anti-Human/Rat/Fish AChR Antibody (Mab35) is an anti-human/rat/fish AChR IgG1 monoclonal antibody. Anti-Human/Rat/Fish AChR Antibody (Mab35) can attack the AChR of neuromuscular junctions. Anti-Human/Rat/Fish AChR Antibody (Mab35) can be used for the construction of myasthenia gravis models .
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- HY-111745
-
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JAK
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Inflammation/Immunology
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Tyk2-IN-5 (compound 6) is a potent, selective and orally active tyrosine kinase 2 (Tyk2) inhibitor that acts on the JH2 structural domain. Tyk2-IN-5 shows a Ki value of 0.086 nM for Tyk2 JH2 and an IC50 value of 25 nM for IFNα. Tyk2-IN-5 efficiently inhibits the production of IFNγ in a pharmacodynamic rat model and is fully efficacious in a rat model of arthritis .
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- HY-106856
-
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NT-11624
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iGluR
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Cancer
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Dimiracetam is an orally active compound, with anti-neuropathic activity. Dimiracetam inhibits hypersensitivity and neurological alterations, and inhibits Sorafenib (HY-10201)-induced neuropathy in cold stimulation rat models .
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- HY-P990107
-
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TGF-β Receptor
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Cancer
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Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) is an TGF-β IgG antibody inhibitor. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) reduces renal fibrosis in unilateral ureteral obstruction (UUO) mice models. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) shows potent anti-tumor effect in various tumor models, such as pancreatic cancer .
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- HY-111996
-
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Potassium Channel
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Neurological Disease
Inflammation/Immunology
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Kv3 activator-1 is a Kv3 family voltage-gated potassium channel activator. Kv3 activator-1 reverses mechanical hyperalgesia in rat models of neuropathic and inflammatory pain, with rapid onset and long-lasting, dose-related effects. Kv3 activator-1 can be used for the research of pain .
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- HY-P1090
-
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Cannabinoid Receptor
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Neurological Disease
|
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Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
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- HY-111029A
-
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GlyT
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Others
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ALX-1393 TFA, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model .
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- HY-175668
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Potassium Channel
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Neurological Disease
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IDOR-1104-0086 is an orally active Kv7 potassium channel opener with an EC50 of 210 nM that can cross blood-brain barrier. IDOR-1104-0086 displays strong selectivity against the hERG channel with an IC20 of 25 μM. IDOR-1104-0086 exhibits efficacy in two rodent models of epilepsy and a favorable tolerability profile. IDOR-1104-0086 can used for the study of epilepsy .
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- HY-W987949
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Others
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Neurological Disease
|
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Z-4105 is an orally active nootropic agent. Z-4105 reverses the amnesic effects of electroconvulsive shock (ECS) and methylazoxymethanol acetate (MAM), and improves learning and memory functions. Z-4105 enhances the activity of the brain cholinergic system without affecting other neurotransmitter systems. Z-4105 significantly alleviates neuropathic pain in rats. Z-4105 can be used in the research of neuropathic pain and brain dysfunction .
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- HY-124831
-
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Neurotensin Receptor
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Neurological Disease
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NTRC-844 (compound 8) is a selective antagonist of neurotensin receptor type 2 (NTS2),with the EC50 of 238 nM. NTRC-844 plays an important role in analgesic animal research .
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- HY-B0712R
-
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Ro 13-9904 free acid (Standard)
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Reference Standards
Bacterial
Antibiotic
GSK-3
Aurora Kinase
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Infection
Inflammation/Immunology
Cancer
|
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Ceftriaxone (Standard) is the analytical standard of Ceftriaxone. This product is intended for research and analytical applications. Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis[1][2][3][4][5][6][7].
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- HY-U00133
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Drug Derivative
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Inflammation/Immunology
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HSR6071, a pyrazinecarboxamide derivative, is an orally active and potent antiallergic agent. HSR6071 potently inhibits the experimental asthma in rat models .
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- HY-111029
-
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GlyT
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Neurological Disease
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ALX-1393, a selective GlyT2 inhibitor, has an antinociceptive effect on thermal, mechanical, and chemical stimulations in a rat acute pain model .
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- HY-123179
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Carbonic Anhydrase
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Cardiovascular Disease
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Mefruside is an orally active diuretic and has a mild hypotensive effect. Mefruside inhibits the synthesis of urea in an isolated rat liver perfusion model. Mefruside can be used in studies of oedema and hypertension .
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- HY-W145695
-
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Biochemical Assay Reagents
Apoptosis
Interleukin Related
IFNAR
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Cardiovascular Disease
Inflammation/Immunology
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Chitoheptaose is an orally active chitooligosaccharide (degree of polymerization = 7). Chitoheptaose can be extracted from the exoskeletons of crustaceans, such as the shells of crabs, shrimps and lobsters. Chitoheptaose reduces pro-inflammatory cytokines while increasing the levels of anti-inflammatory cytokines (decreasing the levels of pro-inflammatory cytokines IL-1β, IL-17A and IFN-γ, and increasing the level of the anti-inflammatory cytokine IL-10). Chitoheptaose possesses antioxidant, anti-inflammatory and anti-Apoptotic activities. Chitoheptaose improves cardiac parameters, alleviates myocarditis injury, and exerts cardioprotective effects in a rat model of myocarditis. Chitoheptaose can be used in studies related to myocarditis .
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- HY-P11043
-
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GLP Receptor
Neuropeptide Y Receptor
Arrestin
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Metabolic Disease
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GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research .
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- HY-170409
-
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Trk Receptor
Apoptosis
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Neurological Disease
Inflammation/Immunology
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BNN27 is the agonist for TrkA receptor and p75NTR receptor, that exhibits neurotrophic and anti-apoptotic effects. BNN27 increases the levels of glutamate, GABA, and glutamine in the rat hippocampus and prefrontal cortex, improves glutamate turnover. BNN27 exhibits neuroprotective efficacy in mouse amyotrophic lateral sclerosis (ALS) model, exhibits anti-inflammatory efficacy in experimental autoimmune encephalomyelitis (EAE) model, exhibits retinal protective efficacy in rat diabete models. BNN27 is blood-brain barrier penetrable .
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- HY-119495
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Thyroid Hormone Receptor
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Neurological Disease
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JTP 2942 is a thyrotropin-releasing hormone analogue. JTP 2942 can promote the release of Acetylcholine in the hippocampus and frontal cortex of rats. JTP 2942 possesses neuroprotective and cognitive-improving activities. JTP 2942 dose-dependently improves motor and neurological deficits in rat models of chronic focal cerebral ischemia. JTP 2942 can be used for the research of cerebral ischemia, motor neuron diseases, and other related conditions .
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- HY-159931
-
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AAK1
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Neurological Disease
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HW161023 (compound 5) is an orally active AP2-associated protein kinase 1 (AAK1) inhibitor with IC50 values of 5.4 nM and 11.9 μM aganist of AAK1and hERG, respectively. HW161023 inhibits the pain in chronic constriction injury of the sciatic nerve rat model .
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- HY-W794785
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5-HT Receptor
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Neurological Disease
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WAY 208466 is a selective 5-HT6 receptor agonist with an EC50 of 7.3 nM. WAY-208466 increases GABA levels following both acute and chronic administration in the dorsolateral frontal cortex of rat models with stereotaxic surgery. WAY 208466 can be used for anxiety-related disorders like obsessive compulsive disorder (OCD) research .
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- HY-165478
-
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5 alpha Reductase
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Endocrinology
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FCE 28260 is an orally active 4-azacyclic 5α-reductase (5αR) inhibitor. FCE 28260 exhibits IC₅₀ values for human 5αR type 1 and 5αR type 2 of 36 and 3.3 nM, respectively, and for human and rat prostates with IC₅₀ values of 16 and 15 nM, respectively. FCE 28260 simultaneously blocks the production of dihydrotestosterone (DHT) in the prostate and peripheral tissues. FCE 28260 can significantly inhibit the induction of prostatic and seminal vesicle hyperplasia by testosterone (T) in rat models, without inhibiting the growth of the prostate in DHT implantation models. FCE 28260 can be used for the studies DHT-dependent diseases such as benign prostatic hyperplasia (BPH) .
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- HY-163121
-
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Glycosyltransferase
TGF-β Receptor
FAK
Galectin
Collagen
|
Endocrinology
Cancer
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PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC50 of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease .
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- HY-169332
-
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Piezo Channel
ERK
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Metabolic Disease
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Piezo1 agonist 1-d2 is a Piezo1 agonist and osteogenesis promoter with an EC50 of 2.21 μM. Piezo1 agonist 1-d2 activates Piezo1 and induces calcium ion influx in mesenchymal stem cells. Piezo1 agonist 1-d2 activates the Erk signaling pathway and promotes osteogenesis of mesenchymal stem cells. Piezo1 agonist 1-d2 alleviates disuse osteoporosis in a hindlimb unloading rat model. Piezo1 agonist 1-d2 can be used for research on osteoporosis .
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- HY-120321
-
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Mineralocorticoid Receptor
Carbonic Anhydrase
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Cardiovascular Disease
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DSR-71167 is an orally active mineralocorticoid receptor (MR) antagonist with an IC50 of 0.26 μM. DSR-71167 exhibits weak carbonic anhydrase (CA) inhibitory activity with an IC50 of 19 μM. DSR-71167 can dose-dependently increase urinary sodium excretion in rat models and has a very low risk of hyperkalemia in potassium-loading rat models. DSR-71167 lowers systolic blood pressure in hypertensive rat models. DSR-71167 can be used for research on hypertension and heart failure .
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- HY-B0712S1
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Ro 13-9904-13C2,d32 triethylammonium salt
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Antibiotic
Aurora Kinase
GSK-3
Bacterial
Isotope-Labeled Compounds
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Infection
Inflammation/Immunology
Cancer
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Ceftriaxone-13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
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- HY-177509
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Cholecystokinin Receptor
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Metabolic Disease
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BBL454 (Compound 43) is a Cholecystokinin 2B (CCK2B) receptor agonist. BBL454 induces hyperactivity and improves memory in rat models while it has weak activity on the peripheral CCK2 receptor and no anxiogenic activity. BBL454 increases gastric acid output in anesthetised rat models. BBL454 can be used for diabetes research .
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- HY-105362
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Endothelin Receptor
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Cardiovascular Disease
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PD 155080 is a selective endothelin A receptor (ETA receptor) antagonist. PD 155080 reduces coronary resistance in the isolated rat heart model. PD 155080 improves myocardial systolic function and diastolic function in the ischemia/reperfusion model. PD 155080 can be used for the study of cardiovascular diseases .
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- HY-172147
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Somatostatin Receptor
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Neurological Disease
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SSTR4 agonist 5 (Compound 5) is the orally active agonist for somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. SSTR4 agonist 5 exhibits good stability in human/rat liver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models .
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- HY-111755
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P2Y Receptor
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Cardiovascular Disease
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P2Y12 antagonist 2 is a potent P2Y12 receptor antagonist. P2Y12 antagonist 2 exhibits excellent antiplatelet aggregation potency with an IC50 value of 2.94 μM as well as antithrombotic efficacy in a rat ferric chloride model. P2Y12 antagonist 2 shows a superior safety profile than Clopidogrel (HY-15283) in a rat tail-bleeding model. P2Y12 antagonist 2 can be used to research thromboembolic disorders .
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- HY-A0113
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Ro 31-3113
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
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Cilazaprilat is an inhibitor of angiotensin-converting enzyme (ACE; IC50=0.7 nM for the rat enzyme) and an active metabolite of Cilazapril (HY-A0043). It decreases creatine kinase release in primary neonatal rat cardiac myocytes in an in vitro model of ischemia-reperfusion injury induced by hypoxia and reoxygenation when used at a concentration of 10 μM.3 Intra-arterial administration of cilazaprilat (3 μg/kg per minute) increases coronary blood flow and fractional shortening in a dog model of coronary hypoperfusion-induced myocardial ischemia.
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- HY-19155A
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ZD-8731
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Angiotensin Receptor
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Cardiovascular Disease
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ICI-D 8731 (compound 5g) is a angiotensin II receptor antagonist with the IC50 of 0.031 μM. ICI-D 8731 shows a rapid and sustained lowering of blood pressure in a renal hypertensive rat model .
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- HY-120710
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- HY-174127
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P2Y Receptor
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Neurological Disease
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P2Y1 antagonist 3 (compound 36b) is a blood-brain barrier (BBB)-penetrant P2Y1 antagonist with an IC50 of 0.50 μM. P2Y1 antagonist 3 exhibits protective effects in a rat middle cerebral artery occlusion (MCAO) model and demonstrates neuroprotective activity against oxidative stress by upregulating nuclear Nrf2 protein levels .
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- HY-117132
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mGluR
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Neurological Disease
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YM-202074 is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
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- HY-103556
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mGluR
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Neurological Disease
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YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a Ki of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 8.6 nM. YM-202074 fumarate has potent neuroprotective effects in transient MCA (tMCA) occlusion rat models .
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- HY-123864
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S 448
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Integrin
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Cardiovascular Disease
Cancer
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SC-68448 (S 448) is a selective αvβ3 antagonist (IC50 = 1 nM). SC-68448 inhibits αvβ3-mediated endothelial cell proliferation. SC-68448 reduces the total level of αvβ6 in NHBE cells. SC-68448 inhibits angiogenesis in a rat corneal neoplasia model. SC-68448 inhibits tumor growth and completely prevents the development of hypercalcemia in a rat Ledich cell tumor model. SC-68448 can be used in research on cardiovascular and cerebrovascular diseases such as hypercalcemia and cancers such as testicular interstitial cell tumors .
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- HY-119262
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
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ABT-866 is an α1A-adrenoceptor agonist and an antagonist at the α1B- and α1D-adrenoceptor subtypes. ABT-866 has an EC50 of 0.60 μM for the α1A in the rabbit urethra. ABT-866 has a pA2 value of 5.4 for the α1B in the rat spleen. ABT-866 has a pA2 value of 6.2 for the α1D in the rat aorta. ABT-866 exhibits good urethral selectivity and lower cardiovascular side effects in stress urinary incontinence models. ABT-866 can be used for the research of diseases such as stress urinary incontinence .
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- HY-101481R
-
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Reference Standards
COX
Apoptosis
MEK
ERK
PPAR
AMPK
NF-κB
Interleukin Related
TNF Receptor
STAT
Wnt
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Flurbiprofen axetil (Standard) is the analytical standard of Flurbiprofen axetil. This product is intended for research and analytical applications. Flurbiprofen axetil is a non-selective COX inhibitor and a nonsteroidal anti-inflammatory agent with anti-inflammatory and analgesic effects. Flurbiprofen axetil inhibits basal-like breast cancer metastasis by inhibiting the MEK/ERK signaling pathway. Flurbiprofen axetil can promote neuroprotection after focal cerebral ischemia in rats by partially activating PPAR-γ. Flurbiprofen axetil alleviates cerebral ischemia/reperfusion injury by reducing inflammation in a transient global cerebral ischemia/reperfusion rat model. Flurbiprofen axetil can alleviate inflammatory responses and cognitive function in a mild cognitive impairment (MCI) SD rat model through the AMPKα/NF-κB signaling pathway .
|
-
- HY-176793
-
|
|
JAK
|
Infection
Inflammation/Immunology
Cancer
|
|
JAK1-IN-18 (Example 2) is a selective JAK1 inhibitor with an IC50 of 0.15 nM for JAK1 over JAK2 and JAK3. JAK1-IN-18 significantly reduces inflammation in DSS (HY-116282C)-induced ulcerative colitis (UC) mouse models and DNBS(HY-W324435)-induced Crohn's disease (CD) rat models. JAK1-IN-18 can be used for autoimmune diseases (such as inflammatory bowel disease), viral infections (such as HBV infection) and cancers (such as blood cancer) research .
|
-
- HY-111047
-
|
|
Topoisomerase
Bacterial
|
Infection
|
|
GSK945237 is a potent and orally active bacterial type IIA topoisomerases inhibitor. GSK945237 shows broad-spectrum activity against Gram-positive and Gram-negative bacteria (IC50 of 0.034 μg/mL against H. influenzae DNA gyrase). GSK945237 demonstrates good in vivo efficacy in a rat respiratory tract infection model. GSK945237 can be used for anti-infection research .
|
-
- HY-176712
-
|
|
GSNOR
Apoptosis
|
Neurological Disease
|
|
GSNOR-IN-1, a prodrug of GSNOR-IN-2 (HY-176275), is a BBB-penetrable S-nitrosoglutathione reductase (GSNOR) inhibitor. GSNOR-IN-1 has significant protective activity against OGD/R-induced injury. GSNOR-IN-1 regulates calcium signaling and synaptic function via Clstn1 S-nitrosation and inhibits neuronal apoptosis. GSNOR-IN-1 significantly reduces infarct volume while improving neurological deficits in ischemic stroke rat models. GSNOR-IN-1 has neuroprotective activity, promising for ischemic stroke research .
|
-
- HY-12706
-
-
- HY-111309
-
|
|
Androgen Receptor
|
Endocrinology
|
|
LGD-2941 is an orally active, potent and selective androgen receptor modulator. LGD-2941 shows excellent anabolic activity in muscle with reduced effect on the prostate in a rat model of hypogonadism. LGD-2941 also improves bone strength in a rat model of post-menopausal osteoporosis .
|
-
- HY-17375R
-
|
|
Progesterone Receptor
Reference Standards
Androgen Receptor
|
Endocrinology
|
|
Allylestrenol (Standard) is the analytical standard of Allylestrenol. This product is intended for research and analytical applications. Allylestrenol is an orally active synthetic anti-androgen sexualsteroid. Allylestrenol can prevent miscarriage in vivo. Allylestrenol significantly affects testosterone progesterone level in rat model. Allylestrenol can reduce ventral prostate weight in rat model .
|
-
- HY-107527A
-
|
|
GlyT
|
Inflammation/Immunology
|
|
Org 25543 is a selective inhibitor of the glycine transporter 2, exhibiting analgesic properties in a rat model of chronic pain.
|
-
- HY-155133
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-34 (compound 8a) is a selective and orally active inhibitor of COX-2 , with an IC50 of 0.42 μM. COX-2-IN-34 has no gastric ulcer toxicity but has anti-inflammatory effects .
|
-
- HY-B0712AR
-
|
Ro 13-9904 sodium hydrate (Standard)
|
Reference Standards
Bacterial
Antibiotic
GSK-3
Aurora Kinase
|
Infection
Cancer
|
|
Ceftriaxone (sodium hydrate) (Standard) is the analytical standard of Ceftriaxone (sodium hydrate). This product is intended for research and analytical applications. Ceftriaxone sodium hydrate (Ro 13-9904 sodium hydrate) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone sodium hydrate is a covalent inhibitor of GSK3β with IC50 value of 0.78 μM. Ceftriaxone sodium hydrate is an inhibitor of Aurora B. Ceftriaxone sodium hydrate has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone sodium hydrate can be used in the study of bacterial infections and meningitis .
|
-
- HY-P5978
-
|
ANP 127-150 (rat)
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
Atriopeptin III (ANP 127-150) (rat), a 24-amino acid atrial peptide, is a potent vasodilator and natriuretic/diuretic agent. Atriopeptin III (rat) improves renal functions and decreases blood pressure in a ureter-obstructed rat kidney model. Atriopeptin III (rat) can be used for research of chronic renal failure .
|
-
- HY-N9737
-
|
|
Others
|
Neurological Disease
|
|
(−)-Acutumine is a tetracyclic chloroalkaloid that exhibits selective cytotoxicity to cultured human T cells and memory-enhancing properties in the Wistar rat model .
|
-
- HY-168211
-
|
|
Epoxide Hydrolase
|
Inflammation/Immunology
|
|
LQ-38 is an orally active inhibitor for soluble epoxide hydrolase (sEH) with an IC50 of 5.2 nM. LQ-38 exhibits anti-inflammatory activity in rat foot edema model and mouse acute pancreatitis model, exhibits analgesic effect in Acetic acid (HY-Y0319)-induced writhing mouse model .
|
-
- HY-P1090A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-W587877
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Triundecanoin is a triacylglycerol. Triundecanoin maintain the glucose supplement during fasting through β-oxidation and acetyl-CoA production in rat models .
|
-
- HY-106365
-
|
|
Glucocorticoid Receptor
|
Endocrinology
|
|
Rofleponide is a synthetic glucocorticoid that has a high affinity for rat thymic glucocorticoid receptors and has high anti-inflammatory efficacy in experimental animal models .
|
-
- HY-167676
-
|
|
DNA/RNA Synthesis
|
Inflammation/Immunology
|
|
Cofpropamine, a caffeine derivative that inhibits polyadenylation, enhances the inhibitory effect of cyclophosphamide (HY-17420) in rat adjuvant arthritis and mouse collagen arthritis models .
|
-
- HY-129641
-
-
- HY-114897
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
L-167307 is an effective pyrrole-based p38 kinase inhibitor that can reduce secondary paw swelling in rat adjuvant-induced arthritis models .
|
-
- HY-108302
-
|
|
Adrenergic Receptor
|
Others
|
|
Nifenalol is a β-adrenergic receptor blocker. Nifenalol inhibits β-adrenoceptor differentiation in right atrium, diaphragm and adipose tissue in a rat model .
|
-
- HY-171037
-
|
PGBx
|
Mitochondrial Metabolism
|
Neurological Disease
|
|
Prostaglandin Bx (PGBx) is an oligomer of PGB1 and 15-keto-PGB, which exhibits mitochondrial protective efficacy. Prostaglandin Bx promotes the neurological recovery in rabbits ischemic spinal cord injury model, and maintains the integrity of the gastric mucosa through inhibition of gastric acid secretion in rat gastric ulcer model .
|
-
- HY-116873
-
|
|
COX
|
Inflammation/Immunology
|
|
Flunoxaprofen is an orally active COX inhibitor. Flunoxaprofen shows anti-inflammatory activity in a rat paw edema model. Flunoxaprofen may be used in research on immune system diseases such as arthritis .
|
-
- HY-111258
-
-
- HY-N14176
-
|
|
Bacterial
|
Infection
|
|
Cyathin A3 has weak activity against Gram-positive bacteria, negative bacteria, actinomycetes and dermatophytes, and has anti-ischemia effect (improving cerebral ischemia in rat model) .
|
-
- HY-111219
-
|
NM-702; NT-702
|
Phosphodiesterase (PDE)
|
Others
|
|
Parogrelil (hydrochloride) (NM-702) is a phosphodiesterase inhibitor with activity in inhibiting intermittent claudication. Parogrelil (hydrochloride) selectively inhibits PDE3, inhibits human platelet aggregation in vitro and rat aortic contraction, and improves walking distance and plantar surface temperature in the rat femoral artery ligation model, with better effects than cilostazol.
|
-
- HY-173142
-
|
|
Drug Derivative
|
Neurological Disease
|
|
Neuroprotective agent 7 (Compound 13) is a BBB-penetrable neuroprotective agent. Neuroprotective agent 7 has a powerful neuroprotective effect and can reduce the cerebral infarct area in the MCAO rat model. Neuroprotective agent 7 can be used in the research of diseases such as cerebral ischemia .
|
-
- HY-180882
-
|
EIDD-3608
|
DNA/RNA Synthesis
|
Infection
|
|
GHP-88310 (EIDD-3608) is a potent, orally active orthoparamyxovirus polymerases inhibitor. GHP-88310 exhibits potent activity against HPIV3 and related respiroviruses, measles virus (MeV) and related morbilliviruses. GHP-88310 exhibits efficacy in both canine distemper virus (CDV) ferret models and HPIV3 cotton rat models. GHP-88310 can be used for orthoparamyxovirus disease research .
|
-
- HY-105693
-
|
|
iGluR
|
Neurological Disease
|
|
Fluorofelbamate, a Felbamate (HY-B0184) analog, is a potent NMDA receptor antagonist. Fluorofelbamate exhibits anticonvulsant and antiepileptogenic effects in an experimental rat model of self-sustaining status epilepticus (SSSE). Fluorofelbamate can be used for epilepsy research .
|
-
- HY-105704
-
|
NSC 170955; WA 335
|
5-HT Receptor
|
Neurological Disease
|
|
Danitracen (NSC 170955) is an orally active, CNS penetrant serotonin antagonist with antidepressant activity. Danitracen reduces serotonin levels in the cerebrum, cerebellum, medulla and the whole brain. Danitracen exhibits anticataleptic effects in rat catalepsy models. Danitracen can be used for catalepsy and depression research .
|
-
- HY-12328
-
|
|
Trk Receptor
|
Neurological Disease
|
|
Trk-IN-2 is a pan-Trk kinase inhibitor with a TrkA enzyme IC50 of 9 nM, cell-based IC50 of 7 nM, and oral activity.Trk-IN-2 exhibits pharmacodynamic effects in rat models of inflammatory pain and neuropathic pain.Trk-IN-2 can be used for the research of inflammatory pain, neuropathic pain .
|
-
- HY-176560
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
Cancer
|
|
Raloxifene alkene (Compound 101) is a serum cholesterol clearance agent. Raloxifene alkene has significant anti-proliferation activity against breast adenocarcinoma cells. Raloxifene alkene effectively reduces serum cholesterol level without significant uterine weight and increase of number oieosinoohils in the stromallaver of ovarleclomized rat models. Raloxifene alkene can be used for post-menopausasyndrome, particularly osteoporosis, estrogen-dependent breast and uterine carcinoma research .
|
-
- HY-181094
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-110 is a selective and orally active competitive inhibitor of α-Glucosidase with an IC50 of 7.09 μM and a Ki of 6.9 μM. α-Glucosidase-IN-110 can reduce fasting blood glucose levels, improve glucose tolerance, and restore the histomorphology of liver and pancreatic tissues in diabetic rat models. α-Glucosidase-IN-110 can be used for the research of diabetes .
|
-
- HY-W274652
-
|
IEM-1770
|
iGluR
Drug Derivative
|
Neurological Disease
|
|
Benzylaspartic acid (IEM-1770), a derivative of aspartic acid, is a NMDA agonist. Benzylaspartic acid has antidepressant activity. Benzylaspartic acid blocks alcohol-abstinence syndrome (AAS) development in chronic alcohol drinking rat models. Benzylaspartic acid can be used for depression research .
|
-
- HY-124183
-
|
|
CXCR
|
Inflammation/Immunology
|
|
SX-576 is a CXCR1 and CXCR2 antagonist with IC50 values of 31 nM and 21 nM, respectively. SX-576 inhibits neutrophil infiltration in a rat model of pulmonary inflammation. SX-576 can be used in studies related to pulmonary inflammation .
|
-
- HY-P11584
-
|
|
Amylin Receptor
CGRP Receptor
|
Metabolic Disease
|
|
KBP-066A is a long-acting dual amylin and calcitonin receptor agonist. KBP-066A can activate the CTR and AMY-R potently, with no off-target activity. KBP-066A reduces fasting blood glucose levels, fasting insulin levels, and body weight in diabetic rat models. KBP-066A can be used for the research of type 2 diabetes mellitus, obesity .
|
-
- HY-180807
-
|
|
p38 MAPK
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
ERK
JNK
|
Cardiovascular Disease
Neurological Disease
|
|
MAPK-IN-6 (compound 116B) is a CNS-penetrant compound that inhibits the MAPK signaling pathway. MAPK-IN-6 reduces oxidative stress in SH-SY5Y neuronal cells by reducing ROS, restoring mitochondrial function, and inhibiting MAPK-driven inflammation. MAPK-IN-6 demonstrates profound neuroprotective efficacy in a rat tBCCAO/R model via ERK-P38-JNK signaling. MAPK-IN-6 can be used as a neuroprotective agent in ischemic stroke research .
|
-
- HY-110268
-
|
|
CXCR
|
Inflammation/Immunology
|
|
NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-119058
-
|
CP-744809
|
Aldose Reductase
|
Metabolic Disease
|
|
ARI-809 (CP-744809) is a highly selective, orally active aldose reductase inhibitor with an IC50 of 1 nM. ARI-809 blocks excessive glucose flux through the polyol pathway. ARI-809 normalizes elevated sorbitol and fructose levels in sciatic nerve tissues of diabetic rat models, inhibits sorbitol accumulation in lens tissues, and brings elevated urinary albumin excretion close to normal. ARI-809 can be used in diabetes research .
|
-
- HY-181682
-
|
|
Neurokinin Receptor
|
Endocrinology
|
|
NK3R antagonist-1 is an orally active neurokinin-3 receptor (NK3R) antagonist with an IC50 of 53.61 nM. NK3R antagonist-1 reduces plasma luteinizing hormone (LH) levels in ovariectomized rat models. NK3R antagonist-1 is applicable to research related to menopausal hot flushes .
|
-
- HY-181929
-
|
H018
|
JAK
|
Inflammation/Immunology
|
RAI-20 (H018) is an orally active JAK1/JAK2 dual inhibitor (IC50=15.1 and 22.7 nM). RAI-20 exhibits excellent pharmacokinetic properties, including plasma stability, systemic exposure, and a long half-life. In a collagen-induced arthritis rat model, RAI-20 shows significant anti-inflammatory and anti-arthritic activities, effectively reducing paw swelling volume and arthritis index. RAI-20 can be used for research on the pathogenesis of rheumatoid arthritis .
|
-
- HY-148479
-
|
|
Biochemical Assay Reagents
|
Infection
|
|
Bixalomer is a phosphate binder. Bixalomer can improve hyperphosphatemia in chronic kidney disease (CKD) rat model. Bixalomer reduces plasma phosphorus level in CKD rat models through binding phosphate in small intestine and reduces phosphate absorption. Bixalomer can be studied in research on hyperphosphatemia .
|
-
- HY-171478
-
|
|
Drug Derivative
|
Others
|
|
SQ 11,447 is a methylurea analogue that demonstrates remarkable resistance to hydrolysis in both in vitro (rat, dog, and human liver homogenates) and in vivo (rat) experimental models.
|
-
- HY-115596
-
|
|
Calcium Channel
|
Neurological Disease
|
|
BTT-369 is a CaVα1·CaVβ3 protein-protein complex antagonist with a Ki of 2.0 μM. BTT-369 inhibits CaV2.2 currents, with an apparent IC50 value of 31 μM. BTT-369 disrupts the interaction between CaVα1 and CaVβ3 subunits. BTT-369 reduces the current density of CaV2.2, and shifts the voltage dependence of steady-state inactivation and activation of CaV2.2 to more positive potentials. BTT-369 alleviates mechanical hyperalgesia in a rat model of tibial nerve injury. BTT-369 can be used for the study of neuropathic pain .
|
-
- HY-B2079
-
-
- HY-181646
-
|
|
Phosphodiesterase (PDE)
TNF Receptor
|
Inflammation/Immunology
|
|
PDE4-IN-34 is a phosphodiesterase 4 (PDE4) inhibitor, with IC50 values of 19 pM and 14 pM against PDE4B1 and PDE4D2, respectively. PDE4-IN-34 shows weak inhibitory activity against PDE8A1, with an IC50 value of 4.092 μM, and exhibits significant selectivity over other subtypes (IC50 > 10 μM). PDE4-IN-34 improves pulmonary function, reduces inflammatory responses and alleviates lung tissue damage in a rat model induced by cigarette smoke combined with LPS (HY-D1056). PDE4-IN-34 can be used for research related to chronic obstructive pulmonary disease .
|
-
- HY-106111A
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Nafagrel hydrochloride is a thromboxane A2 synthetase inhibitor. Nafagrel hydrochloride can prevent the accumulation of thrombus material in a rat model of acute arterial thrombosis .
|
-
- HY-U00075A
-
|
|
Biochemical Assay Reagents
|
Infection
|
|
Indanazoline (hydrochloride) is an orally active imidazoline derivative. Indanazoline (hydrochloride) has a LD50 of 481 mg/kg in rat model. Indanazoline (hydrochloride) can be studied in research on rhinitis .
|
-
- HY-N14177
-
|
|
Bacterial
|
Infection
|
|
Cyathin A4 has weak activity against Gram-positive bacteria, negative bacteria, actinomycetes and dermatophytes, and has anti-ischemia effect (improving cerebral ischemia in rat model) .
|
-
- HY-U00134A
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
Bencyclane (fumarate) is a vasodilating calcium channel blocker. Bencyclane (fumarate) can attenuate mucosal damage in intestinal ischaemia reperfusion injury rat model. Bencyclane (fumarate) can be studied in research on peripheral arterial occlusice diseases .
|
-
- HY-19078
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
SQ-30741 is a thromboxane A2 receptor antagonist. SQ-30741 reduces vasoconstriction in a feline pulmonary vascular bed model. SQ-30741 increases relaxation of aortic endothelium and vascular smooth muscle in adult rats in a spontaneously hypertensive rat model. SQ-30741 can be used in research on cardiovascular diseases such as hypertension .
|
-
- HY-128326
-
|
|
MAP3K
|
Cardiovascular Disease
|
|
ZAK-IN-1 is an orally active and selective selective leucine-zipper and sterile‑α motif kinase (ZAK) inhibitor with IC50 of 4 nM and KD of 8 nM. ZAK-IN-1 exhibits excellent selectivity against a panel of 403 wild-type kinases. ZAK-IN-1 blocks p38/GATA-4 and JNK/c-Jun signaling and shows promising anti antihypertrophic cardiomyopathy (HCM) efficacy. ZAK-IN-1 can be used for the study of HCM .
|
-
- HY-174986
-
|
|
CGRP Receptor
|
Cardiovascular Disease
|
|
CGRP antagonist 7 is a potent calcitonin gene-related peptide receptor (CGRP) antagonist with a Ki of 0.029 nM. CGRP antagonist 7 Inhibit the production of cyclic adenosine monophosphate (cAMP) with an IC50 of 1.5 nM. CGRP antagonist 7 can be used for the study of migraine .
|
-
- HY-N2493
-
Lawsone
2 Publications Verification
|
Fungal
Apoptosis
|
Infection
Cancer
|
|
Lawsone is an orally active naphthoquinone dye that can be isolated from the leaves of Lawsonia inermis. Lawsone can induce apoptosis. Lawsone has antibacterial, antitumor and antioxidant activities. Lawsone can be used in anti-tumor drug research .
|
-
- HY-169780
-
|
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
|
(S)-AMG-628 (Compound 16q) is the S-isomer of AMG-628 (HY-123374). (S)-AMG-628 is the orally active antagonist for TRPV1, that inhibits the Capsaicin (HY-10448)- and acid-induced Ca 2+-influx with IC50 of 7 nM and 5 nM in CHO cell. (S)-AMG-628 ameliorates Capsaicin-induced rats flinching, and reverses the thermal hypersensitivity in CFA-(HY-153808) induced inflammatory pain models .
|
-
- HY-N2493R
-
|
|
Reference Standards
Fungal
Apoptosis
|
Infection
Cancer
|
|
Lawsone is an orally active naphthoquinone dye that can be isolated from the leaves of Lawsonia inermis. Lawsone can induce apoptosis. Lawsone has antibacterial, antitumor and antioxidant activities. Lawsone can be used in anti-tumor drug research .
|
-
- HY-15451R
-
|
BZO-HEXOXIZID (Standard)
|
Reference Standards
Cannabinoid Receptor
|
Neurological Disease
|
|
MDA 19 (Standard) is the analytical standard of MDA 19. This product is intended for research and analytical applications. MDA 19 is a potent and selective agonist of human cannabinoid receptor 2 (CB2), with a Ki of 43.3 nM. MDA 19 has antiallodynic effects in a rat model of neuropathic pain and does not affect rat locomotor activity .
|
-
- HY-119580B
-
|
2,3-trans-3,4-trans-Leucocyanidin; 3,4-trans-Leucocyanidin; (2R,3S,4R)-Leucocyanidin
|
Drug Isomer
|
Inflammation/Immunology
|
|
(+)-Leucocyanidin is the isoform of Leucocyanidin (HY-119580), is an active anti-ulcerogenic ingredient was extracted from Litchi Chinensis. Leucocyanidin demonstrates a significant protective effect against Aspirin-induced erosions in rat models .
|
-
- HY-164040
-
|
|
Somatostatin Receptor
|
Metabolic Disease
|
|
Zavolosotine (Compound 1) is an orally active agonist for somatostatin receptor type 5 (SST5) with EC50 <1 nM. Zavolosotine inhibits insulin and glucagon secretion, increases levels of glucagon in blood in rat model .
|
-
- HY-161705
-
|
|
Apoptosis
|
Neurological Disease
|
|
Anti-apoptotic agent 1 (Compound B4) exhibits neuroprotective activity and good pharmacokinetic properties. Anti-apoptotic agent 1 inhibits apoptosis, prevents stroke recurrence in photothrombotic rat model .
|
-
- HY-116638
-
|
|
Lipoxygenase
|
Endocrinology
|
|
AHR-5333 is a selective human blood neutrophil 5-lipoxygenase inhibitor. AHR-5333 exhibits potent, long-acting activity in rat and guinea pig in vivo models of immediate hypersensitivity .
|
-
- HY-142123
-
|
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
|
Fluocortolone is an orally active anti-inflammatory agent that effectively reduces plasma fibrinogen levels. Fluocortolone inhibits Mycobacterium butyricum-induced foot edema in a rat model of adjuvanted joint inflammation (3-12 mg/kg) .
|
-
- HY-129103
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-412997 is a selective Dopamine D4 agonist with Ki values of 12 and 7.9 nM for the rat and human receptors. A-412997 improves short term memory and cognitive properties in rodent models .
|
-
- HY-106780
-
|
DQ 2511
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Ecabapide (DQ 2511) is an orally active gastroprokinetic agent. Ecabapide can ameliorate gastric emptying of stroke-prone spontaneously hypertensive rat model. Ecabapide can be studied in research on autonomic nervous system disorder .
|
-
- HY-131545
-
|
NT-702 free base; NT-702 free base
|
Phosphodiesterase (PDE)
|
Others
|
|
Parogrelil (NT-702 free base) is a compound with intermittent claudication inhibitory activity that inhibits PDE3, inhibits platelet aggregation and vasoconstriction, and improves walking distance and plantar surface temperature in a rat experimental model.
|
-
- HY-173083
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
MDA7 is the selective agonist for cannabinoid receptor 2 with EC50 of 128 nM and 67.4 nM in human CB2 receptor and rat CB2 receptor. MDA7 exhibits good affinity to human CB2 receptor and rat CB2 receptor with Ki of 422 nM and 238 nM. MDA7 exhibits analgesic activity in rats models .
|
-
- HY-P3719
-
|
|
CCR
|
Inflammation/Immunology
|
|
MOG (35-55) amide, mouse, rat the terminal amidation form of the 35-55 fragment of the myelin oligodendrocyte glycoprotein (MOG) immunogenic peptide (MOG (35-55) (HY-P1240)). MOG(35-55) amide, mouse, rat can be used for experimental autoimmune encephalomyelitis (EAE) modeling .
|
-
- HY-150192
-
|
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
|
Talsupram is a selective noradrenaline inhibitor that has a high affinity for the noradrenaline transporter. Talsupram exhibits anti-hyperalgesic effects. Talsupram can decrease ethanol intake to the levels prior to REM-induced deprivation in rat model .
|
-
- HY-130301
-
-
- HY-119279
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
VUF 10214 is a H4 receptor ligand with a pKi of 8.25. VUF 10214 exhibits significant anti-inflammatory activity in a carrageenan-induced paw edema rat model and can be used for research in the field of inflammatory diseases .
|
-
- HY-P1240
-
|
Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat
|
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
|
MOG (35-55) mouse, rat (Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat) is a minor component of CNS myelin. MOG (35-55) mouse, rat has encephalitogenic activity and induces T cell proliferative. MOG (35-55) mouse, rat induces Th1 cytokine response as well as relatively high levels of IgG antibodies. MOG (35-55) mouse, rat produces a relapsing-remitting neurological disease with extensive plaque-like demyelination. MOG (35-55) mouse, rat (MOG (35-55)) can be used for experimental autoimmune encephalomyelitis (EAE) modeling .
|
-
- HY-123889
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
VK4-116 (Compound 19) is a selective Dopamine D3 receptor (D3R) antagonist with a Ki of 6.84 nM.VK4-116 significantly inhibits Oxycodone-induced hyperlocomotion and locomotor sensitization in mouse models. VK4-116 with pretreatment also inhibits the acquisition of Oxycodone-induced conditioned place preference (CPP) in rat models .
|
-
- HY-178153
-
|
|
iGluR
|
Neurological Disease
|
|
BPAM363 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. BPAM363 selectively potentiates AMPAR activity in human and rat models, with an EC2x value of 0.96 μM in rat embryonic cortex primary neurons. BPAM363 upregulates BDNF protein expression in rat primary cortical neuronal cultures. BPAM363 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. BPAM363 can be used for the study of cognitive disorders .
|
-
- HY-116638A
-
|
|
Lipoxygenase
|
Endocrinology
|
|
AHR-5333 mandelate is a selective human blood neutrophil 5-lipoxygenase inhibitor. AHR-5333 mandelate exhibits potent, long-acting activity in rat and guinea pig in vivo models of immediate hypersensitivity .
|
-
- HY-14458
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
SCH-1518291 (Compound 27) is an orally active PDE10A inhibitor. SCH-1518291 exhibits antipsychotic activity in an ADHD rat model. SCH-1518291 can be used in research on neurological disorders such as psychosis .
|
-
- HY-121191
-
|
N1,N8-Bisnorcymserine; (-)-Bisnorcymserine
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Bisnorcymserine ((-)-Bisnorcymserine) is an inhibitor for butyrylcholinesterase (BChE) with an IC50 of 0.228 nM. Bisnorcymserine reduces the levels of amyloid-β peptide (Aβ), exhibits ameliorates the Alzheimer’s Disease in elderly rat models. Bisnorcymserine is blood-brain barrier penetrate .
|
-
- HY-W754020
-
|
|
Histamine Receptor
|
Others
|
|
Elbanizine inhibits histamine, bradykinin, histamin-release from rat mast cells (IC50 of 0.26 μM) and the IgE-mediated passive cutaneous anaphylaxis (PCA) reaction. Elbanizine exhibits antiallergic and antiasthmatic in guinea pig model .
|
-
- HY-119298
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
AW-814141 is a selective and orally active p38 MAP kinase inhibitor. AW-814141 has an IC50 values of 100 nM and 158 nM for p38-α and β isoforms, respectively. AW-814141 can inhibit the production of TNF-α induced by LPS (HY-D1056). AW-814141 can inhibit paw edema in rats in a dose-dependent manner. AW-814141 exhibits anti-inflammatory activity and can be used in the research of inflammatory diseases such as rheumatoid arthritis .
|
-
- HY-177691
-
-
- HY-P1010
-
Z-LEHD-FMK
Maximum Cited Publications
15 Publications Verification
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
|
Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-120481
-
|
|
FAAH
|
Neurological Disease
|
|
JNJ-40413269 is an inhibitor for FAAH, that inhibits human FAAH and rats FAAH with IC50 of 28 nM and 270 nM. JNJ-40413269 exhibits analgesic efficacy in rat spinal nerve ligation model and exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-106468
-
|
FM-24
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Bornaprolol (FM-24) is a β-adrenoceptor antagonist. Bornaprolol significantly depresses plasma levels of luteinizing hormone (LH) in orchidectomized rat models. Bornaprolol can be used for cardiovascular diseases like hypertension and angina pectoris research .
|
-
- HY-179458
-
-
- HY-B0954A
-
|
|
mAChR
|
Endocrinology
|
|
Oxyphencyclimine is an orally active muscarinic receptor (mAChR) antagonist. Oxyphencyclimine is effective in reducing ulceration index and increasing pepsin activity in rat gastric ulcer model. Oxyphencyclimine can be used in studies of peptic ulcer disease and gastrointestinal spasm .
|
-
- HY-13762
-
|
|
Cytochrome P450
|
Cancer
|
|
Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
- HY-404056
-
-
- HY-108744
-
|
|
HMG-CoA Reductase (HMGCR)
|
Cardiovascular Disease
|
|
Pitavastatin magnesium is an orally active HMG-CoA Reductase inhibitor. Pitavastatin magnesium lowers total cholesterol and low-density lipoprotein cholesterol in a hyperlipidemic rat model. Pitavastatin magnesium can be used in research on cardiovascular and cerebrovascular diseases such as hyperlipidemia .
|
-
- HY-13762A
-
|
|
Cytochrome P450
|
Cancer
|
|
Tesmilifene hydrochloride is an antihistamine agent and a chemical sensitizer. Tesmilifene hydrochloride targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene hydrochloride overcomes multidrug resistance .
|
-
- HY-148258
-
-
- HY-101666R
-
|
|
Deubiquitinase
Reference Standards
Apoptosis
MDM-2/p53
|
Metabolic Disease
Cancer
|
|
HBX 41108 (Standard) is the analytical standard of HBX 41108 (HY-101666). This product is intended for research and analytical applications. HBX 41108 is an inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 424 nM. HBX 41108 inhibits USP7-mediated p53 deubiquitination to stabilize p53 and inhibits cancer cell growth. BX 41108 can be used in cancer and diabetes research .
|
-
- HY-101666
-
|
|
Deubiquitinase
Apoptosis
MDM-2/p53
|
Metabolic Disease
Cancer
|
|
HBX 41108 is an inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 424 nM. HBX 41108 inhibits USP7-mediated p53 deubiquitination to stabilize p53 and inhibits cancer cell growth. BX 41108 can be used in cancer and diabetes research .
|
-
- HY-163756
-
-
- HY-158056
-
|
|
GLUT
URAT1
|
Metabolic Disease
|
|
URAT1/GLUT9-IN-1 (compound 29) can inhibit both uric acid transporter 1 (URAT1) (IC50=2.01 μM) and glucose transporter 9 (GLUT9) (IC50=18.21 μM). URAT1/GLUT9-IN-1 exhibits favorable pharmacokinetic properties and oral bioavailability. URAT1/GLUT9-IN-1 can be uesd for gout and hyperuricemia research .
|
-
- HY-147719
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity .
|
-
- HY-163148
-
-
- HY-12694
-
|
R-108512
|
5-HT Receptor
Apoptosis
Autophagy
|
Metabolic Disease
Cancer
|
|
Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
|
-
- HY-12694R
-
|
R-108512 (Standard)
|
5-HT Receptor
Apoptosis
Autophagy
Reference Standards
|
Metabolic Disease
Cancer
|
|
Prucalopride (succinate) (Standard) is the analytical standard of Prucalopride (succinate). This product is intended for research and analytical applications. Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
|
-
- HY-B0647A
-
-
- HY-163368
-
|
|
HDAC
|
Inflammation/Immunology
|
|
HDAC6-IN-34 (compound 21) is an oral active and selective HDAC6 inhibitor with the IC50 of 18 nM. HDAC6-IN-34 increases the acetylation level of tubulin without affecting histone acetylation in cutaneous T-cell lymphoma cells and inhibits TNF-α secretion in LPS (HY-D1056)-stimulated macrophage cells. HDAC6-IN-34 shows excellent anti-arthritic efficacy in rat .
|
-
- HY-116208
-
|
KU-1257
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Dalcotidine (KU-1257) is an orally active and competitive histamine H2 receptor antagonist. Dalcotidine promotes the healing of chronic ulcers and inhibits gastric acid secretion .
|
-
- HY-N0430
-
|
Coptisin
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
|
-
- HY-B2141
-
|
|
NO Synthase
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
Others
Metabolic Disease
|
|
Bendazol is an orally effective antihypertensive agent. Bendazol acts directly on vascular smooth muscle to dilate blood vessels and reduce peripheral resistance, thereby improving blood circulation. Bendazol significantly inhibits the development of myopia in rabbit models. Bendazol can regulate kidney function by increasing the activity of NO synthase in the rat model of nephrogenic hypertension. In addition, Bendazol has an effect on sexual behavior and spermatogenesis in male rats .
|
-
- HY-159634
-
|
|
COX
|
Inflammation/Immunology
|
|
Zidometacin is a nonsteroidal anti-inflammatory agent. Zidometacin significantly inhibits prostaglandin synthesis with low gastrolesive influence. Zidometacin has antinociceptive and antipyretic activities and shows relatively low ulcerogenicity in rat models. Zidometacin can be used for analgesia and osteoarthritis research .
|
-
- HY-14886
-
|
MEN16132 free base
|
Bradykinin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model .
|
-
- HY-19590
-
|
Ro 15-1570
|
Drug Derivative
|
Cancer
|
|
Etarotene (Ro 15-1570) is a derivative of Arotinoid (HY-106735). Etarotene is an orally active antitumor agent against DMBA (HY-W011845)-induced mammary tumor and causes toxic symptoms of hypervitaminosis A in rat model .
|
-
- HY-129736A
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
P32/98 a potent inhibitor of dipeptidyl peptidase IV with a Ki value of 130 nM. P32/98 improves glucose tolerance, insulin sensitivity and β-cell responsiveness in fatty Zucker rat model .
|
-
- HY-P11480
-
|
|
Trk Receptor
|
Neurological Disease
|
|
TrkA/NGF-IN-1 (Peptide 19) is an inhibitor of protein-protein interactions between TrkA and NGF (IC50: 21 nM for human TrkA in PathHunter assay). TrkA/NGF-IN-1 shows an analgesic effect in a rat incisional pain model .
|
-
- HY-19225
-
|
KA-672 hydrochloride; Anseculin hydrochloride
|
iGluR
|
Neurological Disease
|
Ensaculin is an NMDA receptor channel blocker. Ensaculin has neuroprotective effects in NMDA toxicity models and promotes neuronal growth in primary cultures of rat brain cells. Ensaculin has the potential to be developed as an anti-dementia drug that acts on various neurotransmitter systems .
|
-
- HY-110180
-
|
|
mGluR
|
Neurological Disease
|
|
VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .
|
-
- HY-P1010A
-
|
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
|
Z-LEHD-FMK TFA is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK TFA exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-18734
-
-
- HY-111131
-
|
|
Melanocortin Receptor
|
Metabolic Disease
|
|
RY746 is a selective MC4R agonist, with an EC50 of 10 nM. RY764 effectively inhibits food intake and reduces body weight gain in diet-induced obese (DIO) rat models. RY764 can be used for the study of obesity .
|
-
- HY-14364
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model .
|
-
- HY-127165
-
|
HP 029 free base; Hydroxytacrine
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Velnacrine (HP 029 free base) is an inhibitor for acetylcholinesterase (AChE), with an IC50 of 3.27 μM. Velnacrine reverses the Scopolamine (HY-N0296)-induced amnesia in rat models, and exhibits acute toxicity with LD50 of 65 mg/kg .
|
-
- HY-18734A
-
-
- HY-B1619R
-
|
Cromoglycate (Standard); Cromoglicic acid (Standard); FPL-670 free acid (Standard)
|
GSK-3
NF-κB
Amyloid-β
Reference Standards
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Cromolyn (Standard) is the analytical standard of Cromolyn. This product is intended for research and analytical applications. Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects .
|
-
- HY-B0320A
-
|
Cromoglycate disodium; Cromoglicic acid disodium; FPL-670
|
GSK-3
NF-κB
Amyloid-β
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Cromolyn (Cromoglycate) disodium is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn disodium is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn disodium can be used in the research of bronchial asthma. In addition, Cromolyn disodium has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects .
|
-
- HY-B1619
-
|
Cromoglycate; Cromoglicic acid; FPL-670 free acid
|
GSK-3
NF-κB
Amyloid-β
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Cromolyn (Cromoglycate) is an orally active GSK-3β inhibitor with an IC50 of 2.0 μM. Cromolyn is also a mast cell stabilizer that can inhibit the release of mediators from mast cells, regulate reflex bronchoconstriction, and reduce non-specific bronchial hyperreactivity, and Cromolyn can be used in the research of bronchial asthma. In addition, Cromolyn has multiple activities such as anti-inflammatory, anti-allergic, anti-histamine, anti-cancer, and neuroprotective effects .
|
-
- HY-119805
-
|
|
Others
|
Inflammation/Immunology
|
|
YM 13650 is an orally active anti-nephritic agent. YM 13650 exhibits dose-dependent preventive and therapeutic effects in both the rat immune complex nephritis model and the mouse spontaneous lupus nephritis model. YM 13650 can inhibit the increase in urinary protein, improve serum cholesterol and urea nitrogen levels, alleviate renal pathological damage, and prolong the survival time of mice. YM 13650 can be used in the research of nephritic diseases .
|
-
- HY-170918
-
|
|
Potassium Channel
|
Others
|
|
BKCa activator-1 (Compound 51b) is the orally active activator for the calcium-activated potassium channel BKCa with an EC50 of 2.82 μM. BKCa activator-1 increases K+ efflux, leads to cell membrane hyperpolarization, thereby inhibiting smooth muscle contraction. BKCa activator-1 alleviates urinary incontinence in spontaneously hypertensive rat (SHR) model, exhibits antitussive effect in puinea pig cough model .
|
-
- HY-P992082
-
|
|
VEGFR
|
Cancer
|
|
Anti-Human/Rat VEGF Antibody (A.4.6.1) is an antibody targeting human and rat vascular endothelial growth factor (VEGF) that potently inhibits tumor growth in various animal models. Anti-Human/Rat VEGF Antibody (A.4.6.1) is the parent antibody of Bevacizumab (HY-P9906), and it exhibits high affinity and high selectivity for binding to human VEGF . The isotype control for Anti-Human/Rat VEGF Antibody (A.4.6.1) is Mouse IgG1 kappa, Isotype Control (HY-P99977).
|
-
- HY-P3199
-
|
|
PKC
|
Inflammation/Immunology
|
|
PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction .
|
-
- HY-129736
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
P32/98 hemifumarateis a potent inhibitor of dipeptidyl peptidase IV with a Ki value of 130 nM. P32/98 hemifumarate improves glucose tolerance, insulin sensitivity and β-cell responsiveness in fatty Zucker rat model .
|
-
- HY-159090
-
|
|
Calcium Channel
Angiotensin Receptor
|
Cardiovascular Disease
|
|
AT1R antagonist 3 (Compound 1) is an antagonist for angiotensin II type 1 receptor (AT1R) and an inhibitor for calcium channel type-L CaV1.2 (IC50=0.57 μM). AT1R antagonist 3 exhibits vasodilation efficacy in solated rat aorta (10 μM, 88.7%) and antihypertensive efficacy in rat models .
|
-
- HY-162650
-
|
|
ClpP
|
Cancer
|
|
SL44 is an agonist for human caseinolytic protease P (HsClpP), with an EC50 of 1.30 μM. SL44 inhibits the proliferation of LM3 with an IC50 of 3.1 μM. SL44 induces apoptosis in HCC cells, through the degradation of respiratory chain complex subunits. SL44 exhibits antitumor efficacy in mouse models without obvious toxicity (LD50=400 mg/kg). SL44 exhibits good pharmacokinetic characters in rat models .
|
-
- HY-170499
-
|
BI02982816
|
mGluR
|
Neurological Disease
|
|
VU6024578 (BI02982816) is a selective, orally active positive allosteric modulator (PAM) for metabotropic glutamate receptor (mGluR1), that activates human mGluR1 and rat mGluR1 with EC50 of 54 nM and 46 nM. VU6024578 exhibits antipsychotic activity in rats amphetamine-induced hyperactivity models and MK-801 (HY-15084B)-induced novel object recognition (NOR) models. VU6024578 is blood brain barrier penetrable .
|
-
- HY-14474
-
|
|
Endothelin-Converting Enzyme (ECE)
|
Cardiovascular Disease
|
|
CGS 26303 is an endothelin-converting enzyme (ECE) inhibitor. CGS 26303 increases the expression of endothelin-converting enzyme-1 in endothelial cells. CGS 26303 attenuates cerebral vasospasm in a rabbit subarachnoid hemorrhage model. CGS 26303 improves birth survival and alleviates pulmonary hypoplasia in newborn rats in a rat model of congenital diaphragmatic hernia. CGS 26303 can be used for research on cardiovascular and cerebrovascular diseases and congenital diaphragmatic hernia .
|
-
- HY-162511
-
|
|
Dopamine Transporter
Serotonin Transporter
|
Others
|
|
IP2015 is an inhibitor for monoamine reuptake, that inhibits the reuptake of dopamine, serotonin (5-HT), and noradrenaline. IP2015 increases release of central dopamine and peripheral nitric oxide (NO), causes the NO-mediated relaxation of erectile tissue, and thus induces erection in rat model .
|
-
- HY-P3498
-
|
ZP1846
|
GCGR
|
Others
|
|
Elsiglutide (ZP1846) is a GLP-2 analogue, an orally active and selective GLP-2 receptor agonist, increases cell proliferation and reduces apoptosis in the intestine. Elsiglutide improves Lapatinib (HY-50898)-induced diarrhoea in rat model .
|
-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-Y0816
-
|
|
Biochemical Assay Reagents
|
Others
|
|
(S)-Mandelic Acid is a (S)-enantiomer of Mandelic Acid (HY-W015591). (S)-Mandelic Acid undergoes one-directional chiral inversion to (R)-Mandelic Acid in rat models. (S)-Mandelic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
|
-
- HY-10427
-
|
NRI-022
|
Histone Methyltransferase
|
Neurological Disease
|
|
WAY-260022 is a selective norepinephrine reuptake inhibitor with potent inhibitory activity on norepinephrine reuptake. WAY-260022 exhibits excellent selectivity in inhibiting serotonin and dopamine transporters. WAY-260022 also showed oral efficacy in a rat model of thermoregulatory dysfunction .
|
-
- HY-163702
-
|
|
Adrenergic Receptor
mAChR
|
Inflammation/Immunology
|
|
CHF-6550 is an antagonist for muscarinic M3 receptor and an agonist for β2 adrenoceptor (MABA), with pKi of 9.3 and 10.6, respectively. CHF-6550 exhibits good hepatocyte clearance in rat models and good pharmacokinetic characteristics in guinea pigs .
|
-
- HY-161896
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Transcription factor-IN-1 (Compound 4e) is an inhibitor for transcription factor. Transcription factor-IN-1 exhibits anticonvulsant activity by antagonism with pentylenetetrazole (PTZ) (ED50 =34.5 mg/kg). Transcription factor-IN-1 exhibits antidepressant effects in rat models .
|
-
- HY-159928
-
-
- HY-119035
-
|
|
Platelet-activating Factor Receptor (PAFR)
|
Inflammation/Immunology
|
|
R-75317 is a specific platelet-activating factor (PAF) antagonist. R-75317 can prevent the decline in creatinine clearance (Ccr) in a rat model of glomerulonephritis induced by the injection of antibodies extracted from rabbits against rat glomerular basement membrane (GBM) antigens, delay the onset of proteinuria, and improve glomerular hypertrophy, mesangial matrix proliferation, and interstitial fibrosis. R-75317 may be useful in the study of glomerulonephritis .
|
-
- HY-107969
-
|
|
Dopamine Receptor
COX
NO Synthase
|
Neurological Disease
Cancer
|
|
Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. Haloperidol decanoate can increase the striatal D2 receptor in rat. Haloperidol decanoate can improve conditions of psychoses (mainly schizophrenia). Haloperidol decanoate can lead to increased accumulation of the dopamine metabolites homo-vanillic acid. Haloperidol decanoate can reduce intestinal transport, increase gastric emptying and reduce acid output in rat model .
|
-
- HY-107054
-
|
ETC-1001
|
PPAR
|
Cardiovascular Disease
|
|
ESP-31015 (ETC-1001) is an orally active and non-fibrate based PPARα agonists. ESP-31015 demonstrates significant lipid-regulating effects in the obese Zucker rat model. ESP-31015 can be used in cardiovascular disease research .
|
-
- HY-164605
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Metabolic Disease
|
|
(6S)-CP-470711 (Compound 8) is an inhibitor for sorbitol dehydrogenase, that inhibits human and rat SDH with IC50 of 19 nM and 27 nM. (6S)-CP-470711 ameliorates the Streptozotocin (HY-13753)-induced diabetes in rats models .
|
-
- HY-131416
-
|
|
Others
|
Inflammation/Immunology
|
|
DD-3305 is an anti-inflammatory agent with comparable anti-inflammatory activity to the known anti-inflammatory agent indomethacin (HY-14397). In a carrageenin-induced rat inflammation model, DD-3305 was effective in inhibiting chronic and acute inflammation as well as induced allergies. .
|
-
- HY-W423707
-
|
|
VEGFR
|
Cardiovascular Disease
|
|
TG 100948 is a dual VEGFR and tyrosine kinase Src inhibitor. TG 100948 reduces retinal edema and retinal thickening, and eliminates bullous edema cysts in a rat model of ischemic retinal vein occlusion. TG 100948 can be used for the research of ischemic retinal vein occlusion .
|
-
- HY-106751
-
|
|
Progesterone Receptor
|
Endocrinology
|
|
Anordrin is a contraceptive agent. Anordrin exhibits estrogenicites and can induce decrease in serum progesterone levels in rat models. Anordrin inhibits endometrial epithelial cell mitosis and NAFLD induced by Tamoxifen (HY-13757A) in mouse uterus and liver as an anti-estrogenic and estrogenic agent .
|
-
- HY-119680
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
AT-1459 is a selective and orally active direct Thrombin inhibitor with a Ki value of 4.9 nM. AT-1459 exhibits excellent antithrombotic activity in both rat models of venous and arterial thrombosis. AT-1459 can be used for research on thrombosis-related diseases .
|
-
- HY-100834A
-
|
5,7-DCKA sodium
|
iGluR
|
Neurological Disease
|
|
5,7-Dichlorokynurenic acid (5,7-DCKA) sodium is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid sodium reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid sodium increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid sodium exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
|
-
- HY-100834
-
|
5,7-DCKA
|
iGluR
|
Neurological Disease
|
|
5,7-Dichlorokynurenic acid (5,7-DCKA) is a selective and competitive antagonist of the glycine site on NMDA receptor with a KB of 65 nM. 5,7-Dichlorokynurenic acid reduces NMDA-induced neuron injury. 5,7-Dichlorokynurenic acid increases social interaction time, increases open arm exploration time, disinhibits suppressed conflict responding in rodent models. 5,7-Dichlorokynurenic acid exhibits anxiolytic-like activity in rodent models and supports exploration of glycine’s role in NMDA receptor-mediated synaptic transmission .
|
-
- HY-B1279A
-
|
Dipyrone; Methamizole sodium
|
COX
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Metamizole sodium (Dipyrone) is an orally active cyclooxygenase (COX) inhibitor. Metamizole sodium can inhibit cell proliferation and promote cell apoptosis. Metamizole sodium has anti-inflammatory and antioxidant activities. Metamizole sodium is an antipyretic, analgesic and spasmolytic agent. .Metamizole sodium can be used in research to relieve a variety of pain .
|
-
- HY-B1279
-
|
Dipyrone hydrate; Methamizole sodium hydrate
|
COX
Apoptosis
|
Inflammation/Immunology
|
|
Metamizole sodium hydrate (Dipyrone) is an orally active cyclooxygenase (COX) inhibitor.. Metamizole sodium hydrate can inhibit cell proliferation and promote cell apoptosis. Metamizole sodium hydrate has anti-inflammatory and antioxidant activities. Metamizole sodium hydrate is an antipyretic, analgesic and spasmolytic agent. Metamizole sodium hydrate can be used in research to relieve a variety of pain .
|
-
- HY-B1279R
-
|
Dipyrone hydrate (Standard); Methamizole sodium hydrate (Standard)
|
Reference Standards
COX
Apoptosis
|
Inflammation/Immunology
|
|
Metamizole (sodium hydrate) (Standard) is the analytical standard of Metamizole (sodium hydrate). This product is intended for research and analytical applications. Metamizole sodium hydrate (Dipyrone) is an orally active cyclooxygenase (COX) inhibitor.. Metamizole sodium hydrate can inhibit cell proliferation and promote cell apoptosis. Metamizole sodium hydrate has anti-inflammatory and antioxidant activities. Metamizole sodium hydrate is an antipyretic, analgesic and spasmolytic agent. Metamizole sodium hydrate can be used in research to relieve a variety of pain .
|
-
- HY-138063
-
|
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Siegeskaurolic acid is an orally active anti-inflammatory agent. Siegeskaurolic acid inhibits the productions of nitric oxide (NO), prostaglandin E(2) (PGE(2)), tumor necrosis factor-alpha (TNF-alpha) and the activationon of nuclear factor-kappaB .
|
-
- HY-13224
-
|
|
Kinesin
Apoptosis
Mitosis
|
Cancer
|
|
AZD4877 is another isostere to Ispinesib (HY-50759)and also a kinesin spindle protein (Eg5) inhibitor with IC50 of 2 nM.AZD4877 arrests cell mitosis, leads to the formation of the monopolar spindle phenotype and induces apoptosis. AZD4877 inhibits circulating peripheral blood mononuclear cells (PBMCs) and has anti-cancer activity .
|
-
- HY-177506
-
|
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
FE100726 (Compound 39) is a Cholecystokinin 2 (CCK2) receptor agonist. FE100726 has a superior binding capacity on CCK2 receptor. FE100726 can induce gastric acid secretion in anaesthetized rat models. FE100726 can be used for diabetes research .
|
-
- HY-A0119
-
|
Sodium nitroprusside dihydrate; Sodium Nitroferricyanide(III) Dihydrate
|
Autophagy
|
Cardiovascular Disease
Cancer
|
|
Nitroprusside disodium dehydrate (Sodium nitroprusside dihydrate) is a vasodilator that available for the research of acute hypertension, heart failure. Nitroprusside disodium dehydrate induces autophagy in glutathione-depleted osteoblasts. Nitroprusside disodium dehydrate acts as a nitric oxide (NO) donor in a rat intestinal ischemia reperfusion model .
|
-
- HY-110157
-
|
|
Estrogen Receptor/ERR
|
Neurological Disease
|
|
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender selective neuroprotective effects in a male rat model of Parkinson's disease .
|
-
- HY-124378
-
|
|
MAGL
|
Inflammation/Immunology
|
|
MAGL-IN-17 (Compound ) is an inhibitor for MAGL with a Ki of 0.4 μM. MAGL-IN-17 inhibits mouse MAGL and rat MAGL with IC50 of 0.18 and 0.24 μM. MAGL-IN-17 exhibits anti-inflammatory activity in mouse experimental autoimmune encephalitis models .
|
-
- HY-107510
-
|
|
mGluR
|
Neurological Disease
|
|
YM-230888 is an orally active, selective and allosteric mGlu1 receptor antagonist with a Ki of 13 nM. YM-230888 inhibits mGlu1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 13 nM. YM-230888 shows antinociceptive response in Streptozotocin (HY-13753)-induced hyperalgesia models. YM-230888 significantly reduces pain parameters in complete Freund's adjuvant (HY-153808)-induced arthritic pain models .
|
-
- HY-120615
-
|
|
LPL Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
BMS-520 is a potent, orally active and selective sphingosine-1-phosphate 1 (S1P1) agonist with an EC50 of 0.47nM. BMS-520 shows ~3400-fold selectivity over S1P3. BMS-520 demonstrates impressive efficacy in a rat model of arthritis and in a mouse experimental autoimmune encephalomyelitis (EAE) model of multiple sclerosis. BMS-520 can be used for arthritis and EAE research .
|
-
- HY-147214
-
|
|
YAP
|
Cancer
|
|
GNE-7883 is a pan-TEAD inhibitor that blocks the association of YAP/TAZ with TEAD. GNE-7883 effectively reduces chromatin accessibility at TEAD motifs, inhibits cell proliferation in multiple cell line models, and achieves strong anti-tumor efficacy in vivo. In addition, GNE-7883 effectively overcomes intrinsic and acquired resistance to KRAS (Kirsten rat sarcoma viral oncogene homolog) G12C inhibitors in multiple preclinical models by inhibiting YAP/TAZ activation .
|
-
- HY-P10580
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-P1091
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
|
-
- HY-125928
-
|
|
Sodium Channel
|
Neurological Disease
|
|
AA43279 is an in gamma-aminobutyric acid (GABA) fast-firing interneurons located activator for Nav1.1 channel (SCN1A) with an EC50 of 9.5 μM. AA43279 enhances specific neuronal firing activity in vitro, and exhibits anticonvulsant activity in rat MEST model .
|
-
- HY-113906
-
|
|
GHSR
|
Metabolic Disease
|
|
GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors. GSK1614343 inhibits the calcium response induced by ghrelin with a pIC50 value of 7.90. GSK1614343 represents a useful tool to investigate the physiological relevance of the ghrelin system in rat models .
|
-
- HY-156613
-
|
EP-7041
|
Factor XI
|
Infection
|
|
Frunexian (EP-7041) is a selective and potent inhibitor of coagulation factor XI/activated factor XI, targeting to factor XIa. Frunexian exhibits antithrombotic activity, with no bleeding liability in rat mesenteric arterial puncture model. Frunexian can be used in extracorporeal membrane oxygenation (ECMO) research .
|
-
- HY-163646
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
(Rac)-TZ3O is the (Rac) isomer of TZ3O. TZ3O is an anticholinergic compound with neuroprotective activity. TZ3O improves memory impairment and cognitive decline in a scopolamine-induced Alzheimer's disease rat model and can be used in the study of Alzheimer's disease.
|
-
- HY-N8458
-
|
NSC 272693
|
PGE synthase
|
Inflammation/Immunology
|
|
Cryogenine is an alkaloid originally isolated from H. salicifolia that has anti-inflammatory activity. It inhibits prostaglandin synthetase (IC50=424 μM). Cryogenine (100 mg/kg per day, p.o.) reduces paw edema and the mean arthritic index in a rat model of adjuvant-induced polyarthritis.
|
-
- HY-142123R
-
|
|
Glucocorticoid Receptor
Reference Standards
|
Inflammation/Immunology
|
|
Fluocortolone (Standard) is the analytical standard of Fluocortolone. This product is intended for research and analytical applications. Fluocortolone is an orally active anti-inflammatory agent that effectively reduces plasma fibrinogen levels. Fluocortolone inhibits Mycobacterium butyricum-induced foot edema in a rat model of adjuvanted joint inflammation (3-12 mg/kg) .
|
-
- HY-179475
-
|
|
CaSR
|
Endocrinology
|
|
KP-2067 is a form of the CaSR agonist peptide. KP-2067 can result in dose-dependent activation of CaSR in HEK293T overexpressing hCaSR cell line, with an EC50 of 18.4 μM. KP-2067 significantly reduces plasma parathyroid hormone in rat model .
|
-
- HY-B1130
-
|
|
COX
|
Inflammation/Immunology
|
|
Isoxicam is an orally active nonsteroidal anti-inflammatory compound and a COX-1/COX-2 inhibitor. Isoxicam exhibits potent anti-inflammatory activity in rat models of inflammation and significantly lower ulcerogenic risk. Isoxicam can be used for the study of inflammatory diseases and rheumatic disorders .
|
-
- HY-113322
-
|
3-Hydroxyquinidine
|
Drug Metabolite
|
Cardiovascular Disease
|
|
3-Hydroxyquinine is a metabolite of Quinidine (HY-B1751). 3-Hydroxyquinine prevents ventricular fibrillation and ventricular tachycardia after coronary reperfusion in an isolated rat heart reperfusion arrhythmia model in a concentration-dependent manner. 3-Hydroxyquinine can be used in the study of cardiac arrhythmias .
|
-
- HY-202233
-
|
TBN
|
Drug Derivative
|
Neurological Disease
Inflammation/Immunology
|
|
Tetramethylpyrazine nitrone is a nitrone derivative of tetramethylpyrazine. Tetramethylpyrazine nitrone is an active ingredient from Ligusticum wallichii Franchat. Tetramethylpyrazine nitrone is a potent scavenger of free radicals with neuroprotective activitys in both rat and monkey models of ischemis stroke. Tetramethylpyrazine nitrone can suppress over-expression of neuroinflammatory marker vimentin .
|
-
- HY-128976
-
-
- HY-13533
-
|
NSC 682691; 4-Demethylpenclomedine
|
Drug Metabolite
|
Cancer
|
|
DMPEN (NSC 682691) (4-Demethylpenclomedine) is an alkylating metabolite of Penclomedine (HY-106401). DMPEN has an antitumor activity. DMPEN does not induce Purkinje cells loss with no significant neurocerebellar toxicity in rat cerebellum models. DMPEN can be used for cancers like breast and brain cancer research .
|
-
- HY-P990117
-
|
|
Integrin
|
Cardiovascular Disease
Cancer
|
|
Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) is a mouse-derived Osteopontin/SPP1 IgG1 κ type antibody inhibitor. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) blocks Angiotensin II (HY-13948)-induced DNA synthesis and collagen gel contraction in cardiac fibroblasts. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) significantly inhibits tumor growth in CT26 or MC38 tumors mice models .
|
-
- HY-P10977
-
|
|
Sodium Channel
RIP kinase
|
Neurological Disease
|
|
Tat-ASIC1a (1-20) (mouse, rat) is a competitive ASIC1a membrane-penetrating peptide. Tat-ASIC1a (1-20) (mouse, rat) has significantly neuroprotection effects, and reduces neuronal damage against acidotoxicity by targeting the ASIC1a-RIPK1 pathway and auto-inhibitory mechanism. Tat-ASIC1a (1-20) (mouse, rat) effectively protects brains from ischemic injury in ischemic stroke mice model. Tat-ASIC1a (1-20) (mouse, rat) can be used for neurodegenerative diseases research, such as Huntington disease and Parkinson’s disease .
|
-
- HY-D2968
-
|
|
Fluorescent Dye
|
Neurological Disease
|
|
DCM-ONOO is a near-infrared two-photon fluorescence probe specifically designed for real-time monitoring of the dynamic fluctuations of peroxynitrite (ONOO⁻) in epilepsy models. DCM-ONOO exhibits excellent optical properties, with a single photon excitation (Ex) of 520 nm; a single photon emission (Em) of 685 nm; a two-photon excitation of 820 nm; and a Stokes shift of 165 nm. When DCM-ONOO is combined with ONOO⁻, it shifts from 460 nm to 512 nm, and only generates a significant fluorescence response to ONOO⁻. DCM-ONOO has been successfully applied to rat epilepsy models .
|
-
- HY-P10580A
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-12378
-
BQ-123
3 Publications Verification
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
|
-
- HY-101096
-
|
MK-8998; CX-8998; JZP385
|
Calcium Channel
|
Neurological Disease
Cancer
|
|
Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
|
-
- HY-123904
-
|
|
iGluR
|
Neurological Disease
|
|
UoS12258 is a selective positive allosteric modulator of AMPA receptor. UoS12258 enhances AMPA receptor‐mediated synaptic transmission. UoS12258 improves performance in cognition rat models, including Scopolamine (HY-N0296)‐impaired rats and water maze learning and retention in aged rats .
|
-
- HY-P10898
-
-
- HY-129442
-
|
X 910279; HMR-279; FK-779
|
Drug Derivative
|
Inflammation/Immunology
|
|
MNA 279 (X 910279) is an orally active, immunosuppressive malononitrilamide and A 771726 derivative. MNA 279 suppresses IgM and IgG antibody production. MNA 279 prevents the development of systemic lupus erythematosus (SLE)-like disease in mice. MNA 279 prolongs skin xenograft survival in a mouse-to-rat model .
|
-
- HY-155737
-
|
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
|
ET receptor antagonist 1 (compound 16h) is an orally active ET receptor antagonist (IC50=0.18 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 1 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
|
-
- HY-155739
-
|
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
|
ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist (IC50=0.26 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 3 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
|
-
- HY-155738
-
|
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
|
ET receptor antagonist 2 (compound 16j) is an orally active ET receptor antagonist (IC50=0.22 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 2 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
|
-
- HY-180800
-
|
|
COX
|
Neurological Disease
Inflammation/Immunology
|
Anti-inflammatory agent 110 (Compound 7b) is a analgesic/anti-inflammatory agent. Anti-inflammatory agent 110 has a good binding affinity for COX-2. Anti-inflammatory agent 110 demonstrated potent analgesic and anti-inflammatory activities in the mouse hot plate test and the rat carrageenan edema model .
|
-
- HY-164320
-
|
|
Apoptosis
|
Cancer
|
|
Anticancer agent 245 (Compound 115) inhibits proliferation of cancer cell SKOV3, MDA-MB-231 and HCT-116 with IC50 of 0.021, 0.056 and 0.11 μM, respectively. Anticancer agent 245 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
|
-
- HY-179030
-
|
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-19 (Compound 13i) is an orally effective inhibitor of xanthine oxidase (XO), with an IC50 of 0.2 μM. Xanthine oxidase-IN-19 can significantly reduce serum uric acid levels in acute hyperuricemia rat models. Xanthine oxidase-IN-19 can be used for the study of acute hyperuricemia .
|
-
- HY-107526
-
|
(Rac)-NFPS
|
GlyT
|
Neurological Disease
|
|
NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively . NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion .
|
-
- HY-119152
-
|
|
Insulin Receptor
Tyrosinase
Akt
|
Others
|
|
CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model .
|
-
- HY-18759
-
|
|
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
|
|
BMS-751324 is a p38α MAPK inhibitor. BMS-751324 equips a precursor of carbamyl-methyl linkage, containing esters and phosphate functional groups derived from hydroxyphenylacetic acid (HPA). BMS-751324 effectively inhibits foot swelling and LPS-induced TNFα production in an arthritic rat model .
|
-
- HY-13762S
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
|
Cancer
|
|
Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
|
-
- HY-P1091A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-161506
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE1-IN-7 (Compound 13h) is a selective inhibitor of bPDE1 (IC50= 10 nM). PDE1-IN-7 exhibits significant anti-fibrotic effects in a BDL-induced liver fibrosis rat model. PDE1-IN-7 can be used for research in liver fibrosis .
|
-
- HY-110199
-
|
|
TRP Channel
|
Neurological Disease
|
|
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models .
|
-
- HY-12378A
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-123 TFA is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 TFA inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
|
-
- HY-103327
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
|
-
- HY-157796
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
β2AR agonist 4 (compound A19) is a potent and selective β2-Adrenoceptor agonist with an EC50 of 3.7 pM. β2AR agonist 4 suppresses the inflammatory cytokines and leukocytes upregulation and improves lung function in COPD rat model .
|
-
- HY-W740009
-
|
|
Drug Metabolite
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
4-Oxoetodolac, Etodolac (HY-76251) metabolite, is an orally active antiinflammatory agent. 4-Oxoetodolac blocks prostaglandin production in cultured chondrocyte cells. 4-Oxoetodolac exhibits slight antiinflammatory activity in a rat adjuvant edema model. 4-Oxoetodolac can be used for the research of inflammation .
|
-
- HY-W742532
-
|
N-Ethyl-nor-LSD
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
ETH-LAD (N-Ethyl-nor-LSD) is an activator for 5-HT2A receptor with Ki of 5.1 nM. ETH-LAD exhibits affinity for dopamine receptor D1 and dopamine receptor D2 with Ki of 22.1 nM and 4.4 nM. ETH-LAD acts as psychoactive substance in rat model .
|
-
- HY-P991982
-
|
|
ADC Antibody
|
Cancer
|
|
ZV0201 Antibody (ZV02) is a monoclonal antibody inhibitor targeting Her2. ZV0201 Antibody can be used to synthesize the antibody-drug conjugate (ADC) ZV0201. ZV0201 Antibody can be used to research related to HER2-positive tumors .
|
-
- HY-162584
-
|
|
TRP Channel
|
Others
|
|
TRPC5-IN-6 (Compound 12) is an orally effective transient receptor potential (TRPC5) inhibitor with a IC50 value of 81 nM. TRPC5-IN-6 has good biosafety and low liver and kidney toxicity, and is expected to play an important role in the treatment of chronic kidney disease (CKD) .
|
-
- HY-B0885
-
|
(±)-Econazol
|
Fungal
Bacterial
Calcium Channel
Cytochrome P450
|
Infection
Metabolic Disease
|
|
Econazole ((±)-Econazol) is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage .
|
-
- HY-157936
-
|
|
iGluR
|
Neurological Disease
|
|
GluN2B-NMDAR antagonist-2 (compound S-58) is a potent, selective and cross the blood-brain barrier NMDAR-GluN2B antagonist with an IC50 value of 74.01, nM. GluN2B-NMDAR antagonist-2 shows mild cytotoxicity. GluN2B-NMDAR antagonist-2 decreases the cerebral infarction rates and neurologic deficit scores. GluN2B-NMDAR antagonist-2 has the potential for the research of stroke .
|
-
- HY-14305
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis .
|
-
- HY-153505
-
|
|
ADAMTS
|
Inflammation/Immunology
|
|
ADAMTS-4/5-IN-1 is an orally active, and selective dual ADAMTS-4/5 inhibitor with IC50 values of 2 nM for human ADAMTS-4 and human ADAMTS-5, respectively. ADAMTS-4/5-IN-1 exhibits high selectivity against MMP enzymes. ADAMTS-4/5-IN-1 reduces aggrecan degradation products in synovial fluid. ADAMTS-4/5-IN-1 can be used for the research of osteoarthritis .
|
-
- HY-186083
-
|
|
mAChR
|
Cardiovascular Disease
|
|
Propylbenzilylcholine mustard (PrBCM) is an irreversible, covalently binding selective antagonist targeting rat cardiac muscarinic receptors, with a preference for muscarinic receptor subtypes that show low affinity for agonists. Propylbenzilylcholine mustard inactivates such receptors in a dose- and time-dependent manner in vitro, and its receptor selectivity remains stable across different ionic strengths and in GTP-containing buffer systems. Propylbenzilylcholine mustard can be applied to basic pharmacological studies on the structure and function of muscarinic receptors, especially focusing on the heterogeneity of cardiac muscarinic receptors and related cardiovascular pharmacological research .
|
-
- HY-W783623
-
|
DG(22:6/0:0/22:6); 1,3-Didocosahexaenoin
|
Biochemical Assay Reagents
|
Cardiovascular Disease
|
|
1,3-Didocosahexaenoyl glycerol (DG(22:6/0:0/22:6); 1,3-Didocosahexaenoin) is an ω-3 polyunsaturated fatty acid, which exhibits cardioprotective effects in rat myocardial ischemia/reperfusion (I/R) injury model through conjugation with Poly-l-glutamic acid (PGA) .
|
-
- HY-N8249
-
|
|
nAChR
Interleukin Related
|
Inflammation/Immunology
|
|
Cynandione A is an acetophenone that can be isolated from Cynanchum Wilfordii Radix. Cynandione A protects hepatocytes and cortical neurons from toxicity and improves neurological deficits in a rat model of cerebral ischemia. On the other hand, cynandione A has significant anti-inflammatory effects and inhibits inflammation by activating macrophage α7 nAChR and IL-10 expression .
|
-
- HY-155126
-
|
|
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
LZWL02003 is an anti-neuroinflammatory agent. LZWL02003 has protective effect on MPP +-induced neuronal damage, and reduces the expression of ROS. LZWL02003 improves cognition, memory, learning, and athletic ability in a Rotenone (HY-B1756)-induced PD rat model. LZWL02003 can be used for research of neurodegenerative disease .
|
-
- HY-122051
-
AC1903
1 Publications Verification
|
TRP Channel
|
Metabolic Disease
|
|
AC1903 is a specific and selective inhibitor of TRPC5 and has podocyte-protective properties. AC1903 does no effects on TRPC4 or TRPC6 currents and shows no off-target effects in kinase profiling assays. AC1903 suppresses severe proteinuria and prevents podocyte loss in focal segmental glomerulosclerosis (FSGS) rat model .
|
-
- HY-119912
-
|
Stakane dihydrochloride
|
COX
|
Neurological Disease
Inflammation/Immunology
|
|
Antrafenine (Stakane) dihydrochloride is a non-narcotic analgesic. Antrafenine dihydrochloride demonstrates central analgesic effects in acetic acid writhing test and mouse hot plate test experiments. Antrafenine dihydrochloride significantly alleviates osteoarthritis pain. Antrafenine dihydrochloride exhibits mild anti-inflammatory activity in a rat toe edema model. Antrafenine dihydrochloride can be used for pain and anti-inflammatory research .
|
-
- HY-164532
-
|
|
Chloride Channel
|
Metabolic Disease
|
|
NS3736 is an orally effective chloride channel inhibitor that can be used for the research of osteoporosis. NS3736 targets the CIC-7 channel in osteocytes, blocks osteoclast acidification and resorption in vitro, with IC50=30 μM. In a rat model of ovariectomy-induced osteoporosis, NS3736 can enhance bone strength and bone density .
|
-
- HY-105351
-
|
|
Neprilysin
|
Cardiovascular Disease
|
|
CGS25155 is an orally active neutral endopeptidase 24.11 (NEP 24.11) inhibitor with an IC50 of 3 nM. CGS25155 can slow down the degradation of the cardiac hormone atrial natriuretic peptide (ANP) and exhibits antihypertensive activity in the DOCA-salt induced rat hypertension model. CGS25155 can be used in cardiovascular disease research .
|
-
- HY-106856R
-
|
NT-11624 (Standard)
|
iGluR
Reference Standards
|
Cancer
|
|
Dimiracetam (Standard) (NT-11624 (Standard)) is the analytical standard of Dimiracetam (HY-106856). This product is intended for research and analytical applications. Dimiracetam is an orally active compound, with anti-neuropathic activity. Dimiracetam inhibits hypersensitivity and neurological alterations, and inhibits Sorafenib (HY-10201)-induced neuropathy in cold stimulation rat models .
|
-
- HY-168084
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
IL-17-IN-1 (26) is an orally active IL-17 inhibitor, with IC50 values of 0.013 μM and 0.004 μM for IL-17A and IL-6 release, respectively. IL-17-IN-1 (26) effectively reduces knee swelling in a rat arthritis model .
|
-
- HY-117839
-
|
|
Cholecystokinin Receptor
|
Neurological Disease
|
|
PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models .
|
-
- HY-169963
-
|
|
Phosphodiesterase (PDE)
|
Others
|
|
PDE1-IN-8 (Compound 3f) is the inhibitor for PDE1 with an IC50 of 11 nM. PDE1-IN-8 inhibits cAMP and cGMP signaling pathway, inhibits the differentiation and proliferation of cells into myofibroblast, and exhibits anti-fibrotic efficacy in Bleomycin (HY-17565)-induced rat pulmonary fibrosis model .
|
-
- HY-A0235
-
|
Stakane
|
COX
|
Neurological Disease
|
|
Antrafenine (Stakane) is a non-narcotic analgesic. Antrafenine demonstrates central analgesic effects in acetic acid writhing test and mouse hot plate test experiments. Antrafenine significantly alleviates the pain of osteoarthritis. Antrafenine exhibits mild anti-inflammatory activity in a rat toe edema model. Antrafenine can be used in pain and anti-inflammatory research .
|
-
- HY-101418
-
|
|
P2X Receptor
|
Neurological Disease
|
|
JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology .
|
-
- HY-W587784
-
|
|
PPAR
|
Metabolic Disease
|
|
Norbixin is a carotenoid that has been found in B. orellana.It binds to PPARγ in a cell-free assay (Ki = 1.15 μM) . Norbixin attenuates hyperglycemia, hyperinsulinemia, and insulin resistance, as well as decreases serum lipid levels and cardiac levels of thiobarbituric acid reactive substances (TBARS) and glutathione (GSH) in a rat model of cardio-metabolic syndrome .
|
-
- HY-107969R
-
|
|
Dopamine Receptor
Reference Standards
COX
NO Synthase
|
Neurological Disease
|
|
Haloperidol decanoate (Standard) is the analytical standard of Haloperidol decanoate. This product is intended for research and analytical applications. Haloperidol decanoate is a depot preparation of haloperidol, a commonly used butyrophenone derivative with antipsychotic activity. Haloperidol decanoate can increase the striatal D2 receptor in rat. Haloperidol decanoate can improve conditions of psychoses (mainly schizophrenia). Haloperidol decanoate can lead to increased accumulation of the dopamine metabolites homo-vanillic acid. Haloperidol decanoate can reduce intestinal transport, increase gastric emptying and reduce acid output in rat model .
|
-
- HY-N0265
-
-
- HY-165571
-
|
|
Carboxypeptidase
|
Neurological Disease
|
|
E2072 is a selective, orally active competitive inhibitor of glutamate carboxypeptidase II (GCPII) with a Ki of 10 nM. E2072 alleviates established thermal hyperalgesia in a rat model of chronic constriction injury. E2072 prevents oxaliplatin-induced reductions in nerve conduction velocity and amplitude in mice. E2072 is applicable to research related to neuropathic pain and neuropathy .
|
-
- HY-18734AR
-
|
|
NO Synthase
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
|
|
Carboxy-PTIO (potassium) (Standard) is the analytical standard of Carboxy-PTIO (potassium). This product is intended for research and analytical applications. Carboxy-PTIO potassium is a potent nitric oxide (NO) scavenger that can make a quick reaction with NO to produce NO2. Carboxy-PTIO potassium can prevent hypotension and endotoxic shock through the direct scavenging action against NO in lipopolysaccharide-stimulated rat model .
|
-
- HY-113427
-
|
|
Endogenous Metabolite
Bcl-2 Family
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity .
|
-
- HY-126835
-
|
|
Amino Acid Derivatives
|
Cancer
|
|
A 924 is an amino acid derivative-based, orally active antitumor agent. A 924 is effective in inhibiting ascites tumors in rat models by intraperitoneal injection or oral administration. The LD50 of A 924 in mice is >1.5 g/kg and >4.5 g/kg by intraperitoneal injection or oral administration, respectively. A 924 does not cause teratogenicity or adverse reactions in normal or pregnant mice .
|
-
- HY-110099
-
|
|
CXCR
|
Inflammation/Immunology
|
|
(±)-NBI-74330 is a potent and selective CXCR3 antagonist. (±)-NBI-74330 not only reduces tactile and thermal hypersensitivity but also enhances the analgesic properties of morphine. (±)-NBI-74330 can reduce microglial cell activation, increase astroglial cell activation, and downregulate the expression of some CXCR3 ligands in a rat neuropathic pain model .
|
-
- HY-122063
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
FR260330 is a selective, orally active inhibitor for inducible nitric oxide synthase (iNOS) through suppression of iNOS dimerization. FR260330 inhibits the NO accumulation in rat splenocytes and human DLD-110 cells, with IC50 of 27 and 10 nM. FR260330 ameliorates the Lipopolysaccharides (HY-D1056)-induced inflammatory diseases in rats model .
|
-
- HY-155819
-
|
|
mAChR
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
M3/PDE4 modulator-1 (compound 10f) is a bifunctional molecule that is an M3 mAChR antagonist and a PDE4 inhibitor. M3/PDE4 modulator-1 (10-1000 nM/kg; iv) reduces cysteine eosinophil influx in the OVA rat model .
|
-
- HY-153091
-
|
|
Adrenergic Receptor
5-HT Receptor
Sigma Receptor
|
Neurological Disease
|
|
BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM .
|
-
- HY-172750
-
|
17(R,S)-Benzo-RvD1
|
Drug Derivative
|
Inflammation/Immunology
|
|
17(R,S)-Benzo-resolvin D1 (17(R,S)-Benzo-RvD1) is a Resolvin D1 (HY-125527) analogue with pro-resolving and anti-migratory activity. 17(R,S)-Benzo-resolvin D1 attenuates neointimal hyperplasia in a rat model of acute vascular injury .
|
-
- HY-163061
-
|
|
Histamine Receptor
|
Inflammation/Immunology
|
|
Quinotolast is an orally active antiallergic agent. Quinotolast inhibits histamine release from rat peritoneal cells. Quinotolast inhibits cutaneous cromoglycate in guinea pig model. Quinotolast has inhibitory effect on histamine and peptide leukotrienes release from guinea pig lung fragments and mouse cultured mast cells. Quinotolast can be studied in allergy-related research .
|
-
- HY-12435
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
SAR216471 is a P2Y12 receptor antagonist. SAR216471 reversibly blocks the binding of 2MeSADP to P2Y12 receptors in vitro with an IC50 of 17 nM. SAR216471 can result in the inhibition of platelet aggregation. SAR216471 exhibits anti-thrombotic activity in rat model. SAR216471 can be studied in research on thrombosis .
|
-
- HY-114753
-
|
CR-2249; XY-2401
|
iGluR
|
Neurological Disease
|
|
Neboglamine (CR-2249; XY-2401) is a modulator for N-methyl-D-aspartate (NMDA) receptor. Neboglamine increases the levels of fos-like immunoreactivity (FLI)-positive cells in the prefrontal cortex, nucleus accumbens, and lateral septal nucleus in rat models, .restores NMDA (HY-17551) -mediated neurotransmitter release, and inhibits phencyclidine-induced hyperlocomotion .
|
-
- HY-134521
-
|
|
COX
|
Inflammation/Immunology
|
|
Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg) .
|
-
- HY-117686
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
AZ12441970 is a potent and selectiveToll-like receptor 7 (TLR7) agonist, exhibiting pEC50s of 6.8 and 6.6 for human and rat TLR7. AZ12441970 shows efficacy in a mouse allergic airway model with minimal induction of systemic IFN-α. AZ12441970 can be used for allergic airway disease research .
|
-
- HY-100458
-
|
|
NO Synthase
|
Neurological Disease
|
|
SCR-4026 is a neuroprotective agent with blood-brain barrier penetration ability. SCR-4026 exerts neuroprotective effects by disrupting the interaction between neuronal nNOS and PSD9, with an IC50 of 6.3 μM. SCR-4026 alleviates N-methyl-D-aspartate (NMDA)-induced excitotoxic damage in primary cortical neurons, and also protects neurons in the oxygen-glucose deprivation (OGD) model. SCR-4026 can reduce the cerebral infarct volume in the rat middle cerebral artery occlusion (MCAO) reperfusion model. SCR-4026 can be used for the study of stroke .
|
-
- HY-150038
-
|
NBS-1120
|
NF-κB
Apoptosis
|
Neurological Disease
Cancer
|
|
NOSH-aspirin (NBS-1120) is an orally active hybrid molecule that releases nitric oxide and hydrogen sulfide. NOSH-aspirin inhibits pancreatic cancer cell proliferation and induces apoptosis. NOSH-aspirin inhibits cancer cell growth and suppresses NF-κB and FoxM1 in a mouse model of pancreatic cancer. NOSH-aspirin also alleviates motor deficits and dopaminergic neuron degeneration in a rat model of Parkinson's disease. NOSH-aspirin reduces neuroinflammation caused by microglial and astrocytic activation. NOSH-aspirin can be used in research on cancers such as pancreatic cancer and neurological diseases such as Parkinson's disease .
|
-
- HY-W110138
-
|
|
DNA/RNA Synthesis
Cytochrome P450
ROCK
|
Cancer
|
|
Chloroxoquinoline is an anticancer agent. Chloroxoquinoline damages the DNA templates of cancer cells, inducing DNA breaks and cell death, and inhibits cell invasion via down-regulating Rho/Rho kinase signaling pathway. Chloroxoquinoline enhances the radiation sensitivity of Lewis lung cancer cells and xenograft tumors in tumor-bearing mouse models but decreases efficacy after long term exposure in rat models by auto-induction effects on CYP1A and CYP3A. Chloroxoquinoline has a broad-spectrum anticancer activity, such as non-small-cell lung carcinoma (NSCLC), breast cancer and gastric cancer .
|
-
- HY-135115
-
|
3,4-DHPEA-EA
|
α-synuclein
HDAC
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Oleuropein Aglycone (3,4-DHPEA-EA) is a polyphenol and the aglycone form of oleuropein (HY-N0292), formed by enzymatic, acidic or acetylated hydrolysis of oleuropein. Dietary intake of oleuropein Aglycone (50 mg/kg diet) increases the number of neuronal autophagic vesicles, reverses cognitive deficits in the TgCRND8 transgenic mouse model of Alzheimer's disease, and reduces the levels of histone deacetylase 2 (HDAC2) in the cortex and hippocampus. Oleuropein Aglycone increases urinary norepinephrine, interscapular brown adipose tissue epinephrine, and UCP1 protein levels, and reduced plasma leptin levels and total abdominal adipose tissue weight in a rat model of high-fat diet-induced obesity. Oleuropein Aglycone also reduced lung neutrophil infiltration, lipid peroxidation, and IL-1β levels in a mouse model of carrageenan-induced pleurisy.
|
-
- HY-112460
-
|
|
CDK
|
Cancer
|
|
CDK2-IN-3 (compound 3) is a potent and selective CDK2 inhibitor with an IC50 of 60 nM .
|
-
- HY-15056
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
AMG 9090 is characterized as a compound that acts as a partial agonist of rat TRPA1 channels, demonstrating pharmacological activity in pain and inflammation models. TRPA1 is pivotal in sensing reactive compounds, triggering pain responses in humans and rodents. AMG 9090, along with other trichloro(sulfanyl)ethyl benzamides (TCEB compounds), shows differential effects on human and rat TRPA1 channels: it acts as a potent antagonist of human TRPA1 activated by AITC and noxious cold, whereas it behaves as a partial agonist at rat TRPA1. This suggests AMG 9090's potential as a therapeutic agent targeting TRPA1-mediated pain and inflammation, with additional inhibitory activity against TRPM8 noted .
|
-
- HY-109968A
-
|
CEP-26401 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
|
-
- HY-121554
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Kojic amine is an orally active γ-aminobutyric acid (GABA) analog. Kojic amine acts as a GABA mimic that inhibits sodium-independent [ 3H]GABA binding to rat brain cell membranes. Kojic amine reduces flexor spasms in chronic spinal rat and cat models. Kojic amine prevents tonic extensor convulsions in mice. Kojic amine produces a transient, dose-dependent analgesic effect in the mouse hot-plate test. Kojic amine can be used in research related to skeletal muscle spasm, epilepsy and analgesia [1][2]
|
-
- HY-109968
-
|
CEP-26401
|
Histamine Receptor
|
Neurological Disease
Metabolic Disease
|
|
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
|
-
- HY-123187
-
|
|
JAK
|
Cardiovascular Disease
|
AS2553627 is a type of JAK inhibitor, with IC50 values of 0.46, 0.30, 0.14, and 2.0 nM for JAK1, JAK2, JAK3 and TYK2, respectively. AS2553627 can inhibit the proliferation of human and rat T cells stimulated by IL-2, with IC50 values of 2.4 and 4.3 nM, respectively. AS2553627 can reduce cardiac allograft vasculopathy and fibrosis in a rat heart transplant model, effectively extending survival rates. AS2553627 can be used to prevent acute and chronic rejection in heart transplants .
|
-
- HY-172419
-
|
GM-1020
|
iGluR
|
Neurological Disease
|
|
Blixeprodil (GM-1020) is the orally active antagonist for NMDA receptor with an affinity of Ki=3.25 µM in rat cortical tissue. Blixeprodil inhibits NR1/2A-NMDAR-mediated currents in HEK293 cell with IC50 of 1.192 µM. Blixeprodil exhibits antidepressant in rats models. Blixeprodil can cross blood-brain barrier .
|
-
- HY-P3355
-
|
|
iGluR
|
Neurological Disease
|
|
p-fin4 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 0.4 μM. p-fin4 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p-fin4 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-119530
-
|
BW 57-323
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
|
-
- HY-124051
-
|
|
Elastase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
BAY-8040 is a pyrimidopyridazine derivative which has inhibitory activity against human neutrophil elastase (HNE). BAY-8040 decreases cardiac remodeling and ameliorates cardiac function in a Monocrotaline (HY-N0750)-induced rat model for pulmonary arterial hypertension. BAY-8040 is promising for research of inflammatory pathologies and cardiopulmonary pathologies .
|
-
- HY-P990148
-
|
|
VEGFR
|
Cancer
|
|
Anti-Mouse VEGF-A Antibody (2G11-2A05) is a rat-derived IgG2a κ type antibody inhibitor, tragrting to mouse VEGF-A with high affinity. Anti-Mouse VEGF-A Antibody (2G11-2A05) shows good anti-tumor effect in gastric cancer xenograft models .
|
-
- HY-148195
-
|
NNZ-2591
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Ercanetide (NNZ 2591) is a synthetic analogue of a small peptide of cyclic glycine proline (cGP). Ercanetide shows orally active and cross the blood-brain barrier. Ercanetide shows neuroprotective after ischemic brain injury. NNZ 2591 improves motor function in a rat model of Parkinson's disease. Ercanetide has the potential for the research of ischemic brain injury and angelman syndrome .
|
-
- HY-158374
-
|
|
IRAK
|
Inflammation/Immunology
|
|
BIO-8169 is a selective inhibitor for interleukin receptor-associated kinase 4 (IRAK 4), with an IC50 of 0.23 nM. BIO-8169 exhibits good pharmacokinetic character, reduces the production of pro-inflammatory cytokines, and attenuates the autoimmune encephalomyelitis in EAE mice model. BIO-8169 exhibits good blood brain penetrant with a rat Kpu,u of 0.7 .
|
-
- HY-N0665
-
|
(8E)-Nuezhenide
|
NF-κB
Wnt
|
Inflammation/Immunology
|
|
Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA) .
|
-
- HY-128932
-
|
MT-141
|
Antibiotic
Bacterial
PPAR
Prostaglandin Receptor
PTEN
Akt
mTOR
|
Infection
Cardiovascular Disease
Endocrinology
|
|
Cefminox sodium (MT-141) is a semisynthetic cephamycin, which exhibits antibacterial activity. Cefminox sodium is a broad-spectrum, bactericidal cephalosporin antibiotic. Cefminox sodium also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ. Cefminox sodium upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium also prevents pulmonary arterial hypertension in rat model .
|
-
- HY-147927
-
|
|
Enteropeptidase
|
Metabolic Disease
|
|
Human enteropeptidase-IN-1 (compound 6b) is a highly potent, orally active and low systemic exposure enteropeptidase inhibitor. Human enteropeptidase-IN-1 boosts the increase in fecal protein output, and exhibits potent body weight loss in diet-induced obese (DIO) rat model. Human enteropeptidase-IN-1 can be used for anti-obesity research .
|
-
- HY-P5874
-
|
|
Calcium Channel
|
Inflammation/Immunology
|
|
Myr-TAT-CBD3 is CRMP2-CaV2.2 interaction inhibitor. Myr-tat-CBD3 can significantly attenuate carrageenan-induced thermal hypersensitivity and reverse thermal hypersensitivity induced in a rat model of postoperative pain. Myr-TAT-CBD3 can be used to study inflammation and postoperative pain .
|
-
- HY-158688
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kδ-IN-21 (Compound 31) is a selective inhibitor for phosphoinositide 3-kinases δ (PI3Kδ), with an IC50 of 13.6 nM. PI3Kδ-IN-21 inhibits proliferation and differentation of T cells through PI3K/AKT/mTOR signaling pathway. PI3Kδ-IN-21 exhibits good pharmacokinetic characters in rat model, and attenuates the experimental autoimmune encephalomyelitis in myelin oligodendrocyte glycoprotein (MOG)-induced EAE model .
|
-
- HY-132280
-
|
U 74006F free base
|
Reactive Oxygen Species (ROS)
SARS-CoV
Virus Protease
|
Neurological Disease
Inflammation/Immunology
|
|
Tirilazad (U 74006F free base) is a neuroprotective agent. Tirilazad can also bind tightly to the main protease of the COVID-19 virus and exert anti-SARS-CoV-2 activity. Tirilazad scavenges hydroxyl and lipid peroxyl free radicals and maintains the levels of endogenous antioxidants. Tirilazad reduces cerebral infarct volume and improves neurobehavioral scores in animal models of focal ischemia. Tirilazad can be used in research related to ischemic stroke and subarachnoid hemorrhage .
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- HY-W700354
-
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Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
(S)-(-)-Felodipine is a S-enantiomer of Felodipine. (S)-(-)-Felodipine is an antihypertensive agent. Felodipine is a 1,4-dihydropyridine derivative and a vasoselective calcium antagonist. Felodipine can prevent the activation of the vascular effector cells and interfere with the contractile process in vitro. Felodipine lowers mean arterial blood pressure by 20% in dog model. (S)-(-)-Felodipine shows high metabolic rate in rat and dog liver microsomes .
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- HY-108467
-
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Nahlsgen
|
γ-Glutamyl Transferase (GGT)
|
Cardiovascular Disease
|
|
GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ-GGT inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150 and 51 M -1 s -1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model .
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- HY-180186
-
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Xanthine Oxidase
|
Metabolic Disease
Inflammation/Immunology
|
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Xanthine oxidase-IN-20 is a potent and orally active xanthine oxidase (XO) inhibitor with an IC50 of 1.7 nM. Xanthine oxidase-IN-20 exhibits outstanding serum uric acid (SUA)-lowering efficacy in both mouse and rat acute hyperuricemia models. Xanthine oxidase-IN-20 shows favorable safety profile. Xanthine oxidase-IN-20 can be used for hyperuricemia and gout research .
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-
- HY-P10360
-
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α-synuclein
|
Neurological Disease
|
|
Tat-βsyn-degron is an α-synuclein knockdown peptide that effectively degrades α-synuclein protein via the proteasome pathway. Tat-βsyn-degron effectively reduces α-synuclein protein levels in primary rat cortical neuron cultures. In a Parkinson's mouse toxicity model, Tat-βsyn-degron can alleviate parkinsonian toxin-induced neuronal damage and movement disorders .
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-
- HY-111066
-
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Dopamine Receptor
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Others
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JNJ-37822681 is a fast dissociating D2 antagonist with activity in inhibiting schizophrenia. JNJ-37822681 has high specificity for D2 receptors and is effective in animal models, inducing increased levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibiting antidepressant activity in the mouse tail suspension test, while having a good brain distribution and lower prolactin release.
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- HY-158013A
-
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Dopamine Transporter
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Neurological Disease
|
|
JJC8-088 dioxalate is the dioxalate salt form of JJC8-088 (HY-158013). JJC8-088 dioxalate is a derivative of modafinil. JJC8-088 dioxalate is an inhibitor for dopamine transporter (DAT). JJC8-088 dioxalate exhibits behavioral characteristics similar to cocaine in rat models, and can be to study psychostimulant use disorders .
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- HY-19090
-
|
|
NO Synthase
HSP
|
Cardiovascular Disease
Inflammation/Immunology
|
|
FK 409 is a NO donor that can penetrate cell membranes. FK 409 has a vasodilatory effect on bovine retinal arteries. FK 409 alleviates acute-phase inflammation, induces HSP, and mitigates liver transplantation injury in a rat model of orthotopic liver transplantation. FK 409 can be used in research on cardiovascular diseases and liver transplant rejection and inflammatory immune system disorders .
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- HY-P11111
-
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Drug Derivative
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Others
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QP5 is an Amelogenin (HY-P71627)-derived peptide. QP5 binds on the hydroxyapatite and demineralized tooth enamel surfaces, transitorily stabilize the amorphous calcium phosphate (ACP), control the crystallization of hydroxyapatite and promote the remineralization of caries lesions. QP5 promotes remineralization in rat caries models. QP5 can be used for oral diseases like dental caries research .
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- HY-117991
-
|
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VEGFR
|
Cancer
|
|
DW10075 is a highly selective and orally active VEGFR inhibitor targeting the VEGF/VEGFR pathway. DW10075 selectively inhibits VEGFR-1, VEGFR-2, and VEGFR-3, but has no effect on FGFR and PDGFR. DW10075 inhibits VEGF-induced HUVEC proliferation, migration, and tube formation. And DW10075 inhibits angiogenesis in both the rat aortic ring model and the chick chorionic membrane model. DW10075 also exhibits antiproliferative activity against human cancer cell lines, with IC50s of 2.2 μM and 22.2 μM against U87-MG human glioblastoma cells and A375 melanoma cells, respectively. In the nude mouse U87-MG xenograft tumor model, DW10075 (po) significantly inhibits tumor growth and reduces the expression of CD31 and Ki67 in tumor tissues.
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-
- HY-120476
-
|
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
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JNJ-39729209 is an antagonist for transient receptor potential vanilloid 1 (TRPV1) with pIC50 of 7.9, 8.5, 7.9 and 7.7 for TRPV1 from human, rat, canine and guinea pig. JNJ-39729209 inhibits Capsaicin (HY-10448)-induced hypotension and inhibit thereby hypothermia. JNJ-39729209 exhibits anti-inflammatory and analgesic activities in Carrageenan (HY-125474)- and CFA (HY-153808)-induced thermal hyperalgesia rat models. JNJ-39729209 exhibits anti-cough effects in guinea pigs .
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- HY-171472
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-86929 is a highly potent and selective dopamine D1 receptor agonist with a pKi value of 7.3. In the 6-OHDA (HY-B1081)-induced unilateral nigrostriatal lesion rat model, A-86929 significantly induces rotational behavior. It also improves motor function in the MPTP (HY-15608)-induced Parkinson's disease marmoset model. Additionally, A-86929 demonstrates potential therapeutic value in reducing cocaine-seeking behavior in rats and reversing Haloperidol (HY-14538)-induced cognitive deficits in rhesus monkeys. A-86929 can be used for research in neurological disorders .
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-
- HY-162641
-
|
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IRAK
NF-κB
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
|
|
AF-45 inhibits IRAK4 and IRAK1, with IC50s of 128 nM and 1765 nM. AF-45 inhibits the release of IL-6 and TNF-α in macrophages, with IC50s of 0.53-1.54 μM and 0.6-2.75 μM. AF-45 is also an inhibitor for NF-κB/MAPK signaling pathway. AF-45 exhibits anti-inflammatory activities against DSS-induced ulcerative colitis and Lipopolysaccharide (HY-D1056)-induced acute lung injury in mouse model. AF-45 exhibits good pharmacokinetic characteristics in rat models .
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-
- HY-13954
-
|
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P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta .
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-
- HY-103552
-
|
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mGluR
|
Neurological Disease
|
|
LY487379 hydrochloride is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 hydrochloride potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 hydrochloride promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 hydrochloride can be used for schizophrenia research .
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-
- HY-W415753
-
|
VUFB-15754
|
Drug Derivative
|
Neurological Disease
Inflammation/Immunology
|
|
Alaptide, a spirocyclic synthetic dipeptide and a derivative of melanocyte-stimulating hormone release-inhibiting factor (MIF), is a transdermal permeation modifier. Alaptide loaded on nanofibrous membranes accelerates the healing of skin incisions, particularly the healing of skin burns.
Alaptide is a nootropic agent, that influences the dopaminergic system and increases homovanillic acid level in the striatum of rat models. Alaptide can be used for wound healing with large damaged areas and neurological diseases research .
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-
- HY-182579
-
|
|
p38 MAPK
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
CBS-3408 is an orally active p38α MAPK inhibitor. CBS-3408 inhibits the release of TNFα and IL-1β. CBS-3408 reduces the disease severity of arthritis in mice. CBS-3408 inhibits TNFα release in a rat endotoxemia model. CBS-3408 can be used in studies related to endotoxemia and arthritis .
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-
- HY-14895
-
|
CM346
|
Parasite
Monoamine Oxidase
Sigma Receptor
P-glycoprotein
|
Infection
Cardiovascular Disease
Neurological Disease
|
|
Fabomotizole (CM346) is an insecticide with anxiolytic, antianxiety, and neuroprotective activities and a substrate of p-glycoprotein. Fabomotizole inhibits the ST-segment depression induced by isoproterenol in a rat model of acute subendocardial ischemia. Fabomotizole also inhibits Giardia lamblia and has the potential to inhibit giardiasis. Fabomotizole also targets Sigma1R, NRH:quinone reductase 2 (NQO2), and MAO-A to exert anxiolytic effects .
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-
- HY-122255
-
|
|
mGluR
|
Neurological Disease
|
|
LY487379 is a selective human mGluR2 positive allosteric modulator (PAM). LY487379 potentiates glutamate-stimulated [ 35S]GTPγS binding with EC50 values of 1.7 μM and >10 μM for mGlu2 and mGlu3 receptors respectively. LY487379 promotes cognitive flexibility and facilitates behavioral inhibition in a rat model. LY487379 can be used for schizophrenia research .
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-
- HY-144456
-
|
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-5 is an effective and orally active xanthine oxidase (XO) inhibitor with IC50 value of 0.70 μM. Xanthine oxidase-IN-5 displays favorable agent-like properties with ligand efficiency (LE) and lipophilic ligand efficiency (LLE) values of 0.33 and 3.41, respectively. Xanthine oxidase-IN-5 shows potent hypouricemic effects in hyperuricemic rat model .
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-
- HY-160602
-
|
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Free Fatty Acid Receptor
|
Metabolic Disease
|
|
CPL207280 is an orally active GPR40/FFA1 agonist with an antidiabetic effect. CPL207280 can effectively enhance glucose-stimulated insulin secretion and improve glucose tolerance in MIN6 pancreatic β-cells as well as in healthy Wistar Han rats and diabetic rat models. CPL207280 can be used for the research of type 2 diabetes .
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-
- HY-163378
-
|
|
Complement System
|
Inflammation/Immunology
|
|
C5aR1 antagonist 1 (Compound 7e) is an orally active C5a receptor 1 (C5aR1) antagonist. C5aR1 antagonist 1 is active in DISCO and migration assays, with IC50 values of 38 nM and 17 nM, respectively. C5aR1 antagonist 1 can be used for the research of acute and chronic inflammatory diseases .
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-
- HY-120714
-
-
- HY-176274
-
-
- HY-N2995
-
|
Poricoic acid A(F)
|
NF-κB
Keap1-Nrf2
AMPK
TGF-beta/Smad
Reactive Oxygen Species (ROS)
|
Inflammation/Immunology
Cancer
|
|
Poricoic acid A can be isolated from Poria cocos. Poricoic acid A is an orally active anti-tumor agent. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis. Poricoic acid A also attenuatea fibroblast activation and abnormal extracellular matrix remodeling in renal fibrosis by activating AMPK and inhibiting Smad3. Poricoic acid A significantly reduces the magnitude of rise in serum creatinine and urea levels in rat model when combined with Melatonin. Poricoic acid A ameliorates renal fibrosis and podocyte injury by attenuating oxidative stress and inflammation through regulating NF-κB and Nrf2 in IRI rodent model in combination with Melatonin .
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-
- HY-W018026
-
|
L-p-Hydroxyphenylglycine; 4-Hydroxy-L-phenylglycine; UK 25842
|
Acyltransferase
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
|
|
Oxfenicine (L-p-Hydroxyphenylglycine) is an orally active carnitine palmitoyltransferase-1 inhibitor. Oxfenicine inhibits the oxidation of fatty acids in the heart, protecting cardiac tissue from necrotic damage during ischemia, and also has an inhibitory effect on cardiac tissue apoptosis. In addition, Oxfenicine promotes lipolysis in a high-fat diet rat model. Oxfenicine can be used in the study of cardiovascular and metabolic diseases .
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-
- HY-P1098
-
|
|
Annexin A
NF-κB
|
Inflammation/Immunology
|
|
Ac2-26 is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ameliorates lung ischemia-reperfusion injury. Ac2-26 also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
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-
- HY-101096R
-
|
MK-8998 (Standard); CX-8998 (Standard); JZP385 (Standard)
|
Calcium Channel
Reference Standards
|
Neurological Disease
Cancer
|
|
Suvecaltamide (Standard) is the analytical standard of Suvecaltamide (HY-101096). This product is intended for research and analytical applications. Suvecaltamide (MK-8998) is a selective T-type calcium channel inhibitor with oral efficacy. Suvecaltamide exhibits no cytotoxicity in myeloma cell lines and does not affect the antitumor efficacy of Bortezomib (BTZ). Suvecaltamide reverses BTZ-induced peripheral neuropathy (CIPN) in mouse and rat models, and helps inhibit myeloma growth .
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-
- HY-B1130R
-
|
|
Reference Standards
COX
|
Inflammation/Immunology
|
|
Isoxicam (Standard) is the analytical standard of Isoxicam (HY-B1130). This product is intended for research and analytical applications. Isoxicam is an orally active nonsteroidal anti-inflammatory compound and a COX-1/COX-2 inhibitor. Isoxicam exhibits potent anti-inflammatory activity in rat models of inflammation and significantly lower ulcerogenic risk. Isoxicam can be used for the study of inflammatory diseases and rheumatic disorders .
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-
- HY-W700639
-
|
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Tolafentrine, a dual-selective phosphodiesterase 3/4 (PDE3/4) inhibitor, has been shown to have significant acute and chronic effects in a unilateral diacetamide-induced rat pulmonary hypertension model. Experiments show that long-term administration can significantly alleviate all unilateral bisacetamide-induced hemodynamic and gas exchange abnormalities, reduce right ventricular hypertrophy, and normalize pulmonary vascular remodeling changes .
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-
- HY-P1098A
-
|
|
Annexin A
NF-κB
|
Inflammation/Immunology
|
|
Ac2-26 TFA is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ameliorates lung ischemia-reperfusion injury. Ac2-26 also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
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-
- HY-179700
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-61 is an orally active COX-2 inhibitor with an IC50 of 22 µM, also inhibits COX-1 with an IC50 of 43 µM. COX-2-IN-61 exhibits anti-inflammation effects in a Carrageenan (HY-125474) induced rat paw edema model, with promising safety profiles. COX-2-IN-61 can be used for the research of inflammation .
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-
- HY-179684
-
|
|
CGRP Receptor
5-HT Receptor
ERK
Epigenetic Reader Domain
|
Neurological Disease
|
|
PCC0105005 is a dual-target CGRP Receptor antagonist (IC50 = 1.01 nM) and a partial agonist of 5-HT1F Receptor (EC50 = 77.91 nM). PCC0105005 shows significant efficacy in the rat model of migraine. PCC0105005 significantly reduces the expression of CGRP and c-Fos proteins, and inhibits the phosphorylation levels of ERK and CREB. PCC0105005 can be used for research on migraine .
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-
- HY-W931056
-
|
|
TRP Channel
|
Neurological Disease
|
|
AMG-628 is an orally active inhibitor for TRPV1, that inhibits Capsaicin (HY-10448) or acid (pH 5)-induced Ca 2+ influx into TRPV1- expressing CHO cell with IC50 of 4.9 and 3.1 nM. AMG-628 exhibits analgesic activity in Capsaicin (HY-10448)-induced rat model, and exhibits a half-life of 2.4 h in rats .
|
-
- HY-153968
-
|
|
Xanthine Oxidase
URAT1
|
Metabolic Disease
|
|
URAT1&XO inhibitor 1 (compound 29) is a dual inhibitor of both URAT1 (IC50=~10 μM) and Xanthine Oxidase (IC50=1.01 μM). URAT1&XO inhibitor 1 results hypouricemic effect in potassium oxonate-induced hyperuricemia rat model. URAT1&XO inhibitor 1 is used for hyperuricemia research .
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-
- HY-100840A
-
|
4-Carboxy-3-hydroxyphenylglycine
|
mGluR
|
Neurological Disease
|
|
(RS)-4C3HPG (4-Carboxy-3-hydroxyphenylglycine) is an effective competitive antagonist at the metabotropic glutamate receptor 1 (mGluR1) in the central nervous system, and it is also an agonist at mGluR2/3. (RS)-4C3HPG exhibits neuroprotective effects in an acute global ischemia rat model .
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-
- HY-P990257
-
|
|
c-Fms
|
Cancer
|
|
Anti-Mouse CSF1 Antibody (5A1) is a rat-derived anti-mouse CSF1 IgG1 κ type antibody inhibitor. Anti-Mouse CSF1 Antibody (5A1) can inhibit cells proliferation and macrophage-induced invasion. Anti-Mouse CSF1 Antibody (5A1) shows potent anti-tumor effect in various tumor models, such as neuroblastoma .
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-
- HY-10554
-
|
|
nAChR
|
Neurological Disease
|
|
WYE-103914 is an orally active α7 nAChR (EC50 = 0.49 µM for rat α7 nAChR, EC50 = 0.57 µM for human α7 nAChR) agonist. WYE-103914 exhibits the ability to enhance memory in multiple cognitive models. WYE-103914 is used in combination with antipsychotic drugs. WYE-103914 can be used for research on schizophrenia .
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-
- HY-165528
-
|
XC8
|
CCR
|
Inflammation/Immunology
|
|
Histamine glutarimide (XC8) is an orally active anti-asthma agent. Histamine glutarimide blocks the maturation of chemokines (CCL2, CCL7, CCL8, CCL13) and inhibits the migration of eosinophils and the degranulation of mast cells. In asthma models induced by carrageenan and rat ovalbumin, Histamine glutarimide can reduce airway resistance and the count of eosinophils in bronchoalveolar lavage fluid. Histamine glutarimide can be used in asthma research .
|
-
- HY-118156
-
|
|
Others
|
Others
|
|
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
|
-
- HY-158231
-
|
F127DA
|
Integrin
FAK
|
Inflammation/Immunology
|
|
Polyether F127 Diacrylate (F127DA) is an acrylated polyethylene glycol-polypropylene glycol-polyethylene glycol triblock copolymer. Polyether F127 Diacrylate rapidly crosslinks and cures into a gel under ultraviolet or visible light with the action of a photoinitiator. Polyether F127 Diacrylate exhibits excellent thermogelation properties and favorable biosafety. Polyether F127 Diacrylate can upregulate the Integrin-FAK pathway, enhance collagen production, increase the protein and gene expression levels of COL-1/SCX, and promote fibroblastic differentiation of periodontal ligament stem cells. Polyether F127 Diacrylate promotes periodontal ligament regeneration and reduces abnormal healing in a rat model of delayed replanted teeth . Polyether F127 Diacrylate promotes functional osteochondral regeneration in a rat model of osteoarthritis. Polyether F127 Diacrylate supports adipose tissue survival, rendering it suitable for breast reconstruction applications. Polyether F127 Diacrylate can be used in studies related to periodontal ligament injury, breast defect and osteoarthritis .
|
-
- HY-145607
-
-
- HY-B2012
-
|
DPX-H6573
|
Environmental Pollutants
Fungal
|
Infection
|
|
Flusilazole (DPX-H6573) is a broad-spectrum fungicide and cytochrome P-450 inhibitor that can be used in studies related to fungal infections .
|
-
- HY-176234
-
-
- HY-B0130R
-
|
S-9490 (Standard)
|
Angiotensin-converting Enzyme (ACE)
NF-κB
STAT
Sirtuin
Reference Standards
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Perindopril (Standard) is the analytical standard of Perindopril. This product is intended for research and analytical applications. Perindopril (S-9490) is an orally available, long-acting angiotensin-converting enzyme (ACE) inhibitor. Perindopril inhibits inflammatory cell influx and intimal thickening, preserving elastin on the inside of the aorta. Perindopril effectively inhibits experimental abdominal aortic aneurysm (AAA) formation in a rat model and reduces pulmonary vasoconstriction in rats with pulmonary hypertension .
|
-
- HY-10456
-
|
|
p38 MAPK
Casein Kinase
Wnt
|
Inflammation/Immunology
|
|
TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model .
|
-
- HY-120485
-
|
IRFI-016
|
p38 MAPK
ERK
PKC
|
Cardiovascular Disease
|
|
Raxofelast (IRFI-016) is an antioxidant agent in various models of ischemia-reperfusion injury. Raxofelast has antiproliferative activity in H2O2-stimulated rat aortic smooth muscle cells. Raxofelast attenuates the activation of mitogen-activating protein kinase (MAPK), ERK kinase 1, 2 (MEK1,2) and protein kinase C (PKC) without affecting Ras expression .
|
-
- HY-170586
-
-
- HY-167715
-
|
|
Histamine Receptor
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Traxanox is an orally available diuretic that enhances phagocytosis of yeast granules by mouse peritoneal macrophages and rat peritoneal polymorphonuclear leukocytes in vitro.
Traxanox inhibits IgE-mediated histamine release and cyclic AMP phosphodiesterase
activity.Traxanox exhibits anti-inflammatory activity, as it inhibits the anaphylactoid reaction and reduces pleural fluid accumulation in experimental models of inflammation. Traxanox also demonstrates a synergistic effect when combined with hydrocortisone or indomethacin in suppressing adjuvant arthritis in rats.
|
-
- HY-173503
-
|
|
GLUT
|
Metabolic Disease
|
|
DS-1150b is an orally active GLUT4 activator. DS-1150b has the activity of activating GLUT4 transport and can promote the translocation of GLUT4 to the cell membrane in skeletal muscle cells. DS-1150b has shown hypoglycemic effects in the Zucker obese rat model and can be used in the study of type 2 diabetes mellitus (T2DM) .
|
-
- HY-N0321
-
|
trans-Caftaric acid
|
Others
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Caftaric acid (trans-Caftaric acid) is a polyphenolic antidiuretic, antioxidant and anti-apoptotic agent that can be hydrolyzed by intestinal microbial esterases. Caftaric acid exerts its antioxidant and potential anti-inflammatory effects mainly through intestinal microbial metabolism. Caftaric acid can reduce renal damage, restore electrolyte balance, renal function indicators and antioxidant enzyme activities in a rat albinism model, and further exert anti-oxidative stress and anti-inflammatory activities .
|
-
- HY-P3354
-
|
|
iGluR
|
Neurological Disease
|
|
p3Ysh-3 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 1.09 μM. p3Ysh-3 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p3Ysh-3 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-117560
-
|
|
GABA Receptor
|
Neurological Disease
|
|
PWZ-029 is a selective inverse agonist for 5 GABAA receptors. PWZ-029 is a benzodiazepine site ligand. PWZ-029 shows a weak but significant partial agonistic effect at 1- and 3-containing receptors. PWZ-029 significantly increases retention session latency in mouse fibroblast cells. PWZ-029 can improve object recognition in normal and scopolamine-treated rat model .
|
-
- HY-153780
-
|
DC-806; LY4100504; S-011806
|
Interleukin Related
|
Inflammation/Immunology
|
|
Navepdekinra (DC-806) is an orally active, potent interleukin-17A (IL-17A) inhibitor (IC50 = 10.81 nM). Navepdekinra disrupts the IL-17A protein-receptor interaction, suppressing the downstream pro-inflammatory signaling pathway. Navepdekinra inhibits arthritis in a collage-induced arthritis (CIA) rat model. Navepdekinra can be used for psoriasis, psoriatic arthritis, and ankylosing spondylitis .
|
-
- HY-132610A
-
|
ALN-AS1 sodium
|
Small Interfering RNA (siRNA)
|
Metabolic Disease
|
|
Givosiran (ALN-AS1) sodium is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran sodium downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran sodium demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran sodium can be used for the research of acute hepatic porphyria (AHP) .
|
-
- HY-103327R
-
|
|
Reference Standards
Cannabinoid Receptor
|
Metabolic Disease
|
|
MJ15 (Standard) is the analytical standard of MJ15 (HY-103327). This product is intended for research and analytical applications. MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
|
-
- HY-147428
-
|
MM-110; (±)-18-Methoxycoronaridine
|
nAChR
Parasite
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Infection
Neurological Disease
|
|
Zolunicant (MM-110) is a potent inhibitor against nicotinic α3β4 receptors with an IC50 of 0.90 μM to combat addiction. Zolunicant can decrease the self-administration of several addictive agents including morphine, methamphetamine, nicotine, and ethanol in rat model. Zolunicant can be studied as a potential research for multiple forms of agent abuse . Zolunicant also reveals a potent leishmanicide effect against Leishmania amazonensis .
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- HY-162640
-
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ROR
|
Cancer
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LDR102 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with Ki of 0.10 μM. LDR102 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC50 of 0.36 μM, 1.37 μM and 0.47 μM. LDR102 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
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-
- HY-132610
-
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ALN-AS1
|
Small Interfering RNA (siRNA)
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Metabolic Disease
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Givosiran (ALN-AS1) is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran can be used for the research of acute hepatic porphyria (AHP) .
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- HY-U00237B
-
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Adrenergic Receptor
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Others
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L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
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-
- HY-B0596
-
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TA-0910
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Thyroid Hormone Receptor
Apoptosis
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Neurological Disease
Endocrinology
|
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Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
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-
- HY-155238
-
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GABA Receptor
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Neurological Disease
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|
E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg) .
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- HY-121856
-
|
|
Others
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Inflammation/Immunology
|
|
Flumizole, a derivative of substituted 5,6-diaryl-2,3-dihydroimidazo[2,1-b]thiazoles, was synthesized and evaluated for its immunoregulatory and anti-inflammatory properties in animal models such as rat adjuvant-induced arthritis and mouse oxazolone-induced contact sensitivity assays. This compound class combines structural elements from flumizole and levamisole, aiming to enhance therapeutic efficacy. Symmetrically substituted 5,6-diaryl compounds with specific alkyl heteroatom or halogen substitutions showed optimal potency in the arthritis model. However, variations in activity were less consistent in the contact sensitivity assay. Flumizole and related compounds demonstrate potential as dual-action agents, targeting inflammation and immune modulation, offering promise for therapeutic development in immune-related disorders .
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-
- HY-145814
-
|
|
HSP
Fungal
|
Infection
|
|
HSP90-IN-9 is a potent and selective HSP90 inhibitor. HSP90-IN-9 displays a fungicidal effect in a dose-dependent manner. HSP90-IN-9 inhibits fungal biofilm formation and fungal morphological changes after being combined with FLC. HSP90-IN-9 recovers FLC resistance by down-regulating the expression of related genes (ERG11, CDR1 and CDR2) .
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-
- HY-115566
-
|
|
LPL Receptor
Smo
|
Inflammation/Immunology
|
|
S1PL-IN-31 (compound ) is an oral active sphingosine-1-phosphate (S1P) lyase inhibitor with the IC50 of 210 nM. S1PL-IN-31 is Smoothened receptor antagonist with the IC50 of 440 nM. S1PL-IN-31 can be used for study of experimental autoimmune encephalomyelitis .
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-
- HY-W015815
-
|
|
Endogenous Metabolite
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Neurological Disease
|
|
6-Methylnicotinamide is a nicotinamide derivative. 6-methylnicotinamide is also an endogenous metabolite and its sudden increase in the acute stages of intracerebral hemorrhage (ICH) exacerbates neurological damages in rat model. 6-Methylnicotinamide can significantly enhance the coordination effect between acylamino and undercoordinated defective Pb 2+ cations. 6-Methylnicotinamide results in enhanced efficiency of perovskite solar cells to 24.33% with excellent environmental storage, heat, and light stabilities .
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-
- HY-P990264
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
|
Anti-Mouse CD70 Antibody (FR70) is a rat-derived ant-mouse CD70 IgG2b κ type antibody inhibitor. Anti-Mouse CD70 Antibody (FR70) decreases CD4 +, CD8 + T cells and eosinophils. Anti-Mouse CD70 Antibody (FR70) shows potent anti-inflammatory and anti-immune effects on allergic lung inflammation and cardiac transplant mice models .
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-
- HY-W028142
-
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|
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
|
Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research .
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- HY-12119B
-
|
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
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GW274150 (dihydrochloride) is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 (dihydrochloride) displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 (dihydrochloride) exerts a protective role in an acute model of lung injury inflammation .
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-
- HY-180527
-
|
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SGLT
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
SGLT2-IN-5 (Compound 99) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 23, and 58 nM respectively. SGLT2-IN-5 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-5 can be used for the study of type 2 diabetes .
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-
- HY-114873
-
|
LY25684
|
Phospholipase
COX
Lipoxygenase
Leukotriene Receptor
|
Inflammation/Immunology
|
|
LY256548 (LY25648) is an orally available anti-ischemic and anti-inflammatory compound with central nervous system activity. LY256548 is an inhibitor of phospholipase A2, 5-lipoxygenase (5-LOX), and COX, and inhibits A23187 (HY-N6687)-stimulated leukotriene B4 production. LY256548 inhibits bone damage and paw swelling in the rat Freund's complete adjuvant-induced arthritis (FCA) model .
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- HY-119821R
-
|
|
Reference Standards
Glycosidase
|
Infection
|
|
Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
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-
- HY-117133
-
|
SF0166
|
Integrin
|
Metabolic Disease
|
|
Nesvategrast (SF0166) is a potent and selective αvβ3 antagonist with IC50 values of 0.6 nM, 8 nM, and 13 nM for αvβ3, αvβ6, and αvβ8, respectively. Nesvategrast inhibits cellular adhesion to vitronectin across human, rat, rabbit, and dog cell lines with IC50 values of 7.6 pM to 76 nM. Nesvategrast decreases neovascularization in the oxygen-induced retinopathy mouse model .
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-
- HY-N0665R
-
|
(8E)-Nuezhenide (Standard)
|
Reference Standards
NF-κB
Wnt
|
Inflammation/Immunology
|
|
Specnuezhenide (Standard) is the analytical standard of Specnuezhenide. This product is intended for research and analytical applications. Specnuezhenide ((8E)-Nuezhenide) is isolated from the fruits of?Ligustrum lucidum. Specnuezhenide ((8E)-Nuezhenide) can inhibit IL-1β-induced inflammation in chondrocytes via inhibition of NF-κB and wnt/β-catenin signaling. Specnuezhenide ((8E)-Nuezhenide) exerts anti-inflammatory effects in a rat model of osteoarthritis (OA) .
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-
- HY-180828
-
|
|
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
iNOs-IN-8 (Compound 13h) is an efficient and highly selective inducible nitric oxide synthase (iNOS) inhibitor, with an IC50 of 238 nM. iNOs-IN-8 exhibits significant neuroprotective effects in oxygen-glucose deprivation/reoxygenation (OGD/R) and hydrogen peroxide-induced neuronal and endothelial cell damage. iNOs-IN-8 significantly reduces the volume of cerebral infarction and improves neurological function in rat models. iNOs-IN-8 can be used for the study of ischemic stroke .
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-
- HY-17444
-
|
|
PPAR
|
Metabolic Disease
Cancer
|
|
Tesaglitazar is a dual-target PPARα/γ agonist with an EC50 of 13.4 μM for rat PPARα and 3.6 μM for human PPARα. Tesaglitazar affects lipid and glucose metabolism by activating PPARα and PPARγ receptors, and has the potential to improve blood sugar and relieve pain. Tesaglitazar can be used to induce in vivo tumor models and can be used in the study of type 2 diabetes, dyslipidemia, and neuropathic pain .
|
-
- HY-180528
-
|
|
SGLT
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
SGLT2-IN-6 (Compound 101) is an orally active SGLT2 inhibitor with IC₅₀ values for SGLT2, SGLT1, and DPP4 of 0.8, 6.7, and 72 nM respectively. SGLT2-IN-6 controls blood sugar levels in diabetic rat models and increases the levels of active GLP-1. SGLT2-IN-6 can be used for the study of type 2 diabetes .
|
-
- HY-125064
-
|
|
Src
|
Cancer
|
|
AP22408 is a nonpeptide inhibitor against Src SH2 with an IC50 value of 0.3 μM. AP22408 inhibits rabbit osteoclast-mediated resorption of dentine, exhibits bone-targeting properties based on a hydroxyapatite adsorption assay and demonstrates in vivo antiresorptive activity in a parathyroid hormone-induced rat model. AP22408 is proming for rasearch of osteoporosis and other bone-related diseases such as Paget’s disease, osteolytic bone metastasis and hypercalcemia associated with malignancy .
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-
- HY-12119
-
|
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
GW274150 is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 also displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 exerts a protective role in an acute model of lung injury inflammation .
|
-
- HY-137307
-
|
(22S)-Hydroxycholesterol
|
LXR
ATP-binding cassette (ABC) transporters
|
Inflammation/Immunology
|
|
Cholest-5-ene-3ß,22(S)-diol ((22S)-Hydroxycholesterol) is an orally active oxysterol with no significant cytotoxic, oxidative, or inflammatory effects on human prokaryotic leukemia cells. Cholest-5-ene-3ß,22(S)-diol inhibits weight gain and increased serum triacylglycerol (TAG) levels in rat models .
|
-
- HY-115861
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
UCM765 is a selective MT2-type melatonin receptor ligand with hypnotic, analgesic and anxiolytic activities. The partial agonist effect of UCM765 has attracted attention in pharmacological studies. By structurally modifying UCM765, its water solubility and metabolic stability can be improved, thereby increasing its bioavailability. The biological activity of UCM765 has been verified in a rat model, supporting its potential for further pharmacological studies .
|
-
- HY-123500
-
|
|
Cytochrome P450
|
Cancer
|
|
CGP-45688 is an orally active non-steroidal aromatase inhibitor with an ED50 of 30-100 μg/kg. CGP-45688 can reduce the level of estrogen in the body, thereby inhibiting the growth of estrogen-dependent tumors. CGP-45688 inhibits the growth of estrogen-dependent breast tumors in rat models. CGP-45688 disrupts the ovarian cycle and inhibits the weight of the uterus. CGP-45688 can be used for the study of breast cancer .
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-
- HY-W747879
-
|
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
|
|
Diclofenac Amide- 13C6 is the 13C-labeled Diclofenac amide (HY-134521). Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg) .
|
-
- HY-B0130S1
-
-
- HY-Y0546
-
|
|
Environmental Pollutants
Endogenous Metabolite
Photosensitizer
|
Cancer
|
|
Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
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-
- HY-12119A
-
|
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
GW274150 phosphate is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 phosphate displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 phosphate exerts a protective role in an acute model of lung injury inflammation .
|
-
- HY-11052A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
|
-
- HY-W028142R
-
|
|
Reference Standards
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
|
Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research .
|
-
- HY-119530R
-
|
BW 57-323 (Standard)
|
Nucleoside Antimetabolite/Analog
Reference Standards
|
Others
|
|
Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
|
-
- HY-169986S
-
|
|
JAK
|
Inflammation/Immunology
|
|
TyK2-IN-21-d3 (Compound 3c) is the orally active prodrug of the tyrosine kinase 2. TyK2-IN-21-d3 exhibits good chemical stability in aqueous system under different pHs. TyK2-IN-21-d3 alleviates the effect of gastric acid changes on drug absorption and improve the drug bioavailability in rat model .
|
-
- HY-162639
-
|
|
Glycosidase
Cholinesterase (ChE)
|
Neurological Disease
Metabolic Disease
|
|
α-Glucosidase-IN-68 (Compound 2) is an inhibitor for α-Glucosidase, AChE, and BChE, with IC50 of 0.251, 0.774 and 0.793 μM, respectively. α-Glucosidase-IN-68 exhibits antioxidant efficacy, with IC50 of 0.69 μM and 0.02 μM, in DPPH and ABTS experiments. α-Glucosidase-IN-68 exhibits antidiabetic effect in Streptozotocin (HY-13753)-induced diabetic rat models .
|
-
- HY-113427R
-
|
|
Endogenous Metabolite
Reference Standards
Bcl-2 Family
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
trans-Vaccenic acid (Standard) is the analytical standard of trans-Vaccenic acid (HY-113427). This product is intended for research and analytical applications. trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity.
|
-
- HY-128932R
-
|
MT-141 (Standard)
|
Reference Standards
Antibiotic
Bacterial
PPAR
Prostaglandin Receptor
PTEN
Akt
mTOR
|
Infection
Cardiovascular Disease
Endocrinology
|
|
Cefminox (sodium) (MT-141) (Standard) is the analytical standard of Cefminox (sodium). This product is intended for research and analytical applications. Cefminox sodium is a semisynthetic cephamycin, which exhibits antibacterial activity. Cefminox sodium is a broad-spectrum, bactericidal cephalosporin antibiotic. Cefminox sodium also acts as a dual agonist of prostacyclin receptor (IP) and PPARγ. Cefminox sodium upregulates cAMP production and PTEN expression and inhibits Akt/mTOR signaling. Cefminox sodium also prevents pulmonary arterial hypertension in rat model .
|
-
- HY-W015815R
-
|
|
Reference Standards
Endogenous Metabolite
|
Neurological Disease
|
|
6-Methylnicotinamide is a nicotinamide derivative. 6-methylnicotinamide is also an endogenous metabolite and its sudden increase in the acute stages of intracerebral hemorrhage (ICH) exacerbates neurological damages in rat model. 6-Methylnicotinamide can significantly enhance the coordination effect between acylamino and undercoordinated defective Pb2+ cations. 6-Methylnicotinamide results in enhanced efficiency of perovskite solar cells to 24.33% with excellent environmental storage, heat, and light stabilities .
|
-
- HY-113427S
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Bcl-2 Family
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
trans-Vaccenic acid-d13 is deuterium labeled trans-Vaccenic acid (HY-113427). trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity .
|
-
- HY-P1098B
-
|
|
IKK
|
Inflammation/Immunology
|
|
Ac2-26 ammonium is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 ammonium induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ammonium ameliorates lung ischemia-reperfusion injury. Ac2-26 ammonium also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-10932
-
|
Ro 13-5057
|
nAChR
iGluR
|
Neurological Disease
|
|
Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders .
|
-
- HY-10281
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
YM-60828 is an FXa inhibitor with antithrombotic properties. In the rat arteriovenous shunt model, YM-60828 does not prolong coagulation time but reduces the levels of thrombin-antithrombin III complex (TAT) in a dose-dependent manner. YM-60828 exhibits only anti-FXa activity and does not show anti-thrombin activity, indicating that its antithrombotic effect is independent of thrombin. Therefore, the antithrombotic effect of YM-60828 can be monitored by TAT .
|
-
- HY-162710
-
|
|
Aminopeptidase
|
Inflammation/Immunology
|
|
LTA4H-IN-5 (Compound H122) is an orally active inhibitor for leukotriene A4 hydrolase (LTA4H), that inhibits the LTA4H aminopeptidase and LTA4H hydrolase with IC50 of 0.38 nM and 16.93 nM. LTA4H-IN-5 exhibits good pharmacokinetic characteristics in C57 mice and ameliorates the DNBS-induced ulcerative enteritis in rat models .
|
-
- HY-10819
-
|
|
Antifolate
|
Cancer
|
|
AG2034 is an inhibitor of glycinamide ribonucleotide formyltransferase (GARFT), with a Ki of 28 nM against human GARFT, and it binds with high affinity to the folate receptor (Kd of 0.0042 nM). Additionally, AG2034 is a substrate for rat liver folylpolyglutamate synthetase, with a Km of 6.4 µM. AG2034 inhibits the growth of L1210 and CCRF-CEM cells, with IC50 values of 4 nM and 2.9 nM, respectively, and it has demonstrated antitumor activity in xenograft models such as 6C3HED .
|
-
- HY-16979
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
RK-851 is a highly selective and orally active δ-opioid receptor antagonist, with a negative logarithm of the antagonist concentration (pA2) of 8.84. TRK-851 exhibits the selectivity for the δ receptor of more than 100 times higher than that for the μ or κ receptors. TRK-851 exhibits a potent antitussive effect in a rat model of capsaicin-induced cough. TRK-851 can be used for research on antitussive effects .
|
-
- HY-124517
-
|
|
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Burimamide is a blocker of histamine H2-receptor. Burimamide inhibits gastric acid secretion evoked by Pentagastrin (HY-A0261) or Gastrin. Burimamide also has alpha-adrenoceptor blocking activity. Burimamide in combination with the H1-receptor antagonist Mepyramine (HY-B1281) shows anti-inflammatory activity in a rat paw edema model induced by Compound 48/80 (HY-115768) .
|
-
- HY-101418R
-
|
|
P2X Receptor
Reference Standards
|
Neurological Disease
|
|
JNJ-47965567 (Standard) is the analytical standard of JNJ-47965567 (HY-101418). This product is intended for research and analytical applications. JNJ-47965567 is a centrally permeable, high-affinity, selective P2X7 antagonist, with pKis of 7.9 and 8.7 for human and rat P2X7, respectively. JNJ-47965567 can be used to probe the role of central P2X7 in rodent models of CNS pathophysiology .
|
-
- HY-120496
-
|
ASP3662
|
11β-HSD
|
Neurological Disease
Metabolic Disease
|
|
Clofutriben (ASP3662) is a selective, orally active and brain-penetrant 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with Ki values of 5.3 nM (human), 2.6 nM (mouse), and 23 nM (rat). Clofutriben inhibits conversion of inactive glucocorticoids to active glucocorticoids, reducing intracellular glucocorticoid exposure. Clofutriben ameliorates neuropathic pain, and restores muscle pressure thresholds in rodent models, while lacking effects in inflammatory pain .
|
-
- HY-163538
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
TYM-3-98 is a selective inhibitor for PI3Kδ, with an IC50 of 7.1 nM. TYM-3-98 inhibits proliferationso of B-lymphoma cells. TYM-3-98 inhibits PI3K/AKT/mTOR signaling pathway through induction of apoptosis. TYM-3-98 exhibits good pahrmacokinetic characters and antitumor efficacy in mouse/rat model, without significant toxicity .
|
-
- HY-B0596A
-
|
TA-0910 acetate
|
Thyroid Hormone Receptor
Apoptosis
|
Neurological Disease
Endocrinology
|
|
Taltirelin acetate (TA-0910) is an acetate form of Taltirelin (TA-0910). Taltirelin (TA-0910) is an orally effective analogue of thyrotropin releasing hormone (TRH) and a TRH receptor (TRH-R) superagonist (IC50 at 910 nM). Taltirelin can cross the blood-brain barrier. Taltirelin stimulates an increase in cytosolic Ca 2+ concentration (Ca 2+ release) with an EC50 value of 36 nM. Taltirelin increases cell viability and reduces apoptosis in SH-SY5Y cells and primary rat mesencephalic neurons treated with MPP+ (HY-W008719) or Rotenone (HY-B1756). Taltirelin has neuroprotective effects in both cellular and animal models of Parkinson's disease. Taltirelin alleviates fatigue-like behavior in mouse models of cancer-related fatigue .
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-
- HY-P99171
-
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|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .
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-
- HY-169404
-
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PPAR
|
Metabolic Disease
|
|
PPARγ agonist 15 (Compound 7c) is an agonist for PPARγ. PPARγ agonist 15 inhibits the expression of alpha-amylase (HPA) and alpha-glucosidase (HLAG) with IC50 of 28.35 µM and 26.21 µM. PPARγ agonist 15 enhances glucose uptake in the L6 myotube cell. PPARγ agonist 15 improves glucose homeostasis, insulin sensitivity, and lipid metabolism in rat Streptozotocin (HY-13753)-induced diabetes model .
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-
- HY-137555
-
|
11-dehydro-2,3-dinor TXB2
|
Endogenous Metabolite
|
Metabolic Disease
|
|
11-dehydro-2,3-dinor Thromboxane B2 (11-dehydro-2,3-dinor TXB2) is a metabolite of the TXA2 inactive metabolite TXB2 (Item No. 19030). It is formed from TXB2 by cytosolic aldehyde dehydrogenase (ALDH) and β-oxidation. Levels of 11-dehydro-2,3-dinor TXB2 are increased 5.2-fold in a surgery-induced rat model of tendon overuse.
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-
- HY-15048
-
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PARP
|
Inflammation/Immunology
|
|
GPI 15427 is a potent inhibitor of the enzyme poly (ADP-ribose) polymerase-1 (PARP-1), which plays a harmful role during inflammation. In a rat model of gut injury and inflammation, including splanchnic artery occlusion (SAO) shock and dinitrobenzene sulfonic acid (DNBS)-induced colitis, GPI 15427 demonstrates strong anti-inflammatory effects that reduces inflammatory cell infiltration, histological injury. GPI 15427 also diminishes the accumulation of poly (ADP-ribose) in the ileum and colon of treated rats .
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-
- HY-109747
-
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MMP
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Cancer
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|
RO-28-2653 is an orally active matrix metalloproteinase (MMP) inhibitor. RO-28-2653 exhibits highly selective inhibitory effects on MMP2, MMP9 and membrane-type 1-MMP, and may reduce side effects (such as musculoskeletal pain) compared to broad-spectrum MMP inhibitors. RO-28-2653 shows significant tumor growth inhibition in a rat prostate model. RO-28-2653 can be used in studies of hormone-sensitive tumors .
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- HY-B1350A
-
|
Sodium fusidate; SQ-16360
|
Bacterial
Antibiotic
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
Fusidic acid sodium salt is an orally available antibacterial agent that inhibits bacterial protein synthesis by preventing the release of translation elongation factor G (EF-G) from ribosomes. Fusidic acid sodium salt inhibits the inhibitory and activating effects of interleukins IL-1 and IL-6 on glucose-induced insulin production and exhibits antidiabetic effects in a rat model. Fusidic acid sodium salt improves the symptoms of colitis in rats and inhibits the growth of Toxoplasma gondii and Listeria monocytogenes EGD in vitro, but not in mice .
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-
- HY-111164
-
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p38 MAPK
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CBS-3595 is a dual inhibitor of p38 MAP kinase and phosphodiesterase 4 with anti-inflammatory and anti-allodynic activities. CBS-3595 reduces the production of the proinflammatory cytokine IL-6 and increases the levels of the anti-inflammatory cytokine IL-10 in rats. CBS-3595 reduces paw oedema formation in the Complete Freund’s adjuvant (CFA) (HY-153808)-induced arthritis rat model. CBS-3595 is promising for research of autoimmune diseases .
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-
- HY-169940
-
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HDAC
|
Inflammation/Immunology
|
|
Fibrostat (Compound 5n) is a selective HDAC6 inhibitor that exerts antifibrotic effects by inhibiting HDAC6 activity, with an IC50 value of 63 nM. It also exhibits good selectivity over HDAC1, HDAC3, HDAC5, HDAC8, HDAC10, and HDAC11. Fibrostat significantly downregulates fibrotic markers (fibronectin and collagen 1) in fibroblasts. Additionally, Fibrostat demonstrated no toxicity in rat-perfused heart and zebrafish larvae models. Fibrostat shows potential for research into fibrosis-related diseases .
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-
- HY-109106A
-
|
SK-1403; AJT240; PLS240
|
CaSR
|
Endocrinology
|
|
Upacicalcet sodium is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM). Upacicalcet sodium reduces serum intact parathyroid hormone (iPTH) and serum Ca 2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet sodium sodium improves vascular calcification and bone disorders in the Adenine (HY-B0152)-induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet sodium sodium inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD). Upacicalcet sodium is useful for studying SHPT .
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-
- HY-108467R
-
|
Nahlsgen (Standard)
|
γ-Glutamyl Transferase (GGT)
Reference Standards
|
Cardiovascular Disease
|
|
GGsTop (Standard) is the analytical standard of GGsTop. This product is intended for research and analytical applications. GGsTop (Nahlsgen) is a potent, non-toxic, highly selective and irreversible γ-GGT inhibitor, with a Ki of 170 μM for Human GGT. GGsTop shows a pKa of 9.71, also exhibits Kons of 150 and 51 M-1 s-1 against E.coli GGT and human GGT, respectively. GGsTop protects hepatic ischemia-reperfusion injury in rat model .
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-
- HY-109106
-
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SK-1403 free acid; AJT240 free acid; PLS240 free acid
|
CaSR
|
Endocrinology
|
|
Upacicalcet is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM). Upacicalcet reduces serum intact parathyroid hormone (iPTH) and serum Ca2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet improves vascular calcification and bone disorders in the Adenine (HY-B0152)-induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD). Upacicalcet is useful for studying SHPT .
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-
- HY-101046
-
|
|
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
|
Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research .
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-
- HY-175318S
-
|
|
MDM-2/p53
|
Cancer
|
|
p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer .
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-
- HY-P99124
-
|
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CD3
|
Inflammation/Immunology
|
|
Anti-Mouse CD3 Antibody (17A2) is an anti-mouse CD3 IgG2b antibody inhibitor derived from the host Rat. Anti-Mouse CD3 Antibody (17A2) enhances T-cell proliferation and activation and stimulate IFN-γ or IL-17 production in splenic T cells. Anti-Mouse CD3 Antibody (17A2) significantly suppresses mortality in Graft-versus-host disease (GVHD) mice models .
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-
- HY-162347
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Nav1.7-IN-13 (compound 3g) is a sodium channel inhibitor that significantly inhibits Veratridine (HY-N6691)-induced neuronal activity. Nav1.7-IN-13 inhibits total Na+ current in DRG neurons in a concentration-dependent manner; slows down the activation of Navs. Nav1.7-IN-13 significantly alleviated mechanical pain behavior in a rat model of nerve injury (SNI) and had analgesic activity .
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-
- HY-168333
-
|
|
5-HT Receptor
mTOR
CDK
|
Neurological Disease
|
|
5-HT6 inverse agonist 1 (Compound 33) is an antagonist for 5-HT6 receptor with a Ki of 23 nM and a Kb of 6.62 nM. 5-HT6 inverse agonist 1 inhibits the 5-HT6R mediated Cdk5 and mTOR signaling pathway. 5-HT6 inverse agonist 1 reduces tactile hypersensitivity in spinal nerve ligation (SNL)-induced rat model .
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-
- HY-181482
-
|
|
DAGL
|
Neurological Disease
|
|
A1480LS is a peripherally restricted, orally active covalent and irreversible inhibitor of DAGLα and DAGLβ, with IC50 values of 6 nM and 4 nM against human targets, respectively, and IC50 values ≤15 nM across mouse, rat, dog, monkey and human systems. A1480LS reduces the levels of 2-arachidonoylglycerol, arachidonic acid, and cyclooxygenase- and lipoxygenase-derived eicosanoids. A1480LS inhibits injury-induced production of 2-arachidonoylglycerol and arachidonic acid in the peripheral sciatic nerve, and suppresses the responses of high-threshold and wide-dynamic-range-like dorsal horn neurons to mechanical stimulation. A1480LS alleviates pain behaviors in rat models of inflammatory pain, neuropathic pain and chemotherapy-induced peripheral neuropathy .
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-
- HY-B0199A
-
|
RS 61443 hydrochloride; TM-MMF hydrochloride
|
Interleukin Related
|
Inflammation/Immunology
|
|
Mycophenolate mofetil (RS 61443; TM-MMF) hydrochloride is an orally active antimetabolic immunosuppressant with antiproliferative and anti-inflammatory properties. Mycophenolate mofetil hydrochloride significantly inhibits the production of B, T lymphocytes and the proliferation of smooth muscle cells by selectively blocking the de novo purine synthesis pathway. Mycophenolate mofetil hydrochloride effectively reduces adventitial inflammation, medial necrosis and intimal thickening in rat aortic allografts, and decreases the number of lymphocytes expressing the IL-2 receptor, thereby delaying xenograft rejection. Mycophenolate mofetil hydrochloride shows certain toxicity in a hamster-to-rat limb xenotransplantation model when used in combination with FK506 (HY-13756). Mycophenolate mofetil hydrochloride is widely used in studies related to allograft arteriosclerosis (chronic rejection) .
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-
- HY-186191
-
-
- HY-182351
-
|
|
Calcium Channel
|
Neurological Disease
|
|
ONO-2921 is an orally active and selective N-type calcium channel blocker. ONO-2921 functionally blocks N-type calcium channels. ONO-2921 reduces paw withdrawal responses during persistent nociception and hyperalgesia to heat in neuropathic pain models. ONO-2921 can be used for research on neuropathic pain and nociceptive pain .
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-
- HY-182928
-
|
|
LRRK2
Mps1
|
Neurological Disease
|
|
LRRK2-IN-21 is a selective, blood-brain barrier-permeable LRRK2 kinase inhibitor with an IC50 of 0.35 nM. LRRK2-IN-21 inhibits TTK kinase with an IC50 of 70 nM. LRRK2-IN-21 is applicable to the research of Parkinson's disease .
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-
- HY-19109
-
|
|
Leukotriene Receptor
|
Others
|
|
RG-7152 is a tetrazolyl-substituted leukotriene D4 receptor antagonist that can induce peroxisomal β-oxidation and peroxisome bifunctional enzymes (PBEs) in hepatocytes in various animal models. It has been shown to significantly increase PBE levels and β-oxidation activity in rat and mouse liver homogenates, while smaller effects were observed in guinea pigs and monkeys and no effect in dogs. In vitro studies have also shown that it can induce PBEs comparable to clofibric acid, indicating its potential as a peroxisome proliferator .
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-
- HY-180822
-
|
|
COX
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
COX-2-IN-63 (Compound 6k) is an orally active COX-2 inhibitor with an IC50 of 0.89 μM. COX-2-IN-63 reduces the levels of inflammatory mediators PGE2, TNF-α, and IL-6. COX-2-IN-63 can effectively alleviate acute inflammation in a rat paw edema model and has a lower risk of gastrointestinal side effects. COX-2-IN-63 can be used in anti-inflammatory research .
|
-
- HY-B1119
-
|
|
Environmental Pollutants
Antibiotic
Apoptosis
Bacterial
Fungal
|
Infection
Cancer
|
|
Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 µM and 10 µM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
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-
- HY-Y0546S2
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Photosensitizer
|
Cancer
|
|
Benzophenone- 13C is the 13C labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
- HY-169949
-
|
|
MAP3K
NF-κB
MMP
Leukotriene Receptor
|
Inflammation/Immunology
|
|
TAK-756 is a selective transforming growth factor β-activated kinase 1 (TAK1) inhibitor with a target pIC50 of 8.6. TAK-756 can inhibit TAK1 autophosphorylation and downstream NF-κB phosphorylation, suppress the production of inflammatory and catabolic factors such as MMP-3 and IL-6. TAK-756 exhibits anti-inflammatory effects in a rat joint inflammation model. TAK-756 can be used for the research of inflammatory joint disease, osteoarthritis .
|
-
- HY-100769
-
|
YL0919
|
5-HT Receptor
|
Neurological Disease
|
|
Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [ 3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder .
|
-
- HY-118152
-
|
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
Org-12962 is a potent, selective and brain-penetrant and 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively .Org-12962 displays antiaversive effects in a rat model of panic-like anxiety .
|
-
- HY-123468
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Tyrosine Hydroxylase
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-123468A
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 dihydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 dihydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein, and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 dihydrochloride is an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-171174
-
|
|
CDK
STAT
Wnt
|
Cancer
|
|
CDK8-IN-16 (Compound 51) is an orally active dual inhibitor for CDK8 and CDK19 wih IC50 of 5.1 nM and 5.6 nM. CDK8-IN-16 inhibits the phospho-STAT1 SER727 with an IC50 of 17.9 nM in SW620 cell, inhibits WNT signaling pathway with an IC50 of 7.2 nM in 7dF3 cell. CDK8-IN-16 exhibits good pharmacokinetic characteristics in rat models with an oral bioavailability of 57% .
|
-
- HY-168096
-
|
|
NO Synthase
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
iNOs-IN-5 (Compound BN-4) is an inhibitor for iNOS with an IC50 of 0.1707 μM, and reduces NO levels in LPS (HT-D1056)-induced RAW264.7 cells. iNOs-IN-5 reduces the hypoxic injury stimulated ROS and lactate dehydrogenase expression, and exhibits anti-necrosis and anti-apoptosis efficacy. iNOs-IN-5 exhibits anti-cerebral ischemia and neuroprotective activities in SD rat models. iNOs-IN-5 is blood-brain barrier penetrable .
|
-
- HY-Y0546S1
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Photosensitizer
|
Cancer
|
|
Benzophenone-d5 is the deuterium labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
- HY-Y0546S
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
Photosensitizer
|
Cancer
|
|
Benzophenone-d10 is the deuterium labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
- HY-116062A
-
|
|
Histone Methyltransferase
|
Neurological Disease
|
|
JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
|
-
- HY-B0199S
-
|
|
Isotope-Labeled Compounds
Interleukin Related
|
Cancer
|
|
Mycophenolate Mofetil-d4 is the deuterium labeled Mycophenolate Mofetil. Mycophenolate mofetil (RS 61443; TM-MMF) hydrochloride is an orally active antimetabolic immunosuppressant with antiproliferative and anti-inflammatory properties. Mycophenolate mofetil hydrochloride significantly inhibits the production of B, T lymphocytes and the proliferation of smooth muscle cells by selectively blocking the de novo purine synthesis pathway. Mycophenolate mofetil hydrochloride effectively reduces adventitial inflammation, medial necrosis and intimal thickening in rat aortic allografts, and decreases the number of lymphocytes expressing the IL-2 receptor, thereby delaying xenograft rejection. Mycophenolate mofetil hydrochloride shows certain toxicity in a hamster-to-rat limb xenotransplantation model when used in combination with FK506 (HY-13756). Mycophenolate mofetil hydrochloride is widely used in studies related to allograft arteriosclerosis (chronic rejection) .
|
-
- HY-B0199R
-
|
RS 61443 (Standard); TM-MMF (Standard)
|
Reference Standards
Interleukin Related
|
Cancer
|
|
Mycophenolate Mofetil (Standard) is the analytical standard of Mycophenolate Mofetil. This product is intended for research and analytical applications. Mycophenolate mofetil (RS 61443; TM-MMF) hydrochloride is an orally active antimetabolic immunosuppressant with antiproliferative and anti-inflammatory properties. Mycophenolate mofetil hydrochloride significantly inhibits the production of B, T lymphocytes and the proliferation of smooth muscle cells by selectively blocking the de novo purine synthesis pathway. Mycophenolate mofetil hydrochloride effectively reduces adventitial inflammation, medial necrosis and intimal thickening in rat aortic allografts, and decreases the number of lymphocytes expressing the IL-2 receptor, thereby delaying xenograft rejection. Mycophenolate mofetil hydrochloride shows certain toxicity in a hamster-to-rat limb xenotransplantation model when used in combination with FK506 (HY-13756). Mycophenolate mofetil hydrochloride is widely used in studies related to allograft arteriosclerosis (chronic rejection) .
|
-
- HY-B0199AS
-
|
RS 61443-d4 hydrochloride; TM-MMF-d4 hydrochloride
|
Isotope-Labeled Compounds
Interleukin Related
|
Cancer
|
|
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443; TM-MMF) hydrochloride is an orally active antimetabolic immunosuppressant with antiproliferative and anti-inflammatory properties. Mycophenolate mofetil hydrochloride significantly inhibits the production of B, T lymphocytes and the proliferation of smooth muscle cells by selectively blocking the de novo purine synthesis pathway. Mycophenolate mofetil hydrochloride effectively reduces adventitial inflammation, medial necrosis and intimal thickening in rat aortic allografts, and decreases the number of lymphocytes expressing the IL-2 receptor, thereby delaying xenograft rejection. Mycophenolate mofetil hydrochloride shows certain toxicity in a hamster-to-rat limb xenotransplantation model when used in combination with FK506 (HY-13756). Mycophenolate mofetil hydrochloride is widely used in studies related to allograft arteriosclerosis (chronic rejection) .
|
-
- HY-10932R
-
|
Ro 13-5057 (Standard)
|
Reference Standards
nAChR
iGluR
|
Neurological Disease
|
|
Aniracetam (Standard) is the analytical standard of Aniracetam. This product is intended for research and analytical applications. Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders .
|
-
- HY-107428
-
|
|
MMP
|
Cardiovascular Disease
|
|
PD-166793 is a potent, selective, orally active and wide-broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure .
|
-
- HY-109139
-
|
NIR178; PBF509
|
Adenosine Receptor
|
Neurological Disease
Cancer
|
|
Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A2A receptor (A2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with KB values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response .
|
-
- HY-10456R
-
|
|
Reference Standards
p38 MAPK
Casein Kinase
Wnt
|
Inflammation/Immunology
|
|
TAK-715 (Standard) is the analytical standard of TAK-715 (HY-10456). This product is intended for research and analytical applications. TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model .
|
-
- HY-109106B
-
|
(Rac)-SK-1403 free acid; (Rac)-AJT240 free acid; (Rac)-PLS240 free acid
|
CaSR
|
Endocrinology
|
|
(Rac)-Upacicalcet is the racemate of Upacicalcet (HY-109106). Upacicalcet is a non-peptide calcimimetic that acts as a CaSR agonist (EC50 = 10.8 nM). Upacicalcet reduces serum intact parathyroid hormone (iPTH) and serum Ca2+ levels, reducing hypocalcemia and gastrointestinal complications. Upacicalcet improves vascular calcification and bone disorders in the Adenine (HY-B0152)-induced secondary hyperparathyroidism (SHPT) rat model. Upacicalcet inhibits cortical pore formation and reduces bone fibrosis in rats with chronic kidney disease (CKD). Upacicalcet is useful for studying SHPT .
|
-
- HY-173221
-
|
|
NF-κB
p38 MAPK
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
MJ210 is a modulator of the NF-κB and MAPK pathways with oral activity and the ability to penetrate the blood-brain barrier, and it exhibits neuroprotective activity. In vitro, 5 μM of MJ210 can increase the survival rate of SH-SY5Y cells treated with Rotenone (HY-B1756) to 81.9% and reduce the level of ROS, etc. In vivo, 5 mg/kg of MJ210 can improve the motor impairment in a rat model of Parkinson's disease. MJ210 can be used in the research of neurological diseases, such as Parkinson's disease .
|
-
- HY-112348
-
|
|
Cyclic GMP-AMP Synthase
PKA
ERK
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
|
HA-1004 hydrochloride is a selective inhibitor of PKA, which can inhibit lipolysis and induce vascular relaxation. HA-1004 hydrochloride is also a dual inhibitor of cyclic GMP-dependent protein kinase and cyclic AMP-dependent protein (Cyclic GMP-AMP Synthase), and is involved in smooth muscle, second messenger, cyclic AMP and cyclic GMP regulation mechanisms. HA-1004 hydrochloride an antagonist for calcium, that can be used as a vasodilator to inhibit the contraction of rabbit aortic strips, or to antagonize ERK and tyrosine hydroxylase (TH) phosphorylation in morphine abstinence rat models .
|
-
- HY-100847
-
|
|
PARP
|
Cancer
|
|
AZ0108 is an inhibitor for poly ADP-ribose polymerase (PARP), which inhibits PARP1, PARP2, PARP3, PARP6, TNKS1, TNKS2, with IC50s of <0.03, <0.03, 2.8, 0.083, 3.2, >3 μM, respectively. AZ0108 prevents centrosome clustering with an EC50 of 0.053 μM, and exhibits cytotoxicity in cell OCI-LY-19 with GI50 of 0.017 μM. AZ0108 exhibits good in vivo pharmacokinetic characters in rat/mouse models .
|
-
- HY-N0194
-
|
|
Apoptosis
Parasite
|
Inflammation/Immunology
Cancer
|
|
Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
|
-
- HY-147927A
-
|
|
Enteropeptidase
|
Metabolic Disease
|
|
(S)-Human enteropeptidase-IN-1 (Compound 6c) is an orally active enteropeptidase inhibitor with low systemic exposure (IC50 (initial): 26 nM; IC50 (app): 1.8 nM). (S)-Human enteropeptidase-IN-1 promotes increased fecal protein output and effectively reduces body weight in a diet-induced obese (DIO) rat model. (S)-Human enteropeptidase-IN-1 inhibits enteropeptidase via a reversible covalent mechanism and prolongs the enzyme inactivation time. (S)-Human enteropeptidase-IN-1 can be used in anti-obesity research .
|
-
- HY-120380
-
|
|
MOFs
PARP
|
Neurological Disease
|
|
FeTMPyP is an orally active poly (ADP-ribose) polymerase (PARP) inhibitor. FeTMPyP inhibits cell death, nitrotyrosine formation, and depolarization of mitochondrial transmembrane potential. FeTMPyP reduces homocysteine-induced nitrosative stress and partially restores TFEB protein and mRNA levels. FeTMPyP improves functional and behavioral deficits caused by chronic constriction injury in rats. FeTMPyP alleviates acute cerebral infarction in a rat model of middle cerebral artery occlusion with mild hyperglycemia. FeTMPyP can be used in studies related to neuropathic pain, renal aging, ischemic penumbra, and hyperglycemic stroke .
|
-
- HY-107513
-
|
|
mGluR
|
Neurological Disease
Cancer
|
|
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
|
-
- HY-178342
-
|
|
Xanthine Oxidase
Reactive Oxygen Species (ROS)
SOD
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Xanthine oxidase-IN-18 is a potent orally activeXanthine oxidase (XO) inhibitor (IC50 = 0.263 μM). Xanthine oxidase-IN-18 exerts inhibition by directly and stably binding to the xanthine oxidase Mo-co active site. Xanthine oxidase-IN-18 exhibits reactive oxygen species (ROS) scavenging activity. Xanthine oxidase-IN-18 shows anti-hyperuricemia effects in a Potassium oxonate (HY-17511)-induced hyperuricemic rat model. Xanthine oxidase-IN-18 can be used for hyperuricemia, breast and lung cancer research .
|
-
- HY-P10587
-
|
JNJ-77242113; JNJ-2113; PN-235
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-165407
-
|
|
Elastase
CFTR
|
Inflammation/Immunology
|
|
Neltenexine, a mucolytic agent, is an Elastase inhibitor. Neltenexine diminishes anion secretion in in bronchial epithelial cells by inhibiting the Cl− and HCO3- uptake via Na/K/2Cl++− and Na+/HCO3- cotransporter without blockade of the CFTR channel, and also diminishes anion secretion via stimulation of Cl−/HCO3- exchanger. Neltenexine significantly prevents pulmonary emphysema with a reduction of alveolar deformation in rat models induced by Elastase. Neltenexine can be used for lung diseases such as chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-176214
-
|
|
PPAR
COX
|
Metabolic Disease
|
|
PPARγ agonist 19 (Compound 5e) is a PPARγ agonist. PPARγ agonist 19 has an IC50 of 11.27 μM against COX-1 and an IC50 of 0.05 μM against COX-1. PPARγ agonist 19 increases glucose uptake in rat hemidiaphragm assay and is superior to pioglitazone (HY-13956). PPARγ agonist 19 alleviates hyperglycemia and insulin resistance in an in vivo model of type 2 diabetes in rats and protects against renal and lipidemia damage caused by metabolic dysfunction .
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-
- HY-Y0546R
-
|
|
Reference Standards
Endogenous Metabolite
Photosensitizer
|
Cancer
|
|
Benzophenone (Standard) is the analytical standard of Benzophenone. This product is intended for research and analytical applications. Benzophenone standard is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone standard can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone standard can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone standard exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone standard exhibits estrogenic activity .
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-
- HY-P10587A
-
|
JNJ-77242113 acetate; JNJ-2113 acetate; PN-235 acetate
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) acetate is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra acetate inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra acetate exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra acetate can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-160822
-
|
PF-5212371
|
ADAMTS
MMP
|
Inflammation/Immunology
|
|
AGG-523 (PF-5212371) is an orally active, reversible, non-hydroxamate, zinc-binding selective inhibitor of ADAMTS4 and ADAMTS5 with IC50 of <0.03 and 0.04 μM. AGG-523 also inhibits MMP-2, -8, 12 activity AGG-523 attenuates release of aggrecanase-generated ARG-aggrecan fragments into synovial fluid, reduces surgery-induced ARG-aggrecan release in rat joint models, and inhibits aggrecanase activity to slow cartilage degradation. AGG-523 can be used for the research of osteoarthritis .
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-
- HY-19210
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
|
-
- HY-P5558
-
|
|
VEGFR
|
Neurological Disease
|
|
KLTWQELYQLKYKGI is a VEGF mimetic peptide designed based on the VEGF helix sequence 17-25, with the ability to activate VEGF receptors and exert pro-angiogenic biological activity. KLTWQELYQLKYKGI effectively promotes the attachment, spreading and proliferation of human umbilical vein endothelial cells. KLTWQELYQLKYKGI enhances the proliferation, migration and osteogenic differentiation of bone marrow stromal cells (BMSCs). KLTWQELYQLKYKGI synergistically accelerates angiogenesis and bone regeneration in rat cranial defect models. KLTWQELYQLKYKGI can be used for the research of brain tissue engineering and traumatic brain injury repair and biomaterials for bone tissue engineering and bone repair .
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-
- HY-111140
-
|
|
PGE synthase
Lipoxygenase
PPAR
|
Inflammation/Immunology
|
|
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50 = 3.4 μM) and 5-lipoxygenase (5-LOX; IC50 = 6.5 μM). YS121 exhibits direct, reversible, and specific binding to mPGES-1 (KD = 10-14 μM) . YS121 dose-dependently reduces PGE2 production with an EC50 of 12 μM in IL-1β-stimulated A549 cells . YS121 (compound 9) activates PPAR-α and -γ (EC50 = 1 and 3.6 μM, respectively) . YS121 exhibits anti-inflammatory efficiency in human whole blood as well as in vivo. YS121 can be used for pleurisy research .
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-
- HY-B0340
-
|
DM9384; DZL-221
|
nAChR
iGluR
mGluR
PKC
GABA Receptor
Calcium Channel
|
Neurological Disease
|
|
Nefiracetam is a cognition-enhancing agent. Nefiracetam is an activator of nAChR, N-methyl-D-aspartate receptor (NMDAR), mGluR5, PKC, gamma-aminobutyric acid (GABA), and N/L-type Ca 2+ channels. Nefiracetam promotes neuroplasticity and enhances neuroprotection. Nefiracetam can be used in Alzheimer's disease, epilepsy, and cerebral ischemia research .
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-
- HY-N4107
-
|
|
TGF-beta/Smad
|
Infection
Inflammation/Immunology
Cancer
|
|
Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
|
-
- HY-N4107R
-
|
|
Reference Standards
TGF-beta/Smad
|
Infection
Inflammation/Immunology
Cancer
|
|
Phyllanthin (Standard) is the analytical standard of Phyllanthin. This product is intended for research and analytical applications. Phyllanthin is an effective oral anticancer agent. Phyllanthin inhibits MOLT-4 cell viability, increases apoptosis, inhibits cell migration and invasion. Phyllanthin exerts anti-fibrotic effects by down-regulating TGF signaling pathway via ALK5 and Smad2/3. Phyllanthin also has anti-inflammatory and antibacterial properties .
|
-
- HY-172236
-
|
BNC210; IW-2143
|
nAChR
|
Neurological Disease
|
|
Soclenicant (BNC210) is an orally active α7 nAChR negative alteration modulator (NAM) with no apparent side effects. Soclenicant exhibits acute anxiolytic activity in rodent models of anxiety. Soclenicant inhibits rat and human α7 nAChR currents (in stably transfected cell lines) induced by acetylcholine, nicotine, choline, and the a7-specific agonist PNU-282987 (HY-12560A) with IC50 values in the range of 1.2 to 3 μM. Soclenicant can be used in studies of anxiety, trauma, and stressor-related disorders .
|
-
- HY-173488
-
|
|
NF-κB
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
|
Cancer
|
|
NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and HIF-1α, while simultaneously inducing the activation of Nrf2 .
|
-
- HY-178464
-
|
|
RIP kinase
Mixed Lineage Kinase
Necroptosis
|
Neurological Disease
Inflammation/Immunology
|
|
RIPK1-IN-34 is a selective, brain-penetrant RIPK1 inhibitor (IC50 = 126.70 nM) with almost no inhibitory effect on RIPK3 (IC50 ＞ 10, 000 nM). RIPK1-IN-34 offers substantial neuroprotection by inhibiting the phosphorylation of RIPK1, RIPK3, and mixed lineage kinase domain-like pseudokinase (MLKL) within the necroptosis pathway. RIPK1-IN-34 shows the neuroprotective effect in a rat middle cerebral artery occlusion (MCAO) model. RIPK1-IN-34 can be used for the study of anti-acute ischemic stroke (AIS) .
|
-
- HY-15495B
-
|
(3S)-CC-930 hydrochloride
|
JNK
ERK
p38 MAPK
EGFR
TNF Receptor
|
Inflammation/Immunology
|
|
(3S)-Tanzisertib (hydrochloride) ((3S)-CC-930 (hydrochloride)) is an orally active JNK inhibitor (IC50 values for JNK1, JNK2, and JNK3 are 61, 7, and 6 nM, respectively). (3S)-Tanzisertib (hydrochloride) selectively inhibits ERK1, p38α, and EGFR (IC50 = 0.48, 3.4, and 0.38 μM, respectively). (3S)-Tanzisertib (hydrochloride) inhibits LPS-induced TNFα production in an acute rat PK-PD model. (3S)-Tanzisertib (hydrochloride) can be used in idiopathic pulmonary fibrosis (IPF) research .
|
-
- HY-W653962
-
|
|
Isotope-Labeled Compounds
Apoptosis
Antibiotic
Fungal
Bacterial
|
Infection
Cancer
|
|
Triclosan- 13C6 is 13C labeled Triclosan. Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 μM and 10 μM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
- HY-158223
-
|
CMCSMA
|
Biochemical Assay Reagents
|
Others
|
Carboxymethyl chitosan Methacryloyl (CMCSMA) is methacrylated carboxymethyl chitosan with properties as a 3D printing ink. A composite hydrogel made of Carboxymethyl chitosan Methacryloyl can effectively accelerate bone healing in an infectious microenvironment after implantation in a rat model of Staphylococcus aureus-infected femoral defect . Carboxymethyl chitosan Methacryloyl needs to self-assemble into fibrous hydrogel under the action of photoinitiator LAP (HY-44076), and target bioactive adhesion sites, play an inherent supporting role for tissue cells and biodegradable activity.
Application: cell culture, biological 3D printing, tissue engineering, etc.
|
-
- HY-19337
-
|
BAY 1896953; ORM-15341
|
Androgen Receptor
|
Cancer
|
|
Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
|
-
- HY-117710B
-
|
|
Cholinesterase (ChE)
Amyloid-β
ERK
TNF Receptor
Interleukin Related
|
Neurological Disease
|
|
AD-35 is an orally active anti-Alzheimer's disease (AD) agent with moderate AChE inhibitory activity and metal ion chelating ability. AD-35 exhibits IC50 values for AChE and BuChE of 793 nM and 31428 nM, respectively. AD-35 can form chelates with Cu²⁺ and Fe³⁺, but its chelating ability for Zn²⁺ is relatively weak. AD-35 can inhibit Aβ aggregation and disassemble the formed Aβ aggregates, and inhibit Aβ-induced ERK phosphorylation. AD-35 inhibits neuroinflammation in AD rat models and demonstrates a strong effect in improving cognitive function .
|
-
- HY-B1119R
-
|
|
Reference Standards
Bacterial
Fungal
Antibiotic
Apoptosis
|
Infection
Cancer
|
|
Triclosan (Standard) is the analytical standard of Triclosan. This product is intended for research and analytical applications. Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 µM and 10 µM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
- HY-155517
-
|
|
NOD-like Receptor (NLR)
Pyroptosis
|
Inflammation/Immunology
|
|
INF200 (compound 5) is a sulfonylurea-based inhibitor of NLRP3 and NLRP3-mediated pyroptosis. INF200 has beneficial cardiometabolic effects in rat model of high-fat diet (HFD)-induced metaflammation，and shows anti-inflammatory activity to (10 μM) decreases IL-1β release in human macrophages. INF200 improves glucose and lipid profiles，and attenuates systemic inflammation and biomarkers of cardiac dysfunction (particularly BNP). INF200 also improves myocardial damage-dependent ischemia/reperfusion injury (IRI) in hemodynamic evaluation .
|
-
- HY-175637
-
|
|
COX
MyD88
|
Neurological Disease
Inflammation/Immunology
|
|
COX-2-IN-57 is an orally active COX-2 inhibitor with an IC50 value of 0.02 μM. COX-2-IN-57 reduces MyD88 expression and decreases serum levels of COX-2, PGE2, and COX-1 in Cisplatin (HY-17394)/radiation-induced neuropathy rat model. COX-2-IN-57 demonstrates superior antinociceptive efficacy in hot plate, cold allodynia, and Randall-Selitto tests, along with hepato-/renal protection. COX-2-IN-57 can be used for the study of inflammation .
|
-
- HY-P10870
-
|
|
Peptide-Drug Conjugates (PDCs)
FGFR
Apoptosis
|
Cancer
|
|
Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models .
|
-
- HY-173024
-
|
|
TRP Channel
|
Neurological Disease
|
|
TRPC4/5-IN-3 (Compound 32) is the orally active inhibitor for transient receptor potential canonical channel 4/5 (TRPC4/5) with IC50 of 3.6 nM and 5.5 nM. TRPC4/5-IN-3 inhibits hERG channel with IC50 of 6.5 µM. TRPC4/5-IN-3 exhibits good metabolic stability in human/rat/mouse liver microsomes. TRPC4/5-IN-3 exhibits antidepressant and anxiolytic activity in mouse models, exhibits good pharmacokinetic characteristics in mouse with an oral bioavailability of 87% .
|
-
- HY-181513
-
|
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
DPP-1-IN-2 is a DPP-I inhibitor with a human IC50 of 36.8 nM and oral efficacy. DPP-1-IN-2 binds to intracellular DPP-I, increases its thermal stability, and reduces the activity and expression levels of downstream neutrophil serine proteases by inhibiting its enzymatic activity. DPP-1-IN-2 regulates the secretion of inflammatory factors and chemokines to exert anti-inflammatory effects. DPP-1-IN-2 reverses joint inflammation and tissue damage in adjuvant-induced arthritis rat models. DPP-1-IN-2 is applicable to research related to arthritis .
|
-
- HY-181235
-
|
|
COX
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
|
COX-2/Aromatase-IN-1 is a potent dual inhibitor of COX-2 and aromatase. COX-2/Aromatase-IN-1 can simultaneously inhibit COX-2 and aromatase, significantly suppress inflammation and induce proliferation inhibition of breast cancer cells. COX-2/Aromatase-IN-1 exerts anti-breast cancer and anti-inflammatory effects in the MCF-7 breast cancer cell and carrageenan-induced rat paw edema model. COX-2/Aromatase-IN-1 can be used for the study of inflammation and breast cancer .
|
-
- HY-168366
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
R-6890 is a Brorphine-related opioid receptor antagonist that exhibits differential binding activities toward rat opioid receptors (IC50=4.6 nM (0.05 M Tris; pH 7.4) and 170 nM (0.05 M Tris+0.1 M NaCl)). R-6890 displaces bound labeled opioids from receptors, and its binding affinity is affected by environmental factors, decreasing in the presence of NaCl. R-6890 crosses the blood-brain barrier (BBB) and exerts analgesic effects in the warm water-induced tail-flick reflex model of male Wistar rats .
|
-
- HY-W747491
-
|
|
Isotope-Labeled Compounds
Antibiotic
Apoptosis
Bacterial
Fungal
|
Infection
Cancer
|
|
Triclosan- 13C12 is 13C labeled Triclosan (HY-B1119). Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 μM and 10 μM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
|
-
- HY-B1076
-
|
HMS; 6α-Methyl-11β-hydroxyprogesterone
|
VEGFR
CCR
STAT
|
Neurological Disease
|
|
Medrysone (HMS; 6α-Methyl-11β-hydroxyprogesterone) is a STAT6 modulator and M2 macrophage polarization inducer. Medrysone enhances IL-4-triggered STAT6 activation, upregulates the expression of M2 markers, and promotes the secretion of VEGF and CCL2. Medrysone also enhances the pro-migratory activity of M2-like macrophages toward endothelial cells. By regulating macrophage polarization and related repair pathways, Medrysone significantly promotes corneal wound repair in a rat mechanical injury model. Medrysone can be used for research related to corneal injury .
|
-
- HY-181236
-
|
|
COX
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
|
COX-2/Aromatase-IN-2 is a potent dual inhibitor of COX-2 and aromatase. COX-2/Aromatase-IN-2 can simultaneously inhibit COX-2 and aromatase, suppress inflammation and induce proliferation inhibition of breast cancer cells. COX-2/Aromatase-IN-2 exerts anti-breast cancer and anti-inflammatory effects in the MCF-7 breast cancer cell and carrageenan-induced rat paw edema model. COX-2/Aromatase-IN-2 can be used for the study of inflammation and breast cancer .
|
-
- HY-N0194R
-
|
|
Reference Standards
Apoptosis
Parasite
|
Inflammation/Immunology
Cancer
|
|
Asiatic acid (Standard) is the analytical standard of Asiatic acid. This product is intended for research and analytical applications. Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
|
-
- HY-175888
-
|
Mc-exo-EVC-Exatecan
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
APL-1082 is a drug-Linker conjugate that can be used for ADC synthesis. APL-1082 contains Exatecan (HY-13631) and Linker (HY-175929). APL-1082 reduces aggregation and hydrophobicity in Trastuzumab (HY-P9907) ADCs, enables production of high-DAR (10) ADCs with homogeneity and defined physicochemical properties. APL-1082 forms a Trastuzumab ADC with enhanced stability, showing greater DAR retention over time. APL-1082 can be used for the research of gastric cancer .
|
-
- HY-116142
-
|
|
iGluR
|
Neurological Disease
|
|
CP-283097 is an orally active and conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors .
|
-
- HY-183644
-
|
|
Lysyl Oxidase
|
Cardiovascular Disease
|
|
LNO 9 is an orally active LOXL2 inhibitor and NO donor, with an IC50 of 0.17 μM against human LOXL2. LNO 9 competitively binds to the LTQ cofactor of LOXL2 to form an irreversible complex, thereby inhibiting collagen oxidation and abnormal cross-linking. LNO 9 releases nitric oxide (NO) to increase cGMP levels in pulmonary artery smooth muscle cells. LNO 9 inhibits hypoxia-induced collagen modification and possesses vasodilatory activity. LNO 9 ameliorates right ventricular hypertrophy and pulmonary artery medial thickness in rat models induced by hypoxia and Monocrotaline (HY-N0750), and can be used for research on pulmonary hypertension .
|
-
- HY-P10405
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
TAT-D1 peptide is a dopamine D1-D2 receptor heterodimer inhibitor. TAT-D1 peptide disrupts the function of dopamine D1-D2 receptor heteromers, enhances subchronic amphetamine-induced locomotor activity, and exacerbates the expression of amphetamine-induced locomotor sensitization. TAT-D1 peptide produces rapid anxiolytic and antidepressant-like effects in rat models of depression and anxiety, and inhibits c-fos expression in the nucleus accumbens of rats. TAT-D1 peptide can be used in the research of psychostimulant addiction, depression and anxiety disorders .
|
-
- HY-120314
-
|
|
Apoptosis
Caspase
Endogenous Metabolite
|
Inflammation/Immunology
|
GEA 3162 is an orally active compound that acts as a NO/ONOO⁻ donor. GEA 3162 significantly inhibits the activation of human polymorphonuclear leukocytes (PMNs) through the cGMP pathway, inhibits the release of inflammatory mediators, and exerts anti-inflammatory and protective effects. GEA 3162 induces apoptosis of neutrophils and bone marrow cells by activating caspase-2/3/8/9 through the ONOO⁻ pathway. GEA 3162 has a bidirectional effect in the rat gastric ulcer model: at low doses, it significantly reduces gastric mucosal damage, while at high doses, it aggravates the ulcer area. GEA 3162 can be used for research on inflammatory conditions such as gastric ulcers .
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- HY-B0742
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17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate
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Progesterone Receptor
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Endocrinology
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Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
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- HY-P10405A
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Dopamine Receptor
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Neurological Disease
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TAT-D1 peptide acetate is a dopamine D1-D2 receptor heterodimer inhibitor. TAT-D1 peptide acetate disrupts the function of dopamine D1-D2 receptor heteromers, enhances subchronic amphetamine-induced locomotor activity, and exacerbates the expression of amphetamine-induced locomotor sensitization. TAT-D1 peptide acetate produces rapid anxiolytic and antidepressant-like effects in rat models of depression and anxiety, and inhibits c-fos expression in the nucleus accumbens of rats. TAT-D1 peptide acetate can be used in the research of psychostimulant addiction, depression and anxiety disorders .
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- HY-180806
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RIP kinase
Apoptosis
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Cardiovascular Disease
Neurological Disease
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RIPK1-IN-39 (compound 2) is a potent and selective RIPK1 inhibitor (IC50 = 69.40 nM) exhibiting >100-fold selectivity over RIPK3 (IC50 = 6946 nM). RIPK1-IN-39 protects HT-22 and HT-29 cells from necroptosis by inhibiting the phosphorylation and activation of the RIPK1-RIPK3-MLKL pathway. RIPK1-IN-39 demonstrates neuroprotective effects in a rat model of middle cerebral artery occlusion (MCAO). RIPK1-IN-39 can be used for acute ischemic stroke (AIS) research .
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- HY-162677
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Adrenergic Receptor
5-HT Receptor
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Cardiovascular Disease
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MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research .
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- HY-P990259
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Transmembrane Glycoprotein
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Inflammation/Immunology
Cancer
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Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
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- HY-120314A
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Apoptosis
Caspase
Endogenous Metabolite
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Inflammation/Immunology
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GEA 3162 hydrochloride is an orally active compound that acts as a NO/ONOO⁻ donor. GEA 3162 hydrochloride significantly inhibits the activation of human polymorphonuclear leukocytes (PMNs) through the cGMP pathway, inhibits the release of inflammatory mediators, and exerts anti-inflammatory and protective effects. GEA 3162 hydrochloride induces apoptosis of neutrophils and bone marrow cells by activating caspase-2/3/8/9 through the ONOO⁻ pathway. GEA 3162 hydrochloride has a bidirectional effect in the rat gastric ulcer model: at low doses, it significantly reduces gastric mucosal damage, while at high doses, it aggravates the ulcer area. GEA 3162 hydrochloride can be used for research on inflammatory conditions such as gastric ulcers .
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- HY-135439
-
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5-HT Receptor
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Neurological Disease
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SB-203186 is a highly selective 5-HT4 receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pKB value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction .
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- HY-182456
-
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KMO
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Neurological Disease
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CHDI-340246 is an orally active kynurenine monooxygenase (KMO) inhibitor. CHDI-340246 blocks KMO activity, alters the metabolic flux of the kynurenine pathway, inhibits the production of 3-hydroxykynurenine and quinolinic acid, elevates the levels of kynurenine and kynurenic acid, and restores electrophysiological abnormalities in transgenic mouse models of Huntington's disease. CHDI-340246 can be used in studies related to Huntington's disease .
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- HY-17655
-
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Reactive Oxygen Species (ROS)
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Inflammation/Immunology
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TBE56, a molecular glue, is a BACH1 degrader, with an EC50 of 44 nM. TBE56 is a weak NRF2 inducer and the biotinylated TBE31. TBE56 interacts and promotes the
degradation of BACH1 via a mechanism involving the E3 ligase FBX022. TBE56 reduces intracellular Fe 2+ accumulation, ROS generation, and malondialdehyde (MDA) content, while increasing GSH/GSSG ratio and upregulating GPX4 in Prominin-2-overexpressed BMSCs. TBE56 significantly ameliorates intervertebral disc degeneration (IVDD) in puncture-induced SD rat IVDD model. TBE56 can be used for the study of intervertebral disc degeneration (IVDD) .
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- HY-107428R
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Reference Standards
MMP
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Cardiovascular Disease
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PD-166793 (Standard) is the analytical standard of PD-166793 (HY-107428). This product is intended for research and analytical applications. PD-166793 is a potent, selective, orally active and wide-broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure .
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- HY-180348
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p38 MAPK
ATP Synthase
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Inflammation/Immunology
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KFP-H008 is an orally active potassium-competitive acid blocker. KFP-H008 inhibits gastric acid secretion through blocking H +-K +-ATPase. KFP-H008 reduces ethanol-induced gastric ulcer index and malonaldehyde as well as proinflammatory cytokine expression in vivo. KFP-H008 downregulates p-p38 MAPK and p65 NF-κB expression. KFP-H008 blocks histamine-stimulated acid secretion in rat and dog models. KFP-H008 can be studied in research on acid-related disease, such as ethanol-induced gastric ulcer and gastric epithelial cell damage .
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- HY-116673
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Histone Acetyltransferase
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Neurological Disease
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TTK21 is an activator of the histone acetyltransferases CBP/p300. TTK21 passes the blood–brain barrier, induces no toxicity, and reaches different parts of the brain when conjugated to glucose-based carbon nanosphere (CSP). TTK21 has beneficial implications for the brain functions of neurogenesis and long-term memory .CSP-TTK21 can ameliorate Aβ-impaired long-term potentiation (LTP). CSP-TTK21 may enhance the transcription of genes that promote synaptic health and cognitive function . CSP-TTK21 is orally effective and leads to improvements in motor functions, histone acetylation dynamics in a spinal injury rat model .
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- HY-134160
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5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione; 5-Fluorodihydrouracil
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Nucleoside Antimetabolite/Analog
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Cancer
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5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
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- HY-185463
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Ser/Thr Protease
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Inflammation/Immunology
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β-Tryptase-IN-1 is a selective β-tryptase inhibitor with a Ki of 10 nM. β-Tryptase-IN-1 binds to the inducible S4 + pocket unique to β-tryptase. β-Tryptase-IN-1 can be used for the researches of asthma and chronic obstructive pulmonary disease (COPD) .
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- HY-W142795
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4-sec-BP
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Androgen Receptor
Estrogen Receptor/ERR
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Metabolic Disease
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4-sec-Butylphenol (4-sec-BP) is an androgen receptor ligand that binds to the androgen receptor with a pIC50 of 4.07 . 4-sec-Butylphenol is an estrogen receptor agonist. 4-sec-Butylphenol can be found in industrial effluents, in production water of oil and gas platforms, as well as in river water samples .
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- HY-B1451
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TA-6366
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Angiotensin-converting Enzyme (ACE)
MMP
JNK
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Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Imidapril hydrochloride (TA-6366) is an orally active dual inhibitor of angiotensin-converting enzyme (ACE) and MMP-9. Imidapril hydrochloride inhibits lipopolysaccharide-induced phosphorylation of c-Jun, MKK4 and JNK in monocytes, and downregulates the production of specific inflammatory factors such as TNF-α and IP-10, thereby exerting anti-inflammatory activity. Imidapril hydrochloride also effectively ameliorates mesangial expansion and reduces urinary albumin excretion by inhibiting angiotensin AngII production, lowering glomerular pressure and oxidative stress, thus delaying disease progression. Imidapril hydrochloride can also directly bind to the active site of MMP-9 to inhibit gelatinase activity, and suppress the enlargement of cerebral aneurysms without altering systemic blood pressure. Imidapril hydrochloride is widely applicable to related studies on autoimmune glomerulonephritis, diabetic nephropathy, cerebral aneurysms and other conditions .
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- HY-183375
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Neurological Disease
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AChE/BuChE/BACE-1-IN-1 is a blood-brain barrier-permeable multi-target inhibitor of AChE/BuChE/BACE, with IC50 values of 0.387 μM, 0.430 μM, and 0.531 μM against AChE, BuChE, and BACE-1, respectively. AChE/BuChE/BACE-1-IN-1 reduces the aggregation of β-amyloid protein (Aβ) and hyperphosphorylated tau protein (p-tau). AChE/BuChE/BACE-1-IN-1 can be used for the research of Alzheimer's disease .
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- HY-N0729D
-
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Glutathione Peroxidase
SOD
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Cardiovascular Disease
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Linoleic acid is a critical component of polyunsaturated fatty acids. Linoleic acid reduces GSH-PX and T-SOD activities. Linoleic acid functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid can cause acute oxidative damage to red blood cells, ultimately leading to partial acute anemia. Linoleic acid can be used in the research of skin diseases associated with linoleic acid deficiency .
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- HY-148795
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Apical Sodium-Dependent Bile Acid Transporter
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Metabolic Disease
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Ritivixibat is an apical sodium-dependent bile acid transporter (ASBT/IBAT) inhibitor. Ritivixibat blocks ASBT/IBAT function, thereby reducing bile acid reabsorption, regulating bile acid homeostasis and alleviating liver injury. Ritivixibat protects cholangiocytes from damage caused by cytotoxic bile acids. Ritivixibat is applicable to research related to primary sclerosing cholangitis .
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- HY-111103A
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PAK
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Cancer
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CZh226 hydrochloride is a potent and selective PAK4 inhibitor with an IC50 of 18 nM, and its selectivity for PAK1 is 346 times. The oral bioavailability of CZh226 hydrochloride is poor, and it requires the use of the prodrug PAK4-IN-1 (HY-130628) to improve absorption and metabolic stability. CZh226 hydrochloride can be used for research on colorectal cancer and melanoma .
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- HY-P11399
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Bacterial
Fungal
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Infection
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Tachyplesin-3 is a broad-spectrum cationic antimicrobial peptide. Tachyplesin-3 has inhibitory activity against Gram-positive bacteria, Gram-negative bacteria, fungi and enveloped viruses. Tachyplesin-3 binds to bacterial membrane lipopolysaccharides through positive charges, disrupting membrane integrity and causing leakage of cellular contents. Tachyplesin-3 interferes with bacterial adhesion and aggregation, prevents biofilm formation, and has a synergistic effect when used in combination with Piperacillin (HY-B1923) - Tazobactam (HY-B1418) (TZP) .
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- HY-182713
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Tyrosinase
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Others
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Tyrphostin AG-808 is a protein tyrosine kinase inhibitor that does not reduce neointimal formation. Perivascular implantation of Tyrphostin AG-808 causes medial damage in rats .
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- HY-N14827
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SM-216289
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Drug Derivative
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Neurological Disease
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Xanthofulvin (SM-216289) is an inhibitor of semaphorin 3A. Xanthofulvin blocks its binding to receptors, inhibits growth cone collapse, and accelerates olfactory nerve regeneration in rats in vivo. Xanthofulvin can be used in studies related to traumatic neuronal injury .
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- HY-B1076R
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HMS (Standard); 6α-Methyl-11β-hydroxyprogesterone (Standard)
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Reference Standards
STAT
VEGFR
CCR
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Inflammation/Immunology
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Medrysone (Standard) is the analytical standard of Medrysone. This product is intended for research and analytical applications. Medrysone (HMS; 6α-Methyl-11β-hydroxyprogesterone) is a STAT6 modulator and M2 macrophage polarization inducer. Medrysone enhances IL-4-triggered STAT6 activation, upregulates the expression of M2 markers, and promotes the secretion of VEGF and CCL2. Medrysone also enhances the pro-migratory activity of M2-like macrophages toward endothelial cells. By regulating macrophage polarization and related repair pathways, Medrysone significantly promotes corneal wound repair in a rat mechanical injury model. Medrysone can be used for research related to corneal injury .
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- HY-B1341
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Enidrel; SC-4642; NSC 15432
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Endogenous Metabolite
Progesterone Receptor
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Cancer
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Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
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- HY-P990792
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Transmembrane Glycoprotein
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Inflammation/Immunology
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Anti-Mouse CD4 Antibody (GK1.5) is an anti-mouse CD4 IgG2b monoclonal antibody. Anti-Mouse CD4 Antibody (GK1.5) can significantly deplete CD4 + T cells. Anti-Mouse CD4 Antibody (GK1.5) can extend the survival rate of xenograft models. Anti-Mouse CD4 Antibody (GK1.5) can be used for research on immunology. The recommend isotype control of Anti-Mouse CD4 Antibody (GK1.5): Rat IgG2b kappa, Isotype Control (HY-P990682) .
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- HY-182068
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iGluR
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Cardiovascular Disease
Neurological Disease
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NFI23 is a GluN2B-NMDAR inhibitor with an IC50 of 1.31 μM and a Ki of 5.98 nM against GluN2B-NMDAR. NFI23 can cross the blood-brain barrier. NFI23 binds to the ifenprodil binding site of GluN2B-NMDAR, reduces NMDA-induced Ca 2+ influx and reactive oxygen species (ROS) production, maintains mitochondrial membrane potential, inhibits neuronal apoptosis, and restores the expression of p-ERK1/2. NFI23 exerts neuroprotective effects against NMDA-induced cytotoxicity and in the rat middle cerebral artery occlusion (MCAO) model. NFI23 can be used for the research of ischemic stroke .
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- HY-19337S1
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BAY 1896953-d6; ORM-15341-d6
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Isotope-Labeled Compounds
Androgen Receptor
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Cancer
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Ketodarolutamide-d6 (BAY 1896953-d6) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
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- HY-180824
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p38 MAPK
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Neurological Disease
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P38-α MAPK-IN-11 (Compound 4C) is a selective inhibitor of P38α MAPK that can cross the blood-brain barrier with an IC50 value of 43 nM. P38-α MAPK-IN-11 has extremely low inhibitory activity against other MAPK subtypes, namely p38β, p38γ, and p38δ, with IC50 values of > 100 nM, > 100 nM, and 48.6 mM respectively. P38-α MAPK-IN-11 exhibits outstanding neuroprotective effects and anti-neuroinflammatory effects in Alzheimer's disease-like rat models. P38-α MAPK-IN-11 can be used for the study of Alzheimer's disease .
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- HY-175824
-
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iGluR
NO Synthase
Apoptosis
Reactive Oxygen Species (ROS)
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Neurological Disease
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PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke .
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- HY-168906
-
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Bradykinin Receptor
PI3K
Akt
TNF Receptor
ERK
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Neurological Disease
Inflammation/Immunology
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BI-113823 is an orally active, blood-brain barrier-permeable bradykinin B1 receptor antagonist, with a Ki value of 5.3 nM for human receptors and 13.3 nM for rat receptors. BI-113823 reduces inflammation-induced mechanical hyperalgesia, as well as the mechanical sensitivity of peripheral afferent nerves and spinal nociceptive-specific neurons. BI-113823 alleviates liver fibrosis and portal hypertension, and improves survival in chronic liver disease models. BI-113823 inhibits the activities of monocytes, neutrophils and hepatic stellate cells, as well as the PI3K/Akt signaling pathway. BI-113823 can be used in research related to inflammatory pain, liver fibrosis and portal hypertension .
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- HY-W047432
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|
DL0805
|
ROCK
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Cardiovascular Disease
|
|
5-Nitro-1H-indazole-3-carbonitrile (DL0805) is a Rho kinase(ROCK) inhibitor with an IC50 of 6.67 μM for ROCK-I. 5-Nitro-1H-indazole-3-carbonitrile reduces Norepinephrine (HY-13715)-induced transient contraction and inhibits contraction induced by increasing external calcium in the endothelium-denuded rings of rat models. 5-Nitro-1H-indazole-3-carbonitrile has a vasorelaxant activity but high toxicity. 5-Nitro-1H-indazole-3-carbonitrile can be used for cardiovascular diseases, especially hypertension research .
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- HY-167262
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RAR/RXR
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Metabolic Disease
Cancer
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AGN-191659 is an orally active RAR/RXR agonist with EC50 values of 11 nM, 23 nM, and 37 nM for RXRα, RARβ, and RARγ, respectively. AGN-191659 activates RXRα, RARβ and RARγ to induce gene transcription. AGN-191659 induces tissue transglutaminase activity, inhibits ornithine decarboxylase activity induced by tumor promoters, and suppresses chondrogenesis. AGN-191659 reverses basic fibroblast growth factor-induced endothelial cell proliferation. AGN-191659 induces hypertriglyceridemia in rat models. AGN-191659 inhibits total heparin-releasable lipase activity. AGN-191659 can be used in research related to promyelocytic leukemia and hypertriglyceridemia .
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- HY-135446
-
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Endothelin Receptor
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Cardiovascular Disease
Endocrinology
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BQ-610 is a selective antagonist of the endothelin A receptor (ETA receptor). BQ-610 specifically blocks the ETA receptor, competitively inhibiting the binding of endothelin-1 (ET-1) (a vasoconstrictive peptide) to the receptor, thereby blocking the effects of ET-1 such as vascular smooth muscle contraction, cell mitosis, and inhibition of hormone secretion. BQ-610 significantly alleviates cerebral vasospasm in rabbits. BQ-610 blocks the bronchial epithelial and pulmonary vascular cell proliferation caused by cigarette smoke in rat models. BQ-610 can delay the natural luteal regression in the cow's uterus. BQ-610 can be used for research on vasospasm, abnormal cell proliferation, and reproductive endocrine disorders .
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- HY-116763
-
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COX
LOX-1
|
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COX-2/5-LOX-IN-4 (Compound 1) is a dual inhibitor that acts on both COX-2 and 5-LOX, with IC50 values of 0.05 μM for COX-2 and 0.003 μM for 5-LOX. By inhibiting the arachidonic acid metabolism pathway, COX-2/5-LOX-IN-4 reduces the production of prostaglandins and leukotrienes, alleviating inflammatory responses. In a rat ear edema model, intravenous administration (0.01 and 0.1 mg/kg) reduced edema by 41% and 44%, respectively, demonstrating significant anti-inflammatory effects. COX-2/5-LOX-IN-4 shows promise for studying the mechanisms of inflammatory diseases .
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- HY-136903
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Calcium Channel
Proteasome
Reactive Oxygen Species (ROS)
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
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SNJ-1945 is an orally active Calpain inhibitor that can cross the blood-brain barrier. SNJ-1945 protects rat hearts against cardiac arrest-reperfusion injury by inhibiting the hydrolysis of α-fodrin. SNJ-1945 inhibits VEGF-induced angiogenesis in retinal endothelial cells. SNJ-1945 also protects SH-SY5Y cells from damage induced by MPP+ (HY-W008719) and Rotenone (HY-B1756). SNJ-1945 exhibits anti-inflammatory and neuroprotective activities in a mouse model of multiple sclerosis. SNJ-1945 can be used for the research of cardiovascular, nervous system and inflammatory diseases .
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- HY-19337S
-
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BAY 1896953-d3; ORM-15341-d3
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Isotope-Labeled Compounds
Androgen Receptor
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Cancer
|
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Ketodarolutamide-d3 (BAY 1896953-d3) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
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- HY-149454
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P2Y Receptor
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Cancer
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P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 with antiplatelet activity. P2Y1/P2Y12 antagonist-1 inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. P2Y1/P2Y12 antagonist-1 exhibits potent inhibitory effects in rat thrombosis model.
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- HY-181822
-
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Formyl Peptide Receptor (FPR)
Arrestin
PKA
Interleukin Related
|
Cardiovascular Disease
|
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BMS-986331 is an orally active selective N-Formyl Peptide Receptor 2 (FPR2) agonist with an EC50 of 0.5 nM in humans and 1 nM in rats. BMS-986331 activates Gαi2, GαoA, Gα12, Gα13 signaling pathways, recruits β-arrestin1 and β-arrestin2, and inhibits downstream cAMP. BMS-986331 induces the expression and release of the pro-resolution cytokine IL-10. BMS-986331 improves cardiac structure and function in a rat model of heart failure induced by permanent coronary artery occlusion. BMS-986331 can be used for the research of heart failure .
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- HY-167851
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|
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CXCR
|
Neurological Disease
Cancer
|
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CCX662 is a selective CXCR7 inhibitor with human IC50 values of 9 nM (buffer) and 18 nM (100% human serum), and rat IC50 of 14 nM (100% rat serum). CCX662 blocks CXCL12 binding to CXCR7, inhibits CXCR4-directed trans-endothelial migration of CXCR4 +/CXCR7 + cells. CCX662 can be used for the research of glioblastoma multiforme .
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- HY-180406
-
|
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Neuropeptide Y Receptor
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Neurological Disease
|
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NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal .
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- HY-151093
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-
- HY-W004761
-
|
Hypodiboric acid
|
Biochemical Assay Reagents
Reactive Oxygen Species (ROS)
|
Infection
|
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Tetrahydroxydiboron acts as a hydrogel initiator and bioadhesion promoter, with broad-spectrum antibacterial activity, ROS scavenging capacity and osteogenic induction properties. Tetrahydroxydiboron initiates rapid gelation by generating free radicals through reactions with vinyl monomers and dissolved oxygen, and overcomes oxygen inhibition without deoxygenation or external triggers. Tetrahydroxydiboron achieves strong bioadhesion through interaction with carboxymethyl chitosan. Tetrahydroxydiboron can be used in the research of periodontitis and related inflammatory diseases .
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- HY-P991937
-
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Lipase
|
Inflammation/Immunology
|
|
SOL-116 is a humanized anti-BSSL antibody. SOL-116 blocks BSSL from binding to monocytes. SOL-116 reduces the severity of Pristane (HY-N7819)-induced arthritis in rats .
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-
- HY-W002879
-
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Reactive Oxygen Species (ROS)
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Inflammation/Immunology
|
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4-Hydroxyphenylboronic acid pinacol ester is a ROS-responsive component. 4-Hydroxyphenylboronic acid pinacol ester can structurally modify hyaluronic acid to prepare ROS-responsive intelligent nanocarriers and compound delivery systems. 4-Hydroxyphenylboronic acid pinacol ester endows hyaluronic acid-based nanocarriers with ROS responsiveness, enabling them to rapidly release the encapsulated Curcumin (HY-N0005) in the presence of reactive oxygen species. 4-Hydroxyphenylboronic acid pinacol ester is applicable to research related to periodontitis. 4-Hydroxyphenylboronic acid pinacol ester can also be used for the synthesis of boronic acid-modified resins .
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- HY-181821
-
|
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Parasite
Na+/K+ ATPase
|
Infection
|
|
MMV1581361 is a PfATP4 inhibitor and an orally active, transmission-blocking agent with nanomolar activity against Plasmodium falciparum blood-stage isolates. MMV1581361 disrupts sodium ion (Na +) homeostasis in Plasmodium falciparum. MMV1581361 inhibits male gamete exflagellation, reduces oocyst intensity, and blocks transmission of Plasmodium falciparum. MMV1581361 demonstrates efficacy in the humanized Plasmodium falciparum NOD scid IL2Rγ null mouse model. MMV1581361 can be used for the research of malaria .
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-
- HY-150520
-
|
|
Antibiotic
Phospholipase
|
Infection
Cancer
|
|
Neomycin, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin is a known phospholipase C (PLC) inhibitor. Neomycin potently inhibits both the nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis. Neomycin inhibits IP3-mediated Ca 2+ release, MgATP-dependent Ca 2+ uptake, and electrical excitation-evoked skeletal muscle Ca 2+ transients. Neomycin depletes gut microbiota in specific mouse models, causes hearing impairment, and kidney damage with prolonged exposure. Neomycin can be used for the research of cancer .
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-
- HY-10540
-
|
AEB071 acetate
|
PKC
NF-κB
|
Inflammation/Immunology
|
|
Sotrastaurin (AEB071) acetate is a selective, orally active PKC inhibitor. Sotrastaurin acetate inactivates NF-κB by inhibiting PKC α, β, θ, γ subtypes, thereby reducing the transcription levels of immune response-related genes. Sotrastaurin acetate effectively inhibits alloreactive T cell proliferation, conventional T cell activation, as well as the production of pro-inflammatory cytokines and B lymphocytes. Sotrastaurin acetate also maintains the functional and phenotypic stability of regulatory T cells, enhances Foxp3 expression and restores the balance of helper T lymphocytes. Sotrastaurin acetate can prolong the survival time of allografts, and alleviate inflammatory responses and myasthenic symptoms by reducing anti-AChR antibody levels. Sotrastaurin acetate is widely used in studies related to kidney transplantation, psoriasis and myasthenia gravis .
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-
- HY-119449
-
|
Zanchol
|
Others
|
Inflammation/Immunology
|
|
Florantyrone (Zanchol) is a bile-promoting agent. Florantyrone increases the volume of bile rather than the content of bile acids. Zanchol can stimulate the synthesis of cholesterol in the liver, significantly raising the plasma cholesterol level, increasing the weight of the liver, but has no significant effect on the synthesis of cholesterol in the intestine. Florantyrone can be used in research on biliary motility disorders .
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- HY-B0470
-
|
|
Environmental Pollutants
Antibiotic
Phospholipase
Bacterial
|
Infection
Metabolic Disease
Cancer
|
|
Neomycin sulfate, an aminoglycoside antibiotic, exerts antibacterial activity through irreversible binding of the nuclear 30S ribosomal subunit, thereby blocking bacterial protein synthesis. Neomycin sulfate is a known phospholipase C (PLC) inhibitor. Neomycin sulfate potently inhibits both the nuclear translocation of angiogenin and angiogenin-induced cell proliferation and angiogenesis. Neomycin sulfate inhibits IP3-mediated Ca 2+ release, MgATP-dependent Ca 2+ uptake, and electrical excitation-evoked skeletal muscle Ca 2+ transients. Neomycin sulfate depletes gut microbiota in specific mouse models, causes hearing impairment, and kidney damage with prolonged exposure. Neomycin sulfate can be used for the research of cancer .
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-
- HY-18071A
-
|
|
Na+/H+ Exchanger (NHE)
Autophagy
|
Cardiovascular Disease
|
|
BI-9627 hydrochloride is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 hydrochloride displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 hydrochloride decreases autophagy in HTR-8/SVneo cells. BI-9627 hydrochloride can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 hydrochloride prolongs Ca 2+ recovery time in KO hiPSC-CMs. BI-9627 hydrochloride shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
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-
- HY-181655
-
|
|
Cathepsin
|
Metabolic Disease
|
|
Anti-hepatic fibrosis agent 3 is an orally active anti-hepatic fibrosis compound targeting Cathepsin D. Anti-hepatic fibrosis agent 3 shows an IC50 of 53.18 μM against COL1A1-promoter and a Kd of 8.86 μM for binding to Cathepsin D. Anti-hepatic fibrosis agent 3 directly binds to and promotes the degradation of Cathepsin D, with no significant effect on Cathepsin B or Cathepsin L. Anti-hepatic fibrosis agent 3 inhibits hepatic stellate cell activation and reduces extracellular matrix deposition and inflammatory cytokine expression. Anti-hepatic fibrosis agent 3 exhibits remarkable anti-fibrotic activity in rat BDL and mouse CDAHFD-induced hepatic fibrosis models. Anti-hepatic fibrosis agent 3 can be used for the study of hepatic fibrosis .
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-
- HY-100603A
-
|
|
PI3K
PI4K
|
Infection
|
|
(S)-GSK-F1 (Compound 28) is an inhibitor for type III phosphatidylinositol 4-kinase α (PI4KIIIα). (S)-GSK-F1 inhibits PI4Kα, PI4Kβ, PI4Kγ, PI3Kα, PI3Kβ and PI3Kδ with pIC50 of 8.3, 6.0, 5.6, 5.6, 5.1 and 5.6, respectively. (S)-GSK-F1 exhibits anti-hepatitis C virus (HCV) activity through inhibition of HCV replication. (S)-GSK-F1 exhibits moderate pharmacokinetic characters in rat model .
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-
- HY-118506
-
|
|
FLAP
|
Inflammation/Immunology
|
BRP-7 is a 5-lipoxygenase activating protein (FLAP) inhibitor with an IC50 of 0.31 μM. BRP-7 inhibits the co-localization of 5-lipoxygenase (5-LOX) and FLAP by targeting FLAP, thereby blocking the transfer of arachidonic acid (AA) to 5-LOX and suppressing the production of leukotrienes (LTs) (IC₅₀ = 0.15 μM). BRP-7 does not inhibit cyclooxygenase (COX-1/COX-2) or microsomal prostaglandin E₂ synthase-1 (mPGES-1), and does not affect cell viability or AA release. BRP-7 exhibits significant anti-inflammatory effects in rat pleurisy and mouse peritonitis models. BRP-7 can be used for the study of inflammatory diseases .
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-
- HY-B0742R
-
|
17α-Hydroxyprogesterone hexanoate(Standard); 17α-Hydroxyprogesterone caproate (Standard)
|
Reference Standards
Progesterone Receptor
|
Others
|
|
Hydroxyprogesterone caproate (Standard) is the analytical standard of Hydroxyprogesterone caproate. This product is intended for research and analytical applications. Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
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-
- HY-186105A
-
|
|
Opioid Receptor
Apoptosis
|
Neurological Disease
|
|
(-)-P7C3-S243 is an orally active, blood-brain barrier permeable neuroprotective agent. (-)-P7C3-S243 binds to μ-opioid Receptor and TSPO. (-)-P7C3-S243 inhibits the premature apoptosis death of newborn hippocampal neurons, protects mature nigral dopaminergic neurons, promotes neuronal survival and prevents cognitive impairment. (-)-P7C3-S243 ameliorates depression-like behaviors in rat models. (-)-P7C3-S243 is applicable to research related to Parkinson's disease and Alzheimer's disease .
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-
- HY-177277
-
|
|
PI3K
|
Inflammation/Immunology
|
|
HM5023507 is an orally active and selective PI3Kδ/γ inhibitor with IC50s of 4 and 5 μM for PI3Kδ and PI3Kγ over PI3Kβ and PI3Kα. HM5023507 attenuates the PI3Kδ/γ signaling in human basophils. HM5023507 also attenuates the activation and function of human B and T cells and cytokine and IgG production during cocultures, and Th17 differentiation of CD4 T cells. HM5023507 inhibited semiestablished collagen-induced arthritic inflammation in the rat models. HM5023507 can be used for inflammatory diseases like rheumatoid arthritis research .
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-
- HY-N3847
-
|
Eriodictyol 7-O-β-D-glucoside
|
Keap1-Nrf2
|
Neurological Disease
|
|
Eriodictyol-7-O-glucoside (Eriodictyol 7-O-β-D-glucoside), a flavonoid, is an Nrf2 activator. Eriodictyol-7-O-glucoside exhibits significant scavenging effects on both hydroxyl radicals and superoxide anions, with IC50 values of 0.28 mM and 0.30 mM, respectively. Eriodictyol-7-O-glucoside increases the nuclear localization of Nrf2 and induces the expression of the Nrf2/ARE-dependent genes. Eriodictyol-7-O-glucoside provides protection against oxygen and glucose deprivation (OGD)-induced oxidative insult. Eriodictyol-7-O-glucoside demonstrates neuroprotective efficacy in a rat model of focal cerebral ischemia (MCAO). Eriodictyol-7-O-glucoside can be used for the study of stroke .
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-
- HY-P1123
-
|
|
ATP Citrate Lyase
Free Fatty Acid Receptor
Acetyl-CoA Carboxylase
|
Metabolic Disease
|
|
MEDICA16 is an orally active acetyl-CoA carboxylase and ATP-citrate lyase inhibitor. MEDICA16 limits the acetyl-CoA supply for acetyl-CoA carboxylase, inhibits acetyl-CoA carboxylase activity, exerts citrate-competitive inhibitory effects on ATP-citrate lyase, and reduces hepatic AMPK activity. MEDICA16 can be used in research related to insulin resistance, hyperlipidemia, and obesity .
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-
- HY-183370
-
|
|
JAK
STAT
Interleukin Related
|
Inflammation/Immunology
|
|
JAK2/STAT3-IN-2 is an orally active JAK2/STAT3 inhibitor. JAK2/STAT3-IN-2 inhibits the phosphorylation of tyrosine residues in JAK2 and STAT3, blocks downstream signal transduction, disrupts the dimerization and nuclear translocation of STAT3, and suppresses pro-inflammatory transcriptional activity. JAK2/STAT3-IN-2 inhibits the expression of IL-17A and IL-17F, reduces immune cell infiltration, and inhibits the production of NO simultaneously. JAK2/STAT3-IN-2 exerts a protective effect in a mouse model of ulcerative colitis induced by DSS (HY-116282C). JAK2/STAT3-IN-2 can be used for the research of ulcerative colitis .
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-
- HY-181178
-
|
|
Amyloid-β
|
Neurological Disease
|
|
(Mor-Cor)Ag(III) is a blood-brain barrier-penetrant silver(III) corrole complex that penetrates the blood-brain barrier. (Mor-Cor)Ag(III) scavenges reactive oxygen species induced by Aβ42 and disrupts Aβ42 aggregation, attenuating Aβ42-induced neuronal hyperactivity. (Mor-Cor)Ag(III) can be used for the research of Alzheimer's disease .
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-
- HY-181792
-
|
|
STAT
|
Inflammation/Immunology
|
|
ZDZ-553 is an orally active STAT1 inhibitor with an IC50 value of 0.87 μM. ZDZ-553 modulates STAT1 signaling to affect downstream lipid metabolism and inflammatory pathways. ZDZ-553 attenuates hepatic steatosis in NASH mouse models. ZDZ-553 reduces inflammatory responses in NASH mouse models. ZDZ-553 can be used for the research of nonalcoholic steatohepatitis .
|
-
- HY-182940
-
|
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
SARM1-IN-10 is an orally active SARM1 inhibitor with a pIC50 of 7.1 and a pKd of 8.3. As a base-exchange inhibitor, SARM1-IN-10 forms a NAD + adduct at the active site of the TIR domain of SARM1, blocks enzymatic function, and induces a unique rotameric state of W662 at the catalytic site of SARM1. SARM1-IN-10 acts as a paradoxical neurodegeneration inducer at low doses and an inhibitor at high doses, and it can exacerbate or protect against SARM1-mediated neurodegeneration depending on concentration. SARM1-IN-10 can be used in studies of peripheral neurodegeneration .
|
-
- HY-W013403
-
|
|
IFNAR
|
Infection
|
|
2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
|
-
- HY-147294
-
|
ACT-539313
|
Orexin Receptor (OX Receptor)
Cytochrome P450
|
Neurological Disease
|
|
Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder .
|
-
- HY-B0742S1
-
|
17α-Hydroxyprogesterone hexanoate-d8; 17α-Hydroxyprogesterone caproate-d8
|
Isotope-Labeled Compounds
Progesterone Receptor
|
Others
|
|
Hydroxyprogesterone caproate-d8 (17α-Hydroxyprogesterone hexanoate-d8) is the deuterium labeled Hydroxyprogesterone caproate (HY-B0742). Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
|
-
- HY-10201
-
Sorafenib
Maximum Cited Publications
283 Publications Verification
Bay 43-9006
|
Raf
VEGFR
FLT3
Autophagy
Apoptosis
STAT
Akt
MMP
Cadherin
p38 MAPK
ERK
MEK
PI3K
PARP
Bcl-2 Family
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Sorafenib (Bay 43-9006) is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib inhibits tumor growth and metastasis in mouse and rat models. Sorafenib can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma .
|
-
- HY-P992410
-
|
|
PAI-1
TGF-beta/Smad
|
Inflammation/Immunology
|
|
MEDI-579 is a fully human monoclonal antibody against PAI-1, with a KD value of 6 pM for human PAI-1 and 105 pM for rat PAI-1. MEDI-579 restores renal plasmin activity and inhibits PAI-1-mediated intracellular signal transduction. MEDI-579 reduces albuminuria, glomerulosclerosis severity, TGF-β1 expression level, and phosphorylated Smad2 level induced in diabetic mice. MEDI-579 decreases the levels of active PAI-1 in plasma and kidneys, and increases plasma plasmin level in a mouse model of lupus nephritis. MEDI-579 can be used in research related to diabetic nephropathy and lupus nephritis. The recommended isotype control is human IgG1 kappa (HY-P99001) .
|
-
- HY-18071
-
BI-9627
3 Publications Verification
|
Na+/H+ Exchanger (NHE)
Autophagy
|
Cardiovascular Disease
|
|
BI-9627, a chemical probe, is a potent sodium-hydrogen exchanger isoform 1 (NHE1) inhibitor (IC50 = 6 and 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays). BI-9627 displays >30-fold selectivity against NHE2 and with no measurable inhibitory activity against the NHE3 isoform. BI-9627 decreases autophagy in HTR-8/SVneo cells. BI-9627 can significantly reduce the pHi of human sperm and partially reverse the effect of DMA. BI-9627 prolongs Ca 2+ recovery time in KO hiPSC-CMs. BI-9627 shows low DDI (agent-agent interaction) potential, excellent pharmacokinetics in rat and dog, and remarkably potent activity in the isolated heart model of ischemia-reperfusion injury .
|
-
- HY-10201A
-
|
Bay 43-9006 tosylate
|
Raf
VEGFR
FLT3
Autophagy
Apoptosis
STAT
Akt
MMP
Cadherin
p38 MAPK
ERK
MEK
PI3K
PARP
Bcl-2 Family
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Sorafenib (Bay 43-9006) tosylate is a potent oral active multikinase inhibitor. Sorafenib blocks autophosphorylation and activity of receptor tyrosine kinases (VEGFR-2, VEGFR-3) and RAF family kinases, thereby suppressing the RAF/MEK/ERK and PI3K/Akt pathways, inhibiting STAT3 phosphorylation, and selectively inhibiting the MAPK pathway in cancer cells. Sorafenib tosylate induces cell cycle arrest, autophagy, apoptosis, and PARP cleavage, reduces Bcl-2, Bcl-XL, cyclin D1 levels, and activates Bak and Bax. Sorafenib tosylate inhibits tumor growth and metastasis in mouse and rat models. Sorafenib tosylate can be used for cancer research, such as colon, breast, non-small-cell lung cancer (NSCLC), ovarian, pancreatic, melanoma, colorectal and hepatocellular carcinoma .
|
-
- HY-182021
-
|
|
Amine N-methyltransferase
|
Endocrinology
|
|
NNMT-IN-8 is a non-SAM-mimicking bisubstrate inhibitor and a selective methyltransferase NNMT inhibitor, with IC50 values of 0.0084 μM and 0.0085 μM against human NNMT, and an IC50 of 0.0072 μM against mouse NNMT. NNMT-IN-8 exhibits prominent renal distribution characteristics and moderate bioavailability in rodents. NNMT-IN-8 dose-dependently inhibits renal NNMT in renal fibrosis models, thereby exerting antifibrotic effects. NNMT-IN-8 can be used to investigate the mechanisms of renal fibrosis .
|
-
- HY-182358
-
|
|
Apoptosis
|
Cancer
|
|
TMLZ-G46 is an orally active ZNF207 inhibitor with blood-brain barrier penetration ability, with a Kd value of 68 nM. TMLZ-G46 inhibits cancer cell proliferation, stemness, migration and invasion, induces G0/G1 cell cycle arrest and apoptosis, and suppresses colony formation. TMLZ-G46 can be used in glioma research .
|
-
- HY-N17737
-
|
|
Fatty Acid Synthase (FASN)
Cytochrome P450
|
Metabolic Disease
Inflammation/Immunology
|
|
Floramanoside F is a type of flavonol glycoside compound. Floramanoside F has a moderate free radical scavenging effect, with a SC₅₀ value of 25.1 μM. Floramanoside F has a relatively weak inhibitory activity on aldose reductase, with a IC₅₀ value greater than 100 μM. Floramanoside F has strong binding affinity with key target enzymes of type 1 diabetic nephropathy (T1DN) (Fasn, Cyp2e1, Cyp4a32), and can inhibit lipid accumulation and oxidative stress, thereby alleviating renal inflammation and fibrosis. Floramanoside F can be used to study type 1 diabetic nephropathy and diabetic complications .
|
-
- HY-14318
-
|
SIB-1508Y free base
|
nAChR
|
Neurological Disease
|
|
Altinicline (SIB-1508Y free base) is a selective α4β2 nicotinic acetylcholine receptor (nAChR) agonist, with no activity against α7 or α1β1γδ nAChRs and only extremely low activity against α3β4 nAChRs. Altinicline reverses escape deficits and increases avoidance responses. Altinicline is applicable to research related to depression .
|
-
- HY-116514
-
|
|
Farnesyl Transferase
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
(S)-(-)-Perillyl alcohol, a monoterpene, is an orally active farnesyl transferase and geranylgeranyl transferase inhibitor. (S)-(-)-Perillyl alcohol up-regulates the mannose-6-phosphate receptor, facilitating TGF-β1 activation and cytostasis,. (S)-(-)-Perillyl alcohol induces apoptosis in cancer cells, modulates cyclin D1 and AP-1 activity. (S)-(-)-Perillyl alcohol exhibits antitumor activity against sarcoma tumors in mice. (S)-(-)-Perillyl alcohol can be used for the research of squamous cell carcinoma of the esophagus and sarcoma 180 .
|
-
- HY-181559S
-
|
AG06827
|
mAChR
|
Neurological Disease
|
|
VU6025733 (AG06827) is a highly selective, orally active and blood-brain barrier-penetrant positive allosteric modulator of the muscarinic acetylcholine receptor subtype M4 (M4 mAChR). VU6025733 exerts a potentiating effect on acetylcholine-induced receptor activation with an EC50 of 23 nM for hM4 and 55 nM for rM4. VU6025733 shows high selectivity over other muscarinic acetylcholine receptor subtypes, dose-dependently reduces amphetamine-induced hyperlocomotion in rats. VU6025733 is applicable to the research of schizophrenia, Parkinson's disease, and Alzheimer's disease .
|
-
- HY-136805
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Kv1.5-IN-1 is a Kv1.5 channel inhibitor. Its target selectivity and pharmacodynamic effects were evaluated in an in vitro rat model. After the introduction of a methoxy group at the R5 position, Kv1.5-IN-1 showed inhibitory potency similar to that of the unsubstituted compound. Its IC50 value for hKv1.5 channels was 0.51 μM. Kv1.5-IN-1 exhibited a high degree of selectivity, nearly 2,600 times higher than compound Ik and 300 times higher than compound IId, indicating that it may be a safe inhibitor. Due to its good pharmacological behavior, Kv1.5-IN-1 deserves further pharmacodynamic and pharmacokinetic evaluation. These properties make Kv1.5-IN-1 a potential Kv1.5 channel inhibitor that may have application prospects in the treatment of related diseases.
|
-
- HY-W008270R
-
|
γ-Crotonolactone (Standard)
|
Reference Standards
Endogenous Metabolite
|
Others
|
|
2(5H)-Furanone (Standard) is the analytical standard of 2(5H)-Furanone. This product is intended for research and analytical applications. 2(5H)-Furanone (γ-Crotonolactone) is an endogenous metabolite. 2(5H)-Furanone mimics N-acyl homoserine lactone signals, occupies the binding site of LuxR homologs, and interferes with quorum sensing-mediated gene regulation. 2(5H)-Furanone inhibits quorum sensing mediated by AHLs with different acyl chain lengths. 2(5H)-Furanone inhibits biofilm formation of environmental Aeromonas hydrophila strains on polystyrene plates. 2(5H)-Furanone suppresses spike-and-wave discharges in a rat model of generalized absence seizures and exhibits selective activity against absence seizures. 2(5H)-Furanone can be used in studies related to bacteria infections and generalized absence seizures.
|
-
- HY-185426
-
|
SC-011
|
Antibody-Drug Conjugates (ADCs)
|
Cancer
|
|
ABBV-011 (SC-011) is a SEZ6-targeted, antibody-drug conjugate (ADC). ABBV-011 binds cell surface-expressed SEZ6 by anti-SEZ6 antibody Turmetabart (HY-P991041), triggers ADC-receptor complex internalization into lysosomes, releases Calicheamicin (HY-19609) payload, and mediates cytotoxicity. ABBV-011 induces tumor regression and mediates selective killing of SEZ6-positive cells. ABBV-011 can be used for the research of small cell lung cancer .
|
-
- HY-P10739
-
|
|
Exosomes
Collagen
|
Inflammation/Immunology
|
|
WYRGRL is a selective, high-affinity collagen type II-binding peptide with a IC50 of 140 nM. Collagen type II is the most abundant and specific structural protein in the extracellular matrix of articular cartilage. WYRGRL can precisely target small-molecule compounds such as Dexamethasone (HY-14648) and nanocarrier-engineered exosomes to cartilage, significantly enhancing their therapeutic effects on osteoarthritis .
|
-
- HY-N8698
-
Picein
1 Publications Verification
|
SOD
Ferroptosis
Keap1-Nrf2
Heme Oxygenase (HO)
Glutathione Peroxidase
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Picein is an antioxidant and anti-inflammatory agent. Picein can be isolated from the leaves of Picrorhiza kurroa. Picein reduces MDA levels and increases the levels of SOD, GPX and TAC. Picein alleviates oxidative stress and promotes bone regeneration in osteoporotic bone defects by inhibiting Ferroptosis (via activation of the Nrf2/HO-1/GPX4 pathway). Picein prevents scopolamine (HY-N0296)-induced passive avoidance memory impairment in rats. Picein can be used in research related to osteoporotic bone defects and Alzheimer's disease .
|
-
- HY-12764R
-
-
- HY-W089800
-
|
trans-2-Nonen-1-al
|
COX
Lipoxygenase
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
|
|
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .
|
-
- HY-12764
-
6-OAU
4 Publications Verification
GTPL5846
|
GPR84
ERK
Bacterial
Antibiotic
|
Inflammation/Immunology
|
|
6-OAU (GTPL5846) (6-n-octylaminouracil) is an GPR84 (G protein-coupled receptor 84) agonist, with an EC50 value of 105 nM. 6-OAU works as a chemoattractant to both PMNs and macrophages, and amplifies the proinflammatory cytokine IL-8, shows proinflammatory function. 6-OAU also displays anti-bacterial function .
|
-
- HY-134160S
-
|
5-DHFU-13C,15N2; 5-Fluorodihydropyrimidine-2,4-dione-13C,15N2; 5-Fluorodihydrouracil-13C,15N2
|
Isotope-Labeled Compounds
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
5,6-Dihydro-5-Fluorouracil- 13C, 15N2 (5-DHFU- 13C, 15N2) is the 13C- and 15N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
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-
- HY-N15378
-
|
|
IAP
Bcl-2 Family
COX
TNF Receptor
Caspase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
β-carotene-15,15ʹ-epoxide is a XIAP antagonist with apoptosis-inducing and antitumor activity, found in the leaves of Spondias mombin. In a DMBA (HY-W011845)-induced rat model of breast cancer, β-carotene-15,15ʹ-epoxide binds to the BIR3 domain of the anti-apoptotic protein XIAP, blocking its interaction with caspase-9 and thereby promoting tumor cell apoptosis. In addition, β-carotene-15,15ʹ-epoxide significantly downregulates the expression of BCL-2, COX-2, and TNF-α in tumor tissues, reduces MDA levels, increases catalase activity, and modulates serum levels of LDH, ALP, and ALT, demonstrating strong antioxidant, anti-inflammatory, and metabolic protective effects. β-carotene-15,15ʹ-epoxide may be used in research on inflammation-related conditions and cancers such as breast cancer .
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-
- HY-110390
-
|
|
Carboxylesterase (CES)
Free Fatty Acid Receptor
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
Ferroptosis
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
GR148672X is an inhibitor of carboxylesterase 1 (CES1) and hepatic microsomal triglyceride hydrolase (TGH). GR148672X blocks the catalytic activity of CES1, impairs the functions of triglyceride and cholesteryl ester lipase, reduces triglyceride mobilization and secretion, and decreases apolipoprotein B-100 secretion in primary rat hepatocytes. Under low-glucose conditions, GR148672X inhibits the survival of colorectal cancer cells by reducing free fatty acid availability, inducing toxic triglyceride accumulation, ROS production, mitochondrial damage, ferroptosis and apoptosis. GR148672X can be used in studies related to colorectal cancer and atherosclerosis .
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-
- HY-P11259
-
|
|
Urotensin Receptor
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
UPG-111 is a peptide compound that acts as a negative allosteric modulator of the Urotensin II receptor (UTR). UPG-111 exhibits a dual inhibitory effect on the vasoconstriction induced by UTR agonists - it reduces both the maximum response intensity and the sensitivity of the agonist. UPG-111 does not induce calcium release or cause contraction of the endothelium-deprived rat aortic rings. UPG-111 can be used for the study of various diseases related to the angiotensinergic system .
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-
- HY-W013403S
-
|
|
IFNAR
|
Infection
|
|
2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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-
- HY-N0430A
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
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-
- HY-186072
-
|
|
NOD-like Receptor (NLR)
Interleukin Related
Cytochrome P450
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
NT-0527 is a selective, orally active, and brain-permeable NLRP3 inflammasome inhibitor. NT-0527 can specifically block the formation of the NLRP3 inflammasome, resulting in the reduction in the maturation and release of IL-1β, exhibit inhibition on CYP2C19. NT-0527 displays anti-inflammatory activity in the mouse LPS (HY-D1056) /ATP (HY-B2176)-induced peritonitis model. NT-0527 can be used for the research of neuroinflammatory disorders (Parkinson's disease, Alzheimer's disease, amyotrophic lateral sclerosis) and peripheral inflammatory disorders (type II diabetes, atherosclerosis, gout, etc.) associated with NLRP3 inflammasome .
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-
- HY-P992098
-
|
NEI-01
|
Protein Arginine Deiminase
|
Cancer
|
|
Adargiminase (NEI-01) is a modified arginine-depleting enzyme and albumin binder. Adargiminase catalyzes the conversion of arginine to citrulline and ammonia, reduces plasma arginine levels to undetectable levels, and binds to serum albumin from Mus musculus (mouse), Rattus norvegicus (rat), Canis lupus familiaris (dog) and Homo sapiens (human) to extend its half-life. Adargiminase inhibits the viability of ASS1-negative pancreatic cancer cells, and reduces tumor volume and weight. Adargiminase can be used for the research of pancreatic cancer .
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-
- HY-186073
-
|
|
HDAC
|
Neurological Disease
|
|
HDAC1 activator-1 is a specific HDAC1 activator with orally activity, exerting no significant effects on other HDAC family members. HDAC1 activator-1 exhibits neuroprotective activity, ameliorates cognitive and motor function deficits by reducing neuronal loss and gliosis. HDAC1 activator-1 specifically activates HDAC1 in SH-SY5Y cells and exerts regulatory effects on aberrant cell cycle and DNA damage. HDAC1 activator-1 can be used for the research of TDP-43 proteinopat1-related neurodegenerative diseases including Amyotrophic Lateral Sclerosis (ALS) and cerebral ischemia-related neurological injury .
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-
- HY-175340
-
|
|
Potassium Channel
TSPO
|
Neurological Disease
|
|
Kv7.2/Kv7.3 activator-3 (GRT-X) is an orally active Kv7.2/Kv7.3 and TSPO activator. Kv7.2/Kv7.3 activator-3 activates Kv7.2/Kv7.3, Kv7.4, and Kv7.5 with EC50 values of 0.37, 2.06, and 0.75 μM, respectively, and binds to TSPO with Ki values of 0.07 μM (rat membrane) and 4.60 μM (human U-118 MG cells). Kv7.2/Kv7.3 activator-3 prevents motor neuron degeneration in mice and humans conditioned by ALS/FTD astrocytes. Kv7.2/Kv7.3 activator-3 stimulates dorsal root ganglion axonal growth through TSPO and Kv7.2/3 activation. Kv7.2/Kv7.3 activator-3 has anti-epileptic effects in epileptic seizure models. Kv7.2/Kv7.3 activator-3 reduces pain hypersensitivity in patients with diabetic neuropathy, promotes neuronal survival and regeneration after cervical neuropathy in rats, and accelerates the recovery of normal function of sensory and motor neurons .
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-
| Cat. No. |
Product Name |
Type |
-
- HY-D2968
-
|
|
Fluorescent Dye
|
|
DCM-ONOO is a near-infrared two-photon fluorescence probe specifically designed for real-time monitoring of the dynamic fluctuations of peroxynitrite (ONOO⁻) in epilepsy models. DCM-ONOO exhibits excellent optical properties, with a single photon excitation (Ex) of 520 nm; a single photon emission (Em) of 685 nm; a two-photon excitation of 820 nm; and a Stokes shift of 165 nm. When DCM-ONOO is combined with ONOO⁻, it shifts from 460 nm to 512 nm, and only generates a significant fluorescence response to ONOO⁻. DCM-ONOO has been successfully applied to rat epilepsy models .
|
| Cat. No. |
Product Name |
Type |
-
- HY-Y0816
-
|
|
Biochemical Assay Reagents
|
|
(S)-Mandelic Acid is a (S)-enantiomer of Mandelic Acid (HY-W015591). (S)-Mandelic Acid undergoes one-directional chiral inversion to (R)-Mandelic Acid in rat models. (S)-Mandelic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research .
|
-
- HY-158231
-
|
F127DA
|
Biochemical Assay Reagents
|
|
Polyether F127 Diacrylate (F127DA) is an acrylated polyethylene glycol-polypropylene glycol-polyethylene glycol triblock copolymer. Polyether F127 Diacrylate rapidly crosslinks and cures into a gel under ultraviolet or visible light with the action of a photoinitiator. Polyether F127 Diacrylate exhibits excellent thermogelation properties and favorable biosafety. Polyether F127 Diacrylate can upregulate the Integrin-FAK pathway, enhance collagen production, increase the protein and gene expression levels of COL-1/SCX, and promote fibroblastic differentiation of periodontal ligament stem cells. Polyether F127 Diacrylate promotes periodontal ligament regeneration and reduces abnormal healing in a rat model of delayed replanted teeth . Polyether F127 Diacrylate promotes functional osteochondral regeneration in a rat model of osteoarthritis. Polyether F127 Diacrylate supports adipose tissue survival, rendering it suitable for breast reconstruction applications. Polyether F127 Diacrylate can be used in studies related to periodontal ligament injury, breast defect and osteoarthritis .
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-
- HY-N0729D
-
|
|
Biochemical Assay Reagents
|
|
Linoleic acid is a critical component of polyunsaturated fatty acids. Linoleic acid reduces GSH-PX and T-SOD activities. Linoleic acid functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid can cause acute oxidative damage to red blood cells, ultimately leading to partial acute anemia. Linoleic acid can be used in the research of skin diseases associated with linoleic acid deficiency .
|
-
- HY-W004761
-
|
Hypodiboric acid
|
Biochemical Assay Reagents
|
|
Tetrahydroxydiboron acts as a hydrogel initiator and bioadhesion promoter, with broad-spectrum antibacterial activity, ROS scavenging capacity and osteogenic induction properties. Tetrahydroxydiboron initiates rapid gelation by generating free radicals through reactions with vinyl monomers and dissolved oxygen, and overcomes oxygen inhibition without deoxygenation or external triggers. Tetrahydroxydiboron achieves strong bioadhesion through interaction with carboxymethyl chitosan. Tetrahydroxydiboron can be used in the research of periodontitis and related inflammatory diseases .
|
-
- HY-W089800
-
|
trans-2-Nonen-1-al
|
Biochemical Assay Reagents
|
|
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .
|
-
- HY-W002879
-
|
|
Biochemical Assay Reagents
|
|
4-Hydroxyphenylboronic acid pinacol ester is a ROS-responsive component. 4-Hydroxyphenylboronic acid pinacol ester can structurally modify hyaluronic acid to prepare ROS-responsive intelligent nanocarriers and compound delivery systems. 4-Hydroxyphenylboronic acid pinacol ester endows hyaluronic acid-based nanocarriers with ROS responsiveness, enabling them to rapidly release the encapsulated Curcumin (HY-N0005) in the presence of reactive oxygen species. 4-Hydroxyphenylboronic acid pinacol ester is applicable to research related to periodontitis. 4-Hydroxyphenylboronic acid pinacol ester can also be used for the synthesis of boronic acid-modified resins .
|
-
- HY-158223
-
|
CMCSMA
|
Biochemical Assay Reagents
|
Carboxymethyl chitosan Methacryloyl (CMCSMA) is methacrylated carboxymethyl chitosan with properties as a 3D printing ink. A composite hydrogel made of Carboxymethyl chitosan Methacryloyl can effectively accelerate bone healing in an infectious microenvironment after implantation in a rat model of Staphylococcus aureus-infected femoral defect . Carboxymethyl chitosan Methacryloyl needs to self-assemble into fibrous hydrogel under the action of photoinitiator LAP (HY-44076), and target bioactive adhesion sites, play an inherent supporting role for tissue cells and biodegradable activity.
Application: cell culture, biological 3D printing, tissue engineering, etc.
|
-
- HY-W145695
-
|
|
Biochemical Assay Reagents
|
|
Chitoheptaose is an orally active chitooligosaccharide (degree of polymerization = 7). Chitoheptaose can be extracted from the exoskeletons of crustaceans, such as the shells of crabs, shrimps and lobsters. Chitoheptaose reduces pro-inflammatory cytokines while increasing the levels of anti-inflammatory cytokines (decreasing the levels of pro-inflammatory cytokines IL-1β, IL-17A and IFN-γ, and increasing the level of the anti-inflammatory cytokine IL-10). Chitoheptaose possesses antioxidant, anti-inflammatory and anti-Apoptotic activities. Chitoheptaose improves cardiac parameters, alleviates myocarditis injury, and exerts cardioprotective effects in a rat model of myocarditis. Chitoheptaose can be used in studies related to myocarditis .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1240
-
|
Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat
|
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
|
MOG (35-55) mouse, rat (Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat) is a minor component of CNS myelin. MOG (35-55) mouse, rat has encephalitogenic activity and induces T cell proliferative. MOG (35-55) mouse, rat induces Th1 cytokine response as well as relatively high levels of IgG antibodies. MOG (35-55) mouse, rat produces a relapsing-remitting neurological disease with extensive plaque-like demyelination. MOG (35-55) mouse, rat (MOG (35-55)) can be used for experimental autoimmune encephalomyelitis (EAE) modeling .
|
-
- HY-P1098
-
|
|
Annexin A
NF-κB
|
Inflammation/Immunology
|
|
Ac2-26 is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ameliorates lung ischemia-reperfusion injury. Ac2-26 also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-P10587
-
|
JNJ-77242113; JNJ-2113; PN-235
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-P3719
-
|
|
CCR
|
Inflammation/Immunology
|
|
MOG (35-55) amide, mouse, rat the terminal amidation form of the 35-55 fragment of the myelin oligodendrocyte glycoprotein (MOG) immunogenic peptide (MOG (35-55) (HY-P1240)). MOG(35-55) amide, mouse, rat can be used for experimental autoimmune encephalomyelitis (EAE) modeling .
|
-
- HY-P1010
-
Z-LEHD-FMK
Maximum Cited Publications
15 Publications Verification
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
|
Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-12378
-
BQ-123
3 Publications Verification
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
BQ-123 is a potent and selective endothelin A (ETA) receptor antagonist with an IC50 of 7.3 nM and a Ki of 25 nM. BQ-123 inhibits endothelin-1-mediated proliferation of human pulmonary artery smooth muscle cells and lowers blood pressure in different rat models of hypertension .
|
-
- HY-148195
-
|
NNZ-2591
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Ercanetide (NNZ 2591) is a synthetic analogue of a small peptide of cyclic glycine proline (cGP). Ercanetide shows orally active and cross the blood-brain barrier. Ercanetide shows neuroprotective after ischemic brain injury. NNZ 2591 improves motor function in a rat model of Parkinson's disease. Ercanetide has the potential for the research of ischemic brain injury and angelman syndrome .
|
-
- HY-P1240B
-
|
Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat acetate
|
Peptides
|
Neurological Disease
Inflammation/Immunology
|
|
MOG (35-55) (Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat) acetate is a minor component of CNS myelin. MOG (35-55) (acetate) has encephalitogenic activity and induces T cell proliferative. MOG (35-55) (acetate) induces Th1 cytokine response as well as relatively high levels of IgG antibodies. MOG (35-55) (acetate) produces a relapsing-remitting neurological disease with extensive plaque-like demyelination. MOG (35-55) (Myelin Oligodendrocyte Glycoprotein Peptide (35-55), mouse, rat) acetate can be used for experimental autoimmune encephalomyelitis (EAE) modeling .
|
-
- HY-P10739
-
|
|
Exosomes
Collagen
|
Inflammation/Immunology
|
|
WYRGRL is a selective, high-affinity collagen type II-binding peptide with a IC50 of 140 nM. Collagen type II is the most abundant and specific structural protein in the extracellular matrix of articular cartilage. WYRGRL can precisely target small-molecule compounds such as Dexamethasone (HY-14648) and nanocarrier-engineered exosomes to cartilage, significantly enhancing their therapeutic effects on osteoarthritis .
|
-
- HY-145512
-
|
NLT
|
Dopamine Receptor
|
Neurological Disease
|
|
N-(α-Linolenoyl) tyrosine (NLT) is a dopaminergic agonist capable of crossing the blood-brain barrier. N-(α-Linolenoyl) tyrosine increases the level, turnover rate and release amount of dopamine in the striatum. N-(α-Linolenoyl) tyrosine modulates rotational behavior in a rat model with unilateral striatal injury and alleviates excessive blinking symptoms in models induced by dopamine-depleting agents. N-(α-Linolenoyl) tyrosine can be used for research on Parkinson's disease and idiopathic blepharospasm .
|
-
- HY-W041988
-
|
|
Bacterial
|
Infection
|
|
Fmoc-Glu-OMe is a glutamic acid derivative. Fmoc-Glu-OMe exhibits significant antibacterial activity and excellent gelation properties in silver nitrate (AgNO3) solution. Fmoc-Glu-OMe promotes wound healing in rat models and eliminates bacteria in MRSA-infected rat wound models. Fmoc-Glu-OMe can be used in studies related to wound infections and MRSA-infected wounds .
|
-
- HY-P5558
-
|
|
VEGFR
|
Neurological Disease
|
|
KLTWQELYQLKYKGI is a VEGF mimetic peptide designed based on the VEGF helix sequence 17-25, with the ability to activate VEGF receptors and exert pro-angiogenic biological activity. KLTWQELYQLKYKGI effectively promotes the attachment, spreading and proliferation of human umbilical vein endothelial cells. KLTWQELYQLKYKGI enhances the proliferation, migration and osteogenic differentiation of bone marrow stromal cells (BMSCs). KLTWQELYQLKYKGI synergistically accelerates angiogenesis and bone regeneration in rat cranial defect models. KLTWQELYQLKYKGI can be used for the research of brain tissue engineering and traumatic brain injury repair and biomaterials for bone tissue engineering and bone repair .
|
-
- HY-P10580
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-119152
-
|
|
Insulin Receptor
Tyrosinase
Akt
|
Others
|
|
CMX-2043 is a novel analogue of α-Lipoic Acid (HY-N0492). CMX-2043 is effective in antioxidant effect, activation of insulin receptor kinase, soluble tyrosine kinase, and Akt phosphorylation. CMX-2043 shows protection against ischemia-reperfusion injury (IRI) in rat model .
|
-
- HY-P11111
-
|
|
Drug Derivative
|
Others
|
|
QP5 is an Amelogenin (HY-P71627)-derived peptide. QP5 binds on the hydroxyapatite and demineralized tooth enamel surfaces, transitorily stabilize the amorphous calcium phosphate (ACP), control the crystallization of hydroxyapatite and promote the remineralization of caries lesions. QP5 promotes remineralization in rat caries models. QP5 can be used for oral diseases like dental caries research .
|
-
- HY-P1098A
-
|
|
Annexin A
NF-κB
|
Inflammation/Immunology
|
|
Ac2-26 TFA is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ameliorates lung ischemia-reperfusion injury. Ac2-26 also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-P1091
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1090
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P3498
-
|
ZP1846
|
GCGR
|
Others
|
|
Elsiglutide (ZP1846) is a GLP-2 analogue, an orally active and selective GLP-2 receptor agonist, increases cell proliferation and reduces apoptosis in the intestine. Elsiglutide improves Lapatinib (HY-50898)-induced diarrhoea in rat model .
|
-
- HY-P10580A
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide TFA, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide TFA ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide TFA promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide TFA protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide TFA decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-P1098B
-
|
|
IKK
|
Inflammation/Immunology
|
|
Ac2-26 ammonium is the N-terminal peptide of annexin 1, and has anti-inflammatory activity. Ac2-26 ammonium induces a decrease in IKKβ protein in lysosomes by chaperone-mediated autophagy (CMA). Ac2-26 ammonium ameliorates lung ischemia-reperfusion injury. Ac2-26 ammonium also inhibits airway inflammation and hyperresponsiveness in an asthma rat model .
|
-
- HY-P11043
-
|
|
GLP Receptor
Neuropeptide Y Receptor
Arrestin
|
Metabolic Disease
|
|
GEP44 is a peptide biased triple agonist targeting Glucagon-like peptide 1 receptor (GLP-1R), neuropeptide Y1 Receptor (Y1-R), and neuropeptide Y2 Receptor (Y2-R). GEP44 induces Y1-R antagonist-controlled, GLP-1R-dependent stimulation of insulin secretion in both rat and human pancreatic islets by counteracting effects of Y1-R and GLP-1R agonism. GEP44 promotes insulin-independent Y1-R-mediated glucose uptake in muscle tissue and significantly reduces food intake and body weight in diet-induced obese rat models. GEP44 can be used for obesity and type 2 diabetes mellitus research .
|
-
- HY-P1010A
-
|
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
|
Z-LEHD-FMK TFA is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK TFA exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-179475
-
|
|
CaSR
|
Endocrinology
|
|
KP-2067 is a form of the CaSR agonist peptide. KP-2067 can result in dose-dependent activation of CaSR in HEK293T overexpressing hCaSR cell line, with an EC50 of 18.4 μM. KP-2067 significantly reduces plasma parathyroid hormone in rat model .
|
-
- HY-P10360
-
|
|
α-synuclein
|
Neurological Disease
|
|
Tat-βsyn-degron is an α-synuclein knockdown peptide that effectively degrades α-synuclein protein via the proteasome pathway. Tat-βsyn-degron effectively reduces α-synuclein protein levels in primary rat cortical neuron cultures. In a Parkinson's mouse toxicity model, Tat-βsyn-degron can alleviate parkinsonian toxin-induced neuronal damage and movement disorders .
|
-
- HY-P10405A
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
TAT-D1 peptide acetate is a dopamine D1-D2 receptor heterodimer inhibitor. TAT-D1 peptide acetate disrupts the function of dopamine D1-D2 receptor heteromers, enhances subchronic amphetamine-induced locomotor activity, and exacerbates the expression of amphetamine-induced locomotor sensitization. TAT-D1 peptide acetate produces rapid anxiolytic and antidepressant-like effects in rat models of depression and anxiety, and inhibits c-fos expression in the nucleus accumbens of rats. TAT-D1 peptide acetate can be used in the research of psychostimulant addiction, depression and anxiety disorders .
|
-
- HY-P3199
-
|
|
PKC
|
Inflammation/Immunology
|
|
PKCβII Peptide Inhibitor I is a PKCβII inhibitor. PKCβII Peptide Inhibitor I shows cardioprotective effects in rat cardiac Ischemia/reperfusion injury model. PKCβII Peptide Inhibitor I also prevents vascular endothelial dysfunction .
|
-
- HY-P10898
-
-
- HY-P10587A
-
|
JNJ-77242113 acetate; JNJ-2113 acetate; PN-235 acetate
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) acetate is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra acetate inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. Icotrokinra acetate exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra acetate can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-P10870
-
|
|
Peptide-Drug Conjugates (PDCs)
FGFR
Apoptosis
|
Cancer
|
|
Pep1-DNP conjugate 9 is a functionalized peptide which is composed of the DNP-Hapten and the FGFR1 binding peptide. Pep1-DNP conjugate 9 exhibits good affinity to FGFR1 with KD of 5.01 μM. Pep1-DNP conjugate 9 recruits anti-DNP antibodies to the surface of FGFR1-positive cells, inhibits the FGF2-induced proliferation in rat skeletal myoblast cells, and induces apoptosis. Pep1-DNP conjugate 9 exhibits antitumor efficacy in mouse models .
|
-
- HY-P10405
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
TAT-D1 peptide is a dopamine D1-D2 receptor heterodimer inhibitor. TAT-D1 peptide disrupts the function of dopamine D1-D2 receptor heteromers, enhances subchronic amphetamine-induced locomotor activity, and exacerbates the expression of amphetamine-induced locomotor sensitization. TAT-D1 peptide produces rapid anxiolytic and antidepressant-like effects in rat models of depression and anxiety, and inhibits c-fos expression in the nucleus accumbens of rats. TAT-D1 peptide can be used in the research of psychostimulant addiction, depression and anxiety disorders .
|
-
- HY-P5978
-
|
ANP 127-150 (rat)
|
Natriuretic Peptide Receptor (NPR)
|
Cardiovascular Disease
|
|
Atriopeptin III (ANP 127-150) (rat), a 24-amino acid atrial peptide, is a potent vasodilator and natriuretic/diuretic agent. Atriopeptin III (rat) improves renal functions and decreases blood pressure in a ureter-obstructed rat kidney model. Atriopeptin III (rat) can be used for research of chronic renal failure .
|
-
- HY-P1090A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin(rat) TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin(rat) TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin(rat) TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-P10977
-
|
|
Sodium Channel
RIP kinase
|
Neurological Disease
|
|
Tat-ASIC1a (1-20) (mouse, rat) is a competitive ASIC1a membrane-penetrating peptide. Tat-ASIC1a (1-20) (mouse, rat) has significantly neuroprotection effects, and reduces neuronal damage against acidotoxicity by targeting the ASIC1a-RIPK1 pathway and auto-inhibitory mechanism. Tat-ASIC1a (1-20) (mouse, rat) effectively protects brains from ischemic injury in ischemic stroke mice model. Tat-ASIC1a (1-20) (mouse, rat) can be used for neurodegenerative diseases research, such as Huntington disease and Parkinson’s disease .
|
-
- HY-P1091A
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
Hemopressin TFA is a nonapeptide derived from the α1-chain of hemoglobin, is originally isolated from rat brain homogenates. Hemopressin TFA is orally active, selective and inverse agonist of CB1 cannabinoid receptors. Hemopressin TFA exerts antinociceptive action in inflammatory pain models .
|
-
- HY-P3355
-
|
|
iGluR
|
Neurological Disease
|
|
p-fin4 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 0.4 μM. p-fin4 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p-fin4 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-P5874
-
|
|
Calcium Channel
|
Inflammation/Immunology
|
|
Myr-TAT-CBD3 is CRMP2-CaV2.2 interaction inhibitor. Myr-tat-CBD3 can significantly attenuate carrageenan-induced thermal hypersensitivity and reverse thermal hypersensitivity induced in a rat model of postoperative pain. Myr-TAT-CBD3 can be used to study inflammation and postoperative pain .
|
-
- HY-P3354
-
|
|
iGluR
|
Neurological Disease
|
|
p3Ysh-3 is a peptide inhibitor of STEP Phosphatase-GluA2 AMPA receptor interaction with a Ki of 1.09 μM. p3Ysh-3 restores the memory deficits and displays anxiolytic and antidepressant effects in a scopolamine-treated rat model. p3Ysh-3 is a promising lead compound for novel cognitive enhancers and/or behavioral modulators .
|
-
- HY-P11259
-
|
|
Urotensin Receptor
|
Cardiovascular Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
UPG-111 is a peptide compound that acts as a negative allosteric modulator of the Urotensin II receptor (UTR). UPG-111 exhibits a dual inhibitory effect on the vasoconstriction induced by UTR agonists - it reduces both the maximum response intensity and the sensitivity of the agonist. UPG-111 does not induce calcium release or cause contraction of the endothelium-deprived rat aortic rings. UPG-111 can be used for the study of various diseases related to the angiotensinergic system .
|
-
- HY-P11584
-
|
|
Amylin Receptor
CGRP Receptor
|
Metabolic Disease
|
|
KBP-066A is a long-acting dual amylin and calcitonin receptor agonist. KBP-066A can activate the CTR and AMY-R potently, with no off-target activity. KBP-066A reduces fasting blood glucose levels, fasting insulin levels, and body weight in diabetic rat models. KBP-066A can be used for the research of type 2 diabetes mellitus, obesity .
|
-
- HY-P4096C
-
|
|
Peptides
|
Inflammation/Immunology
|
|
Cys-scHAP-1 is an N-terminal cysteine-labeled disordered peptide of HAP-1. Cys-scHAP-1 can be used to construct scHAP-1-targeted liposomes, which bind to human and rabbit fibroblast-like synoviocytes and localize to inflamed joints in vivo in a rat adjuvant-induced arthritis model. Cys-scHAP-1 is applicable to arthritis research .
|
-
- HY-P11480
-
|
|
Trk Receptor
|
Neurological Disease
|
|
TrkA/NGF-IN-1 (Peptide 19) is an inhibitor of protein-protein interactions between TrkA and NGF (IC50: 21 nM for human TrkA in PathHunter assay). TrkA/NGF-IN-1 shows an analgesic effect in a rat incisional pain model .
|
-
- HY-P11399
-
|
|
Bacterial
Fungal
|
Infection
|
|
Tachyplesin-3 is a broad-spectrum cationic antimicrobial peptide. Tachyplesin-3 has inhibitory activity against Gram-positive bacteria, Gram-negative bacteria, fungi and enveloped viruses. Tachyplesin-3 binds to bacterial membrane lipopolysaccharides through positive charges, disrupting membrane integrity and causing leakage of cellular contents. Tachyplesin-3 interferes with bacterial adhesion and aggregation, prevents biofilm formation, and has a synergistic effect when used in combination with Piperacillin (HY-B1923) - Tazobactam (HY-B1418) (TZP) .
|
-
- HY-175824
-
|
|
iGluR
NO Synthase
Apoptosis
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke .
|
-
- HY-P4096A
-
|
|
Peptides
|
Inflammation/Immunology
|
|
Cys-HAP-1 is a synovium-homing peptide that specifically binds to human and rabbit fibroblast-like synoviocytes, and does not bind to human umbilical vein endothelial cells regardless of TNF-α treatment. Cys-HAP-1 enables targeted drug delivery to inflamed joints after conjugation with liposomes loaded with anti-arthritic agents. Cys-HAP-1 can be used in studies related to adjuvant arthritis .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P990117
-
|
|
Integrin
|
Cardiovascular Disease
Cancer
|
|
Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) is a mouse-derived Osteopontin/SPP1 IgG1 κ type antibody inhibitor. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) blocks Angiotensin II (HY-13948)-induced DNA synthesis and collagen gel contraction in cardiac fibroblasts. Anti-Mouse/Rat/Human Osteopontin/SPP1 Antibody (MPIIIB10) significantly inhibits tumor growth in CT26 or MC38 tumors mice models .
|
-
(5)
-
- HY-P990148
-
|
|
VEGFR
|
Cancer
|
|
Anti-Mouse VEGF-A Antibody (2G11-2A05) is a rat-derived IgG2a κ type antibody inhibitor, tragrting to mouse VEGF-A with high affinity. Anti-Mouse VEGF-A Antibody (2G11-2A05) shows good anti-tumor effect in gastric cancer xenograft models .
|
-
(5)
-
- HY-P990792
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
|
Anti-Mouse CD4 Antibody (GK1.5) is an anti-mouse CD4 IgG2b monoclonal antibody. Anti-Mouse CD4 Antibody (GK1.5) can significantly deplete CD4 + T cells. Anti-Mouse CD4 Antibody (GK1.5) can extend the survival rate of xenograft models. Anti-Mouse CD4 Antibody (GK1.5) can be used for research on immunology. The recommend isotype control of Anti-Mouse CD4 Antibody (GK1.5): Rat IgG2b kappa, Isotype Control (HY-P990682) .
|
-
(5)
-
- HY-P99171
-
|
|
Interleukin Related
|
Inflammation/Immunology
Cancer
|
|
Gevokizumab is a potent anti-IL-1β antibody, negatively modulates IL-1β signaling through an allosteric mechanism. Gevokizumab selectively decreases the binding affinity of IL-1β for the IL-1 receptor type I (IL-1RI) signaling receptor instead of IL-1 counter-regulatory decoy receptor (IL-1 receptor type II) .
|
-
(5)
-
- HY-P99124
-
|
|
CD3
|
Inflammation/Immunology
|
|
Anti-Mouse CD3 Antibody (17A2) is an anti-mouse CD3 IgG2b antibody inhibitor derived from the host Rat. Anti-Mouse CD3 Antibody (17A2) enhances T-cell proliferation and activation and stimulate IFN-γ or IL-17 production in splenic T cells. Anti-Mouse CD3 Antibody (17A2) significantly suppresses mortality in Graft-versus-host disease (GVHD) mice models .
|
-
(5)
-
- HY-P990302
-
|
|
nAChR
|
Neurological Disease
|
|
Anti-Human/Rat/Fish AChR Antibody (Mab35) is an anti-human/rat/fish AChR IgG1 monoclonal antibody. Anti-Human/Rat/Fish AChR Antibody (Mab35) can attack the AChR of neuromuscular junctions. Anti-Human/Rat/Fish AChR Antibody (Mab35) can be used for the construction of myasthenia gravis models .
|
-
(5)
-
- HY-P990107
-
|
|
TGF-β Receptor
|
Cancer
|
|
Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) is an TGF-β IgG antibody inhibitor. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) reduces renal fibrosis in unilateral ureteral obstruction (UUO) mice models. Anti-Mouse/Human/Rat/Monkey/Hamster/Canine/Bovine TGF-β Antibody (1D11.16.8) shows potent anti-tumor effect in various tumor models, such as pancreatic cancer .
|
-
(5)
-
- HY-P990257
-
|
|
c-Fms
|
Cancer
|
|
Anti-Mouse CSF1 Antibody (5A1) is a rat-derived anti-mouse CSF1 IgG1 κ type antibody inhibitor. Anti-Mouse CSF1 Antibody (5A1) can inhibit cells proliferation and macrophage-induced invasion. Anti-Mouse CSF1 Antibody (5A1) shows potent anti-tumor effect in various tumor models, such as neuroblastoma .
|
-
(5)
-
- HY-P990264
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
|
|
Anti-Mouse CD70 Antibody (FR70) is a rat-derived ant-mouse CD70 IgG2b κ type antibody inhibitor. Anti-Mouse CD70 Antibody (FR70) decreases CD4 +, CD8 + T cells and eosinophils. Anti-Mouse CD70 Antibody (FR70) shows potent anti-inflammatory and anti-immune effects on allergic lung inflammation and cardiac transplant mice models .
|
-
(5)
-
- HY-P990259
-
|
|
Transmembrane Glycoprotein
|
Inflammation/Immunology
Cancer
|
|
Anti-Mouse CD96 Antibody (3.3) is a rat-derived anti-mouse CD96 IgG1 λ type antibody inhibitor. Anti-Mouse CD96 Antibody (3.3) blocks binding of CD155 to CD96. Anti-Mouse CD96 Antibody (3.3) can enhance the antitumor efficacy of multiple immune-checkpoint inhibitors. Anti-Mouse CD96 Antibody (3.3) shows potent anti-tumor and anti-metastatic activity in various tumor models. Anti-Mouse CD96 Antibody (3.3) can be used for the researches of cancer and inflammation, such as mammary carcinoma .
|
-
(5)
-
- HY-P992082
-
|
|
VEGFR
|
Cancer
|
|
Anti-Human/Rat VEGF Antibody (A.4.6.1) is an antibody targeting human and rat vascular endothelial growth factor (VEGF) that potently inhibits tumor growth in various animal models. Anti-Human/Rat VEGF Antibody (A.4.6.1) is the parent antibody of Bevacizumab (HY-P9906), and it exhibits high affinity and high selectivity for binding to human VEGF . The isotype control for Anti-Human/Rat VEGF Antibody (A.4.6.1) is Mouse IgG1 kappa, Isotype Control (HY-P99977).
|
-
(5)
-
- HY-P991982
-
|
|
ADC Antibody
|
Cancer
|
|
ZV0201 Antibody (ZV02) is a monoclonal antibody inhibitor targeting Her2. ZV0201 Antibody can be used to synthesize the antibody-drug conjugate (ADC) ZV0201. ZV0201 Antibody can be used to research related to HER2-positive tumors .
|
-
(5)
-
- HY-P991937
-
|
|
Lipase
|
Inflammation/Immunology
|
|
SOL-116 is a humanized anti-BSSL antibody. SOL-116 blocks BSSL from binding to monocytes. SOL-116 reduces the severity of Pristane (HY-N7819)-induced arthritis in rats .
|
-
(5)
-
- HY-P992410
-
|
|
PAI-1
TGF-beta/Smad
|
Inflammation/Immunology
|
|
MEDI-579 is a fully human monoclonal antibody against PAI-1, with a KD value of 6 pM for human PAI-1 and 105 pM for rat PAI-1. MEDI-579 restores renal plasmin activity and inhibits PAI-1-mediated intracellular signal transduction. MEDI-579 reduces albuminuria, glomerulosclerosis severity, TGF-β1 expression level, and phosphorylated Smad2 level induced in diabetic mice. MEDI-579 decreases the levels of active PAI-1 in plasma and kidneys, and increases plasma plasmin level in a mouse model of lupus nephritis. MEDI-579 can be used in research related to diabetic nephropathy and lupus nephritis. The recommended isotype control is human IgG1 kappa (HY-P99001) .
|
-
(5)
-
- HY-P992098
-
|
NEI-01
|
Protein Arginine Deiminase
|
Cancer
|
|
Adargiminase (NEI-01) is a modified arginine-depleting enzyme and albumin binder. Adargiminase catalyzes the conversion of arginine to citrulline and ammonia, reduces plasma arginine levels to undetectable levels, and binds to serum albumin from Mus musculus (mouse), Rattus norvegicus (rat), Canis lupus familiaris (dog) and Homo sapiens (human) to extend its half-life. Adargiminase inhibits the viability of ASS1-negative pancreatic cancer cells, and reduces tumor volume and weight. Adargiminase can be used for the research of pancreatic cancer .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-B0470
-
-
-
- HY-N0194
-
-
-
- HY-N2493
-
-
-
- HY-N0265
-
-
-
- HY-N0321
-
-
-
- HY-119580
-
-
-
- HY-N2995
-
-
-
- HY-Y0546
-
|
|
Structural Classification
Microorganisms
Classification of Application Fields
Ketones, Aldehydes, Acids
Metabolic Disease
Endogenous metabolite
Disease Research Fields
Source Classification
|
Environmental Pollutants
Endogenous Metabolite
Photosensitizer
|
|
Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
|
-
-
- HY-B0199A
-
|
RS 61443 hydrochloride; TM-MMF hydrochloride
|
Structural Classification
Monophenols
Classification of Application Fields
Phenols
Endogenous metabolite
Disease Research Fields
Source Classification
Cancer
|
Interleukin Related
|
|
Mycophenolate mofetil (RS 61443; TM-MMF) hydrochloride is an orally active antimetabolic immunosuppressant with antiproliferative and anti-inflammatory properties. Mycophenolate mofetil hydrochloride significantly inhibits the production of B, T lymphocytes and the proliferation of smooth muscle cells by selectively blocking the de novo purine synthesis pathway. Mycophenolate mofetil hydrochloride effectively reduces adventitial inflammation, medial necrosis and intimal thickening in rat aortic allografts, and decreases the number of lymphocytes expressing the IL-2 receptor, thereby delaying xenograft rejection. Mycophenolate mofetil hydrochloride shows certain toxicity in a hamster-to-rat limb xenotransplantation model when used in combination with FK506 (HY-13756). Mycophenolate mofetil hydrochloride is widely used in studies related to allograft arteriosclerosis (chronic rejection) .
|
-
-
- HY-113427
-
-
-
- HY-B1350A
-
-
-
- HY-W008270
-
-
-
- HY-N0430
-
|
Coptisin
|
Alkaloids
Structural Classification
Classification of Application Fields
Coptis chinensis Franch.
Ranunculaceae
Metabolic Disease
Quinoline Alkaloids
Plants
Disease Research Fields
Source Classification
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
|
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
|
-
-
- HY-N0665
-
-
-
- HY-N3847
-
|
Eriodictyol 7-O-β-D-glucoside
|
Flavonoids
Classification of Application Fields
Labiatae
Flavonones
Phenols
Polyphenols
Metabolic Disease
Plants
Disease Research Fields
Petalostemun purpureum
Source Classification
|
Keap1-Nrf2
|
|
Eriodictyol-7-O-glucoside (Eriodictyol 7-O-β-D-glucoside), a flavonoid, is an Nrf2 activator. Eriodictyol-7-O-glucoside exhibits significant scavenging effects on both hydroxyl radicals and superoxide anions, with IC50 values of 0.28 mM and 0.30 mM, respectively. Eriodictyol-7-O-glucoside increases the nuclear localization of Nrf2 and induces the expression of the Nrf2/ARE-dependent genes. Eriodictyol-7-O-glucoside provides protection against oxygen and glucose deprivation (OGD)-induced oxidative insult. Eriodictyol-7-O-glucoside demonstrates neuroprotective efficacy in a rat model of focal cerebral ischemia (MCAO). Eriodictyol-7-O-glucoside can be used for the study of stroke .
|
-
-
- HY-116514
-
-
-
- HY-N8698
-
Picein
1 Publications Verification
|
Nyssaceae
Plants
Saccharides
Source Classification
|
SOD
Ferroptosis
Keap1-Nrf2
Heme Oxygenase (HO)
Glutathione Peroxidase
|
|
Picein is an antioxidant and anti-inflammatory agent. Picein can be isolated from the leaves of Picrorhiza kurroa. Picein reduces MDA levels and increases the levels of SOD, GPX and TAC. Picein alleviates oxidative stress and promotes bone regeneration in osteoporotic bone defects by inhibiting Ferroptosis (via activation of the Nrf2/HO-1/GPX4 pathway). Picein prevents scopolamine (HY-N0296)-induced passive avoidance memory impairment in rats. Picein can be used in research related to osteoporotic bone defects and Alzheimer's disease .
|
-
-
- HY-W089800
-
|
trans-2-Nonen-1-al
|
Source Classification
|
COX
Lipoxygenase
Apoptosis
|
|
trans-2-Nonenal (trans-2-Nonen-1-al) is an endogenous peroxidation product of polyunsaturated fatty acids, acting as an inhibitor of COX and 12-LOX, as well as an inducer of apoptosis. trans-2-Nonenal is also a malodorous compound secreted by the human body, and its content gradually increases with aging. trans-2-Nonenal inhibits the activities of multiple enzymes such as platelet membrane-bound PTPase, preferentially covalently modifies proteins at lysine residues to form immunogenic adducts, and regulates platelet Arachidonic acid (HY-109590) metabolism. trans-2-Nonenal also exhibits significant cytotoxicity, reduces the viability of keratinocytes, promotes their apoptosis, and effectively decreases the thickness of epidermal models and the number of proliferating cells. trans-2-Nonenal is commonly used in studies of thrombotic, atherosclerotic diseases, renal adenocarcinoma, etc. .
|
-
-
- HY-N0430A
-
|
|
Alkaloids
Structural Classification
Chelidonium majus
Classification of Application Fields
Metabolic Disease
Quinoline Alkaloids
Plants
Disease Research Fields
Papaveraceae
Source Classification
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
|
Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
|
-
-
- HY-N3710
-
-
-
- HY-N4107
-
-
-
- HY-N8249
-
-
-
- HY-W015815
-
-
-
- HY-N0194R
-
|
|
Triterpenes
Structural Classification
Terpenoids
Centella asiatica (L.) Urb.
Umbelliferae
Plants
Source Classification
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Reference Standards
Apoptosis
Parasite
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Asiatic acid (Standard) is the analytical standard of Asiatic acid. This product is intended for research and analytical applications. Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
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- HY-B1341
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Enidrel; SC-4642; NSC 15432
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Structural Classification
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Endocrinology
Steroids
Source Classification
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Endogenous Metabolite
Progesterone Receptor
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Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
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- HY-B0199R
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RS 61443 (Standard); TM-MMF (Standard)
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Structural Classification
Monophenols
Phenols
Endogenous metabolite
Source Classification
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Reference Standards
Interleukin Related
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Mycophenolate Mofetil (Standard) is the analytical standard of Mycophenolate Mofetil. This product is intended for research and analytical applications. Mycophenolate mofetil (RS 61443; TM-MMF) hydrochloride is an orally active antimetabolic immunosuppressant with antiproliferative and anti-inflammatory properties. Mycophenolate mofetil hydrochloride significantly inhibits the production of B, T lymphocytes and the proliferation of smooth muscle cells by selectively blocking the de novo purine synthesis pathway. Mycophenolate mofetil hydrochloride effectively reduces adventitial inflammation, medial necrosis and intimal thickening in rat aortic allografts, and decreases the number of lymphocytes expressing the IL-2 receptor, thereby delaying xenograft rejection. Mycophenolate mofetil hydrochloride shows certain toxicity in a hamster-to-rat limb xenotransplantation model when used in combination with FK506 (HY-13756). Mycophenolate mofetil hydrochloride is widely used in studies related to allograft arteriosclerosis (chronic rejection) .
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- HY-N14827
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- HY-W015815R
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Alkaloids
Pyridine Alkaloids
Endogenous metabolite
Source Classification
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Reference Standards
Endogenous Metabolite
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6-Methylnicotinamide is a nicotinamide derivative. 6-methylnicotinamide is also an endogenous metabolite and its sudden increase in the acute stages of intracerebral hemorrhage (ICH) exacerbates neurological damages in rat model. 6-Methylnicotinamide can significantly enhance the coordination effect between acylamino and undercoordinated defective Pb2+ cations. 6-Methylnicotinamide results in enhanced efficiency of perovskite solar cells to 24.33% with excellent environmental storage, heat, and light stabilities .
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- HY-N2493R
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- HY-W587784
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Bixaceae
Bixa orellana Linn.
Ketones, Aldehydes, Acids
Plants
Source Classification
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PPAR
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Norbixin is a carotenoid that has been found in B. orellana.It binds to PPARγ in a cell-free assay (Ki = 1.15 μM) . Norbixin attenuates hyperglycemia, hyperinsulinemia, and insulin resistance, as well as decreases serum lipid levels and cardiac levels of thiobarbituric acid reactive substances (TBARS) and glutathione (GSH) in a rat model of cardio-metabolic syndrome .
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- HY-N9737
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- HY-N14176
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- HY-138063
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- HY-119821R
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Structural Classification
Microorganisms
Phenols
Polyphenols
Source Classification
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Reference Standards
Glycosidase
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Thiamiprine (Standard) is the analytical standard of Thiamiprine. This product is intended for research and analytical applications. Thiamiprine (BW 57-323) is a compound related to azathioprine. Its nucleoside forms are similar to the parent compound in terms of cytotoxicity in vitro (except for the arabinoside). In the rat adjuvant arthritis model in vivo, its riboside and 2'-deoxyriboside are less active than the parent compound. The arabinoside is inactive and nontoxic. It has similar potency to the other parent compounds tested, but has a different safety profile.
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- HY-N0665R
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- HY-113427R
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- HY-Y0546R
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Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Endogenous metabolite
Source Classification
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Reference Standards
Endogenous Metabolite
Photosensitizer
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Benzophenone (Standard) is the analytical standard of Benzophenone. This product is intended for research and analytical applications. Benzophenone standard is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone standard can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone standard can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone standard exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone standard exhibits estrogenic activity .
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- HY-N4107R
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- HY-W008270R
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γ-Crotonolactone (Standard)
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Structural Classification
Natural Products
Endogenous metabolite
Source Classification
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Reference Standards
Endogenous Metabolite
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2(5H)-Furanone (Standard) is the analytical standard of 2(5H)-Furanone. This product is intended for research and analytical applications. 2(5H)-Furanone (γ-Crotonolactone) is an endogenous metabolite. 2(5H)-Furanone mimics N-acyl homoserine lactone signals, occupies the binding site of LuxR homologs, and interferes with quorum sensing-mediated gene regulation. 2(5H)-Furanone inhibits quorum sensing mediated by AHLs with different acyl chain lengths. 2(5H)-Furanone inhibits biofilm formation of environmental Aeromonas hydrophila strains on polystyrene plates. 2(5H)-Furanone suppresses spike-and-wave discharges in a rat model of generalized absence seizures and exhibits selective activity against absence seizures. 2(5H)-Furanone can be used in studies related to bacteria infections and generalized absence seizures.
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- HY-N15378
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Structural Classification
Natural Products
Spondias mombin L.
Plants
Anacardiaceae
Source Classification
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IAP
Bcl-2 Family
COX
TNF Receptor
Caspase
Apoptosis
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β-carotene-15,15ʹ-epoxide is a XIAP antagonist with apoptosis-inducing and antitumor activity, found in the leaves of Spondias mombin. In a DMBA (HY-W011845)-induced rat model of breast cancer, β-carotene-15,15ʹ-epoxide binds to the BIR3 domain of the anti-apoptotic protein XIAP, blocking its interaction with caspase-9 and thereby promoting tumor cell apoptosis. In addition, β-carotene-15,15ʹ-epoxide significantly downregulates the expression of BCL-2, COX-2, and TNF-α in tumor tissues, reduces MDA levels, increases catalase activity, and modulates serum levels of LDH, ALP, and ALT, demonstrating strong antioxidant, anti-inflammatory, and metabolic protective effects. β-carotene-15,15ʹ-epoxide may be used in research on inflammation-related conditions and cancers such as breast cancer .
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- HY-N14177
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- HY-N17737
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-Y0546S
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Benzophenone-d10 is the deuterium labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
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- HY-B0199S
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Mycophenolate Mofetil-d4 is the deuterium labeled Mycophenolate Mofetil. Mycophenolate mofetil (RS 61443; TM-MMF) hydrochloride is an orally active antimetabolic immunosuppressant with antiproliferative and anti-inflammatory properties. Mycophenolate mofetil hydrochloride significantly inhibits the production of B, T lymphocytes and the proliferation of smooth muscle cells by selectively blocking the de novo purine synthesis pathway. Mycophenolate mofetil hydrochloride effectively reduces adventitial inflammation, medial necrosis and intimal thickening in rat aortic allografts, and decreases the number of lymphocytes expressing the IL-2 receptor, thereby delaying xenograft rejection. Mycophenolate mofetil hydrochloride shows certain toxicity in a hamster-to-rat limb xenotransplantation model when used in combination with FK506 (HY-13756). Mycophenolate mofetil hydrochloride is widely used in studies related to allograft arteriosclerosis (chronic rejection) .
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- HY-W747491
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Triclosan- 13C12 is 13C labeled Triclosan (HY-B1119). Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 μM and 10 μM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
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- HY-Y0546S2
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Benzophenone- 13C is the 13C labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
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- HY-W653962
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Triclosan- 13C6 is 13C labeled Triclosan. Triclosan is a broad-spectrum antibacterial agent that inhibits bacterial fatty acid synthesis at the enoyl-acyl carrier protein reductase (FabI) step. Triclosan inhibits E. coli enoyl-acyl carrier protein reductase (FabI) and FabI containing a glycine-to-valine substitution at position 93 (FabIG93V) with IC50s of 2 μM and 10 μM, respectively. Triclosan causes apoptotic effect in cultured rat neural stem cells (NSC). Triclosan exacerbates colitis and colitis-associated colorectal tumorigenesis in animal models .
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- HY-169332
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Piezo1 agonist 1-d2 is a Piezo1 agonist and osteogenesis promoter with an EC50 of 2.21 μM. Piezo1 agonist 1-d2 activates Piezo1 and induces calcium ion influx in mesenchymal stem cells. Piezo1 agonist 1-d2 activates the Erk signaling pathway and promotes osteogenesis of mesenchymal stem cells. Piezo1 agonist 1-d2 alleviates disuse osteoporosis in a hindlimb unloading rat model. Piezo1 agonist 1-d2 can be used for research on osteoporosis .
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- HY-B0712S1
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Ceftriaxone-13C2,d3 triethylammonium salt is 13C and deuterated labeled Ceftriaxone (HY-B0712). Ceftriaxone (Ro 13-9904 free acid) is a broad spectrum β-lactam third-generation cephalosporin antibiotic, which has good antibacterial activity against a variety of gram-negative and positive bacteria. Ceftriaxone is a covalent inhibitor of GSK3β with IC50 value of 0.78 mM. Ceftriaxone is an inhibitor of Aurora B. Ceftriaxone has anti-inflammatory, antitumor and antioxidant activities. Ceftriaxone can be used in the study of bacterial infections and meningitis .
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- HY-113427S
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trans-Vaccenic acid-d13 is deuterium labeled trans-Vaccenic acid (HY-113427). trans-Vaccenic acid is a naturally occurring trans fatty acid (TFA). trans-Vaccenic acid inhibits nasopharyngeal carcinoma (NPC) cell growth and induces apoptosis through the inhibition of Bad/Akt phosphorylation. trans-Vaccenic acid is a precursor for the synthesis of saturated fatty acid in the rumen and of conjugated Linoleic acid (CLA) at the tissue level. trans-Vaccenic acid exerts hypolipidemic effects in a rat model of obesity .
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- HY-175318S
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p53 Activator 15 is an orally active p53 Y220C activator. p53 Activator 15 enhances the DNA binding of p53 Y220C (SC50 = 0.58 nM) and significantly inhibits NUGC-3 cell proliferation. p53 Activator 15 effectively inhibits tumor growth in NUGC-3 xenograft mouse and rat models. p53 Activator 15 can be used to study gastric cancer .
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- HY-B0199AS
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Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443; TM-MMF) hydrochloride is an orally active antimetabolic immunosuppressant with antiproliferative and anti-inflammatory properties. Mycophenolate mofetil hydrochloride significantly inhibits the production of B, T lymphocytes and the proliferation of smooth muscle cells by selectively blocking the de novo purine synthesis pathway. Mycophenolate mofetil hydrochloride effectively reduces adventitial inflammation, medial necrosis and intimal thickening in rat aortic allografts, and decreases the number of lymphocytes expressing the IL-2 receptor, thereby delaying xenograft rejection. Mycophenolate mofetil hydrochloride shows certain toxicity in a hamster-to-rat limb xenotransplantation model when used in combination with FK506 (HY-13756). Mycophenolate mofetil hydrochloride is widely used in studies related to allograft arteriosclerosis (chronic rejection) .
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- HY-134160S
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5,6-Dihydro-5-Fluorouracil- 13C, 15N2 (5-DHFU- 13C, 15N2) is the 13C- and 15N-labeled labeled 5,6-Dihydro-5-Fluorouracil (HY-134160). 5,6-Dihydro-5-Fluorouracil (5-DHFU; 5-Fluorodihydropyrimidine-2,4-dione) is the active metabolite of the thymidylate synthase inhibitor prodrug 5-fluorouracil (HY-90006), which is formed from 5-fluorouracil by dihydropyrimidine dehydrogenase (DPD). 5,6-Dihydro-5-Fluorouracil is cytotoxic to HaCaT keratinocytes (IC50=13.5 μM). Intravenous administration of 5,6-Dihydro-5-Fluorouracil (90 mg/kg/wk) in combination with 5-fluorouracil and the DPD inhibitor eniluracil (HY-10533) slows tumor growth in a rat colon cancer model.
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- HY-13762S
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Tesmilifene-d4 is the deuterium labeled Tesmilifene (HY-13762). Tesmilifene is an antihistamine agent and a chemical sensitizer. Tesmilifene targets cytochrome P450, exhibits hormonal effects on DNA synthesis in MCF-7 cells, and stimulates the tumor growth in mouse/rat models. Tesmilifene overcomes multidrug resistance .
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- HY-W747879
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Diclofenac Amide- 13C6 is the 13C-labeled Diclofenac amide (HY-134521). Diclofenac amide is a prodrug for Diclofenac sodium (HY-15037). Diclofenac amide is an orally active inhibitor for COX-1/2, that inhibits the production of prostaglandins (PG) and thromboxanes (TX). Diclofenac amide exhibits anti-inflammatory efficacy in Carrageenan (HY-125474)-induced rat paw edema model without causing gastric ulcer (300 μmol/kg) .
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- HY-B0130S1
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Perindopril-d5 (S-9490-d5) is deuterium labeled Perindopril. Perindopril (S-9490) is an orally available, long-acting angiotensin-converting enzyme (ACE) inhibitor. Perindopril inhibits inflammatory cell influx and intimal thickening, preserving elastin on the inside of the aorta. Perindopril effectively inhibits experimental abdominal aortic aneurysm (AAA) formation in a rat model and reduces pulmonary vasoconstriction in rats with pulmonary hypertension .
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- HY-Y0546S1
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Benzophenone-d5 is the deuterium labeled Benzophenone (HY-Y0546). Benzophenone is an endogenous metabolite. Benzophenone is a photosensitizer, that absorbs UV light, transfers its energy to DNA, and triggers DNA damage. Benzophenone can be used as the fragrance enhancer, ultraviolet curing agent, additive in plastics, or the flavor ingredient. Benzophenone can also be used in the manufacturing of insecticides, agricultural chemicals, hypnotics, antihistamines, and other pharmaceuticals. Benzophenone exhibits certain carcinogenicity in mouse/rat models under long term exposure. Benzophenone exhibits estrogenic activity .
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- HY-W013403S
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2'-Deoxy-2'-fluorouridine-d2 is the deuterium labeled 2'-Deoxy-2'-fluorouridine . 2'-Deoxy-2'-fluorouridine is a derivative of the pyrimidine nucleoside uridine. 2'-Deoxy-2'-fluorouridine is a nucleoside analog that inhibits the replication of wild-type viruses by binding to the viral RNA. Hepatitis C polyU/UC RNA strands containing 2'-Deoxy-2'-fluorouridine, bind to RIG-I but do not activate RIG-I signaling in a reporter assay using Huh7 cells. 2'-Deoxy-2'-fluorouridine also has been used as a starting material in the synthesis of respiratory syncytial virus (RSV) polymerase inhibitors. 2'-Deoxy-2'-fluorouridine can incorporate into DNA and RNA in rat and woodchuck model upon administration. 2'-Deoxy-2'-fluorouridine can be studied in anti-viral research .
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- HY-19337S1
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Ketodarolutamide-d6 (BAY 1896953-d6) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
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- HY-19337S
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Ketodarolutamide-d3 (BAY 1896953-d3) is the deuterium labeled Ketodarolutamide (HY-19337). Ketodarolutamide (ORM-15341) is a potent, high-affinity nonsteroidal competitive full antagonist of androgen receptor (AR). Ketodarolutamide displays a Ki value of 8 nM for rat wild-type AR and an IC50 value of 38 nM in AR-HEK293 cells . Ketodarolutamide inhibits testosterone-induced nuclear translocation of the AR and antagonizes both overexpressed and mutant ARs . Ketodarolutamide specifically suppresses the proliferation of AR-dependent prostate cancer cells and exhibits antitumor activity in models of castration-resistant prostate cancer (CRPC) . Ketodarolutamide is suitable for the mechanistic and therapeutic research of prostate cancer .
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- HY-B0742S1
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Hydroxyprogesterone caproate-d8 (17α-Hydroxyprogesterone hexanoate-d8) is the deuterium labeled Hydroxyprogesterone caproate (HY-B0742). Hydroxyprogesterone caproate (17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate) is a progesterone receptor (progesterone receptor) ligand and steroid hormone transcription inhibitor. Hydroxyprogesterone caproate downregulates estrogen receptors in target tissues and activates their metabolic pathways, and exhibits equivalent affinity for progesterone receptor A and progesterone receptor B. Hydroxyprogesterone caproate shows no consistent teratogenicity or developmental toxicity in rat, mouse and monkey models, but induces resorption or abortion in rhesus monkeys at human-equivalent doses. Hydroxyprogesterone caproate promotes the production of TNF-α in lipopolysaccharide-stimulated whole blood from non-pregnant women. Hydroxyprogesterone caproate can be used in scientific research related to preterm birth .
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| Cat. No. |
Product Name |
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Classification |
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- HY-B1341
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Enidrel; SC-4642; NSC 15432
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Alkynes
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Norethynodrel (Enidrel; SC-4642) is an orally active progestogen analog that reduces estrogen-like effects and enhances progestogen-like responses in endometrial stromal cells. Norethynodrel also promotes cell maturation and predecidual cell formation by inducing organelle hyperplasia and glycogen accumulation. Norethynodrel competitively inhibits drug-metabolizing enzymes in rat liver microsomes, thereby prolonging Pentobarbital sleep time, while exhibiting multiple effects including reduced body weight gain, attenuated heart rate elevation and ovulation inhibition. In mouse models, Norethynodrel significantly increases the incidence of mammary adenocarcinoma, cervical cancer and pituitary tumors. Norethynodrel can be used for mechanism research on related diseases such as mammary adenocarcinoma, cervical cancer, ovarian tubular adenoma and pituitary adenoma .
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- HY-14318
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SIB-1508Y free base
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Alkynes
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Altinicline (SIB-1508Y free base) is a selective α4β2 nicotinic acetylcholine receptor (nAChR) agonist, with no activity against α7 or α1β1γδ nAChRs and only extremely low activity against α3β4 nAChRs. Altinicline reverses escape deficits and increases avoidance responses. Altinicline is applicable to research related to depression .
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| Cat. No. |
Product Name |
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Classification |
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- HY-132610A
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ALN-AS1 sodium
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siRNAs
siRNA drugs
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Givosiran (ALN-AS1) sodium is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran sodium downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran sodium demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran sodium can be used for the research of acute hepatic porphyria (AHP) .
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- HY-132610
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ALN-AS1
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siRNAs
siRNA drugs
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Givosiran (ALN-AS1) is a small interfering RNA that targets hepatic aminolevulinate synthase 1 (ALAS1) messenger RNA. Givosiran downregulates ALAS1 mRNA and prevents accumulation of neurotoxic δ-aminolevulinic acid (ALA) and porphobilinogen (PBG) levels. Givosiran demonstrates potent inhibitory activity against ALAS1 in mouse, rat, and cynomolgus monkey models. Givosiran can be used for the research of acute hepatic porphyria (AHP) .
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