Search Result
Results for "
Sprague-Dawley rat
" in MedChemExpress (MCE) Product Catalog:
5
Biochemical Assay Reagents
| Cat. No. |
상품명 |
Target |
연구분야 |
Chemical Structure |
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- HY-P10587
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JNJ-77242113; JNJ-2113; PN-235
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Interleukin Related
STAT
IFNAR
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Inflammation/Immunology
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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 .
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- HY-P99221
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RN-624; PF 4383119
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Trk Receptor
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Neurological Disease
Inflammation/Immunology
Cancer
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Tanezumab (RN-624) is a humanized anti-NGF mAb with high affinity and specificity. Tanezumab blocks NGF binding to its receptors, p75 and TrkA, in the peripheral nervous system. Tanezumab can be used in studies of acute and chronic pain such as osteoarthritis, knee and neuralgia, as well as post-herpetic neuralgia .
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- HY-N0730
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Autophagy
Apoptosis
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Neurological Disease
Inflammation/Immunology
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Diosgenin glucoside, a saponin compound extracted from Trillium tschonoskii, provides neuroprotection by regulating microglial M1 polarization. Diosgenin glucoside protects against spinal cord injury by regulating autophagy and alleviating apoptosis .
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- HY-P991272
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PF-05230900
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Interleukin Related
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Inflammation/Immunology
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ATR-107 (PF-05230900) is a humanized monoclonal antibody inhibitor that targets the interleukin-21 receptor (IL-21R). The Ka value of ATR-107 is 2-4 nM in cynomolgus monkeys, 16 nM in mice, and 71 nM in rats. ATR-107 can be used in research related to systemic lupus erythematosus and air pouch inflammation .
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- HY-100113
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AT2 receptor agonist C21
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Angiotensin Receptor
p38 MAPK
TGF-beta/Smad
TGF-β Receptor
MMP
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Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
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Buloxibutid (AT2 receptor agonist C21) is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a Ki value of 0.4 nM for porcine AT2R. Buloxibutid exerts effects such as vasodilation, anti-inflammation, anti-fibrosis (promoting the expression of collagenase MMP-13) and tissue repair mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway as well as the inflammatory NF-κB pathway. Buloxibutid can be used in research related to idiopathic pulmonary fibrosis, hypertension, and systemic sclerosis .
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- HY-E70558
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5 alpha Reductase
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Metabolic Disease
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5α-reductase, Rat (Sprague-Dawley) Liver is an enzyme involved in steroid metabolism and participates in the androgen metabolic pathway. 5α-reductase, Rat (Sprague-Dawley) Liver catalyzes the conversion of testosterone to 5α-dihydrotestosterone (DHT). DHT plays important roles in the development of male sex organs, hair growth, prostate function, and other aspects .
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- HY-133668
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Drug Metabolite
Cytochrome P450
PPAR
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Endocrinology
Cancer
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Monoethyl phthalate is an orally active PDX-1 activator and the major hydrolytic metabolite of Diethyl phthalate (HY-Y0284) in vivo, with reproductive toxicity. Monoethyl phthalate targets aromatase (aromatase/CYP19A1) and PPAR to induce cell proliferation. The plasma protein binding rate of Monoethyl phthalate in rats and humans is lower than that of Diethyl phthalate. It exhibits significant enterohepatic circulation in rats and mainly accumulates in liver tissues. Monoethyl phthalate shows no estrogenic activity in estrogen-dependent human breast cancer cells. Monoethyl phthalate can be used in studies of reproductive toxicity and related environmental endocrine disruption mechanisms .
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- HY-142240
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HSK16149
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Calcium Channel
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Neurological Disease
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Crisugabalin is an orally active, selective ligand for the α2δ subunit of voltage-gated calcium channels, with a target IC50 of 3.96 nM in rats. Crisugabalin inhibits the binding of [ 3H]gabapentin to the α2δ subunit, reduces calcium influx, decreases neuronal excitability, and impairs nociceptive transmission. Crisugabalin alleviates mechanical allodynia, neuropathic pain and inflammatory pain in rats, and reduces phase II pain behaviors. Crisugabalin can be used in research related to chronic pain, neuropathic pain, diabetic neuropathy, fibromyalgia, inflammatory pain, diabetic peripheral neuropathy and postherpetic neuralgia.
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- HY-129630
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Microtubule/Tubulin
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Neurological Disease
Cancer
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Tetrahydrocortisol is a cortisol metabolite that inhibits dexamethasone-induced formation of cross-linked actin networks. Tetrahydrocortisol can be used in the research of primary open-angle glaucoma, glucocorticoid-induced ocular hypertension, Lewis lung carcinoma, and EMT-6 mouse breast cancer .
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- HY-W102714
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CDTA
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Biochemical Assay Reagents
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Neurological Disease
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1,2-Cyclohexylenedinitrilotetraacetic acid (CDTA) is a chelating agent. 1,2-Cyclohexylenedinitrilotetraacetic acid has an ability to remove manganese from brain and liver (in vivo) and their sub-cellular fractions (in vitro), of rats pretreated with manganese sulphate .
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- HY-N0493
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COX
Lipoxygenase
NF-κB
p38 MAPK
ERK
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
PI3K
Apoptosis
Autophagy
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Neurological Disease
Inflammation/Immunology
Cancer
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Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma .
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- HY-Y1191
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- HY-113093
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Endogenous Metabolite
Toll-like Receptor (TLR)
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Neurological Disease
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Ethyl glucuronide is an endogenous metabolite. Ethyl glucuronide is the metabolite of ethanol. Ethyl glucuronide is a biomarker for ethanol exposure that accumulates in hair and reflects the alcohol intake over a time period. Ethyl glucuronide is the agonist for TLR4 .
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- HY-B1059
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- HY-160023
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D3S-001
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Ras
PERK
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Cancer
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Elisrasib (D3S-001) is an orally active and selective inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2. D3S-001 also inhibits the phosphorylation of cellular ERK1/2. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
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- HY-118424
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iGluR
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Neurological Disease
Metabolic Disease
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JNJ-55511118 is a selective TARP γ-8 binding AMPA receptor modulator with oral bioavailability and blood-brain barrier permeability, with a Ki of 26 nM. JNJ-55511118 reduces voluntary intake of sweetened alcohol in male mice. In rodent models, JNJ-55511118 inhibits hippocampal neurotransmission, reduces specific electroencephalogram frequency bands, induces transient hyperlocomotion, impairs learning and memory abilities, and exerts anticonvulsant effects. JNJ-55511118 is applicable to research related to alcohol use disorder and seizures .
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- HY-158231
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F127DA
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Integrin
FAK
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Inflammation/Immunology
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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
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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-10704
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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-128749
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Potassium D-glucarate
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Endogenous Metabolite
Apoptosis
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Metabolic Disease
Inflammation/Immunology
Cancer
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D-Glucaric acid potassium (Potassium D-glucarate) is an orally active end product of the D-glucuronic acid pathway in mammals. D-Glucaric acid potassium is present in a variety of fruits and vegetables. D-Glucaric acid potassium has cholesterol-lowering and anti-tumor activities. D-Glucaric acid potassium can inhibit tumor cell proliferation and inflammation, and induce apoptosis .
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- HY-114557
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3,5-Diiodo-L-thyronine
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JNK
NF-κB
Sirtuin
PGC-1α
COX
TGF-β Receptor
Collagen
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Metabolic Disease
Inflammation/Immunology
Endocrinology
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NSC 90469 (3,5-Diiodo-L-thyronine) is an orally active thyroid hormone derivative. NSC 90469 inhibits JNK phosphorylation and NF-κB acetylation, blocks SIRT1 protein expression, induces elevated PGC-1α levels, and stimulates COX activity. NSC 90469 enhances UCP1-mediated thermogenesis, increases hepatic Dio1 activity, inhibits TSH levels and hypothalamic-pituitary-thyroid axis function, enhances lipid metabolism, and regulates energy metabolism via the mitochondrial pathway. NSC 90469 prevents blood glucose reduction, reduces urinary albumin excretion, inhibits renal matrix expansion, decreases TGF-β1 expression, and reduces renal fibronectin and type Ⅳ collagen deposition. NSC 90469 also increases energy expenditure and prevents diet-induced overweight. NSC 90469 can be used in studies related to diabetic nephropathy, hypothyroidism, non-alcoholic fatty liver disease, and diet-induced obesity .
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- HY-171844
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iGluR
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Neurological Disease
Inflammation/Immunology
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CX1739 is an orally active, blood-brain barrier permeable, low-efficacy AMPA-glutamate receptor (AMPAR) potentiator. CX1739 enhances excitatory neurotransmission by potentiating glutamate-induced excitatory currents and promoting in vivo long-term potentiation. CX1739 eliminates amphetamine-induced locomotor activity, reverses opioid-, pentobarbital- and ethanol-induced respiratory depression, and exerts pro-cognitive effects in animals. CX1739 impairs motor function recovery and increases the risk of post-injury complications. CX1739 can be used in research related to attention-deficit/hyperactivity disorder, dementia, respiratory depression and spinal cord injury .
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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-E70558A
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5 alpha Reductase
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Endocrinology
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5α-Reductase, Rat (Sprague-Dawley) Testis is the enzyme responsible for the conversion of testosterone into 5-alpha dihydrotestosterone (DHT), which is a potent androgen involved in male sexual differentiation.5α-reductase enzyme family is comprised of 3 subfamilies and 5 isoenzyme members: 5αR1, 5αR2, 5αR3, GPSN2, and GPSN2L .
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- HY-159062
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Biochemical Assay Reagents
NO Synthase
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Neurological Disease
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Goji Extract is a natural product with anti-aging, antioxidant, and neuroprotective effects. The antioxidant effect of Goji Extract has a positive impact on erectile dysfunction and can be used in research to improve erectile function .
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- HY-123068
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SQ 14551
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Drug Derivative
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Cardiovascular Disease
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Captopril disulfide (SQ 14551) is an orally active disulfide dimer prodrug. Captopril disulfide is metabolized to Captopril and acts as a Bradykinin potentiator. Captopril disulfide enhances the vasodilatory effect of Bradykinin in anesthetized rats and the contractile response of isolated guinea pig ileum to Bradykinin. Captopril disulfide exhibits antihypertensive activity in spontaneously hypertensive rats. Captopril disulfide can be used in hypertension-related research .
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- HY-N2512
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Environmental Pollutants
Endogenous Metabolite
FAAH
Autophagy
Bacterial
Fungal
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Infection
Cancer
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1-Monomyristin acts as an insecticide, enzyme inhibitor, antibacterial and antifungal agent, with an IC50 of 18 μM against rat FAAH and an IC50 of 32 μM against rat MAGL. 1-Monomyristin inhibits 2-oleoylglycerol hydrolysis via MAGL. 1-Monomyristin suppresses the growth of Staphylococcus aureus, Aggregatibacter actinomycetemcomitans and Candida albicans. 1-Monomyristin is lethal to brine shrimp . 1-Monomyristin exhibits marginal cytotoxicity against prostate cancer cells. 1-Monomyristin is applicable to research related to bacterial infections, fungal infections, renal cancer, prostate adenocarcinoma and pancreatic cancer .
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- HY-107581
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MK-1903
1 Publications Verification
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GPR109A
MMP
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Metabolic Disease
Inflammation/Immunology
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MK-1903 is an orally active full agonist of GPR109a/HCAR2, with an EC50 of 12.9 nM. MK-1903 activates antilipolytic and vasodilatory pathways, reduces plasma free fatty acid levels, and induces skin flushing. MK-1903 stimulates the expression of HCAR2 protein and regulates the inflammatory response of microglia. MK-1903 prevents the enhanced firing activity of spinal nociceptive neurons. MK-1903 triggers the release of MMP-9 and the formation of NET. MK-1903 can be used in the research of dyslipidemia and neuroinflammation-based central nervous system diseases .
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- HY-N0909
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20(S)-Notoginsenoside R2; Ginsenoside Ng-R2
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Apoptosis
MEK
ERK
Reactive Oxygen Species (ROS)
Caspase
COX
β-catenin
Src
MDM-2/p53
JAK
STAT
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Notoginsenoside R2 (20(S)-Notoginsenoside R2; Ginsenoside Ng-R2) is an orally active notoginsenoside . Notoginsenoside R2 activates P90RSK and Nrf2 via the MEK1/2-ERK1/2 pathway to inhibit 6-OHDA-induced apoptotic damage in nerve cells. Notoginsenoside R2 upregulates SOX8/β-catenin by reducing miR-27a, thereby suppressing Aβ25-35-induced neuronal apoptosis and inflammatory responses . Notoginsenoside R2 alleviates lipid accumulation and mitochondrial dysfunction in diabetic nephropathy by inhibiting c-Src. Notoginsenoside R2 alleviates hepatic fibrosis by inducing hepatic stellate cell senescence and inhibiting the inflammatory microenvironment via JAK/STAT3 suppression . Notoginsenoside R2 can be used in research related to Parkinson's disease, Alzheimer's disease, diabetic nephropathy and hepatic fibrosis .
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- HY-10716A
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GlyT
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Neurological Disease
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PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research .
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- HY-160959
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nAChR
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Neurological Disease
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AN317 is a selective agonist for α6β2-containing nicotinic acetylcholine receptor (nAChR) with Ki of 6.2 nM and 4.1 nM, for α6/α3β2β3 receptor and α4β2 receptor, respectively. AN317 induces dopamine release in the synaptosomes of the rat striatum, enhances dopaminergic neuronal activity in substantia nigra, and exhibits protective efficacy to rat neurons against dopamine neurotoxin MPP +. AN317 exhibits good pharmacokinetic characteristics in rats. AN317 penetrates the blood-brain barrier (BB) .
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- HY-125539
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Antibiotic
Phosphatase
Fungal
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Infection
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Roridin E is a glucose-6-phosphatase (G6Pase) inhibitor and antibiotic, and is a metabolic byproduct of Roridin A (HY-N9599). Roridin E induces significant oxidative stress, characterized by depletion of glutathione in vivo, induction of hepatic lipid peroxidation, and inhibition of renal superoxide dismutase activity. Roridin E reduces blood glucose levels in rats, but exhibits acute toxicity (which is enhanced when co-administered with linoleic acid (HY-N0729)) and causes hepatotoxicity in male albino mice. Roridin E induces a decrease in total blood protein and increases in the levels of total lipids, γ-glutamyltransferase, alkaline phosphatase, and 5'-nucleotidase. Roridin E can be isolated from molds, and possesses cytostatic and antifungal activities similar to those of Verrucarin A (HY-107426) and Roridin A. Roridin E exhibits in vivo activity in rodents and is commonly used in hepatotoxicity-related studies .
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- HY-N4031
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Anaplastic lymphoma kinase (ALK)
METTL3
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Inflammation/Immunology
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Humantenine is a highly toxic indole alkaloid from Gelsemium elegans (Gardn. & Champ.) Benth. that binds to RNA m6A modification regulatory proteins (ALKBH5, METTL). Humantenine stably binds via hydrogen bonding and hydrophobic interactions and disrupts the m6A methylation level of target genes, thereby impairing the expression of intestinal epithelial cell tight junction and cytoskeleton-related genes, causing intestinal barrier dysfunction and significant intestinal cytotoxicity. The intraperitoneal injection LD50 values of Humantenine are <1 mg/kg in mice, 1.2 mg/kg in male rats and 1.5 mg/kg in female rats, respectively. Species differences exist in the metabolism of Humantenine in human, porcine, goat and rat liver microsomes, and demethylation, dehydrogenation and oxidation occur in liver microsomes .
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- HY-P3641A
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GnRH Receptor
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Neurological Disease
Metabolic Disease
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Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
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- HY-W021450A
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Biochemical Assay Reagents
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Neurological Disease
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DL-Fluorocitric acid barium is a glial cell metabolic inhibitor. DL-Fluorocitric acid barium inhibits mechanical hyperalgesia induced by subcutaneous injection of complete Freund's adjuvant in rats. DL-Fluorocitric acid barium inhibits nociceptive behaviors induced by Histamine (HY-B1204) in mice and blocks the phosphorylation of the NMDA receptor NR1 subunit in the lumbar spinal cord of mice. DL-Fluorocitric acid (barium) can be used in the research of mechanical hyperalgesia and nociceptive pain .
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- HY-15264
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MC 1046
1 Publications Verification
Impurity A of Calcipotriol
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VD/VDR
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Cancer
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MC 1046 (Impurity A of Calcipotriol) is a hepatic metabolite and an impurity of Calcipotriol (HY-10001). MC 1046 induces differentiation of histiocytic lymphoma cells. MC 1046 can be used for the research of histiocytic lymphoma .
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- HY-W1015419
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α-Fluoromethylhistidine
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Amino Acid Decarboxylase
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Cardiovascular Disease
Neurological Disease
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α-FMH (α-Fluoromethylhistidine) is an orally active histidine decarboxylase inhibitor. α-FMH depletes histamine in enterochromaffin-like (ECL) cells, reduces the number and volume density of secretory vesicles in ECL cells, and does not affect histamine storage in mast cells. α-FMH abolishes Omeprazole (HY-B0113)-induced vacuolization of ECL cells and decreases gastrin-induced histamine efflux from ECL cells. α-FMH does not alter the granular characteristics of ECL cells, omeprazole-induced hypertrophy of ECL cells, gastrin-induced pancreastatin-like immunoreactivity efflux, nor does it affect gastric acid secretion induced by histamine or vagal stimulation. α-FMH inhibits basal and gastrin-stimulated gastric acid secretion, reduces acid output induced by gastrin+IBMX (HY-12318), but does not directly affect acid generation in isolated parietal cells .
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- HY-170788
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Phosphodiesterase (PDE)
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Metabolic Disease
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PDE7A-IN-1 is an orally active and selective PDE7A inhibitor with an IC50 of 0.0037 μM against PDE7A. PDE7A-IN-1 shows excellent isozyme selectivity over PDE7B. PDE7A-IN-1 elevates intracellular cAMP levels, suppresses ECR5 enhancer activity and reduces sclerostin expression. PDE7A-IN-1 significantly increases bone mineral density in rats. PDE7A-IN-1 can be used for the study of osteoporosis .
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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-117545
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RAR/RXR
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Cancer
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LE-540 is a selective retinoic acid receptor antagonist for RARβ (Ki=0.22 μM). LE-540 shows potential for use in cancer research, particularly for breast cancer and lung cancer .
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- HY-103344
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Aminopeptidase
Carboxypeptidase
mGluR
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Neurological Disease
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ZJ43 is a NAAG peptidase inhibitor and glutamate carboxypeptidase II/III (GCP II/III) inhibitor with human GCP II IC50 of 2.4 nM and Ki of 0.8 nM. ZJ43 blocks N-acetylaspartylglutamate hydrolysis, elevates extracellular N-acetylaspartylglutamate levels, and activates group II metabotropic glutamate receptors (mGluR). ZJ43 can be used for the research of schizophrenia, inflammatory pain, neuropathic pain, and traumatic brain injury .
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- HY-135319
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Bacterial
Antibiotic
ERK
JNK
NF-κB
ROR
Apoptosis
Caspase
GSK-3
Akt
PI3K
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Infection
Metabolic Disease
Inflammation/Immunology
Cancer
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Strictinin is an orally active phenolic compound. Strictinin reduces xanthine oxidase activity, uric acid production, and the activation of ERK1/2, JNK, NF-κB, and NLRP3 inflammasome components in hepatocytes treated with Xanthine (HY-W017389). Strictinin decreases elevated serum uric acid levels and enhanced xanthine oxidase activity in mice treated with potassium oxonate. Strictinin acts as a ROR1 inhibitor and exhibits anticancer activity against highly aggressive non-androgen-dependent prostate cancer. Strictinin induces cancer cell apoptosis (apoptosis), arrests cell cycle, and inhibits cancer cell migration, invasion, and epithelial-mesenchymal transition. Strictinin modulates gut microbiota, inhibits bacterial growth and biofilm formation, accelerates small intestinal transit, and blocks viral entry and replication. Strictinin can be used in research related to hyperuricemia, androgen receptor-negative non-androgen-dependent prostate cancer, triple-negative breast cancer, bacterial infections, constipation, coronavirus infections, dental caries, and infections caused by influenza A, influenza B, and human parainfluenza virus type 1 .
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- HY-P5875A
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
Inflammation/Immunology
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P4pal10 TFA is the TFA salt form of P4pal10 (HY-P5875). P4pal10 TFA is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 TFA inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 TFA reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 TFA ameliorates the injury in rats myocardial ischemia/reperfusion (I/R) models .
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- HY-N1964A
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Drug Derivative
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Metabolic Disease
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Gibberellic acid, suitable for plant cell culture (GA3, suitable for plant cell culture) is a natural plant growth regulator with oral bioactivity. Gibberellic acid, suitable for plant cell culture governs multiple plant developmental events, including seed germination, cell elongation, floral organ formation, and rice spikelet fertility. Gibberellic acid, suitable for plant cell culture optimizes root morphology and secondary metabolite production in Echinacea purpurea hairy roots, and serves as a bioactive seed priming agent to improve chilling stress tolerance in chickpea. Gibberellic acid, suitable for plant cell culture mediates modulation of enzyme activity and secondary metabolism in plants and exerts tissue-specific regulatory effects on antioxidant systems and lipid peroxidation in rats. Gibberellic acid, suitable for plant cell culture can be used in studies of plant growth, metabolism, and abiotic stress responses .
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-
-
- HY-N2196
-
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Others
|
Inflammation/Immunology
|
|
Ajugasterone C is an ecdysteroid isolated from Leuzea carthamoides. Ajugasterone C shows significant inhibitory effect at 100 mg/kg dose on rat paw oedema development due to Carrageenan-induced inflammation in Sprague Dawley rats .
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-
-
- HY-127125
-
|
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COX
|
Inflammation/Immunology
|
|
Diclofenac ethyl ester is the prodrug of Diclofenac (HY-15036), that is encapsulated in polymer micelles in vitro, and released with prolonged circulation time and reduced drug concentrations in the heart and kidneys in vivo .
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-
-
- HY-172200
-
|
|
PD-1/PD-L1
HDAC
|
Inflammation/Immunology
Cancer
|
|
PD-L1/HDAC6-IN-1 is an orally active dual inhibitor of PD-L1 and HDAC6, with IC50 values of 26.8 nM and 78 nM, respectively. PD-L1/HDAC6-IN-1 binds to human and murine PD-L1 proteins with high affinity, while it reduces STAT3 phosphorylation and downregulates PD-L1 expression by inhibiting HDAC6, thus blocking the PD-1/PD-L1 interaction. PD-L1/HDAC6-IN-1 exhibits potent anti-tumor activity in a mouse melanoma model. PD-L1/HDAC6-IN-1 is suitable for research on tumor immune regulation related to melanoma .
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-
-
- 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 .
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-
-
- HY-P3641
-
|
|
GnRH Receptor
|
Neurological Disease
Metabolic Disease
|
|
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
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-
- HY-B2058
-
|
|
Fungal
Androgen Receptor
|
Infection
|
|
Triticonazole is an orally active triazole fungicide and androgen receptor antagonist. Triticonazole inhibits testosterone-induced androgen receptor activation and reduces basal testosterone secretion. Prenatal exposure to Triticonazole causes shortened anogenital distance in male rat fetuses and induces organ-specific histopathological changes in pigs. Triticonazole can be used for detoxification of seeds contaminated with fungal pathogens, but there is a risk of animal poisoning if the treated seeds are used as animal feed .
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-
- HY-N11925
-
|
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Others
|
Cardiovascular Disease
|
|
(+)-Osbeckic acid is a vasorelaxatant that can be isolated from Tartary Buckwheat. (+)-Osbeckic acid has a potent vasorelaxant effect in Sprague-Dawley rat thoracic aorta rings with an EC50 of 887 μM .
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-
- HY-121123
-
|
2-Aminoadamantane-2-carboxylic acid
|
Aminopeptidase
|
Cancer
|
|
Adamantanine (2-Aminoadamantane-2-carboxylic acid) inhibits the transport of methionine (Ki is 0.76 mM) and leucine into Ehrlich ascites carcinoma cells. Adamantanine inhibits proliferation of P388 lymphocytic leukemia cells with an IC50 of >1 mM. Adamantanine inhibits the leucine aminopeptidase with an I/S0.5 of 10.5 .
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-
- HY-P5130
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Big endothelin-1 (rat 1-39) is a 39-residues peptide. Big endothelin-1 (rat 1-39) induces diuretic and natriuretic response in conscious Sprague-Dawley rats. Big endothelin-1 (rat 1-39) raises blood pressure in mice .
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-
- HY-172147
-
|
|
Somatostatin Receptor
|
Neurological Disease
|
|
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-120287
-
|
|
Somatostatin Receptor
|
Endocrinology
|
|
L-054522 is an agonist for somatostatin receptor subtype 2 with Kd of 0.01 nM. L-054522 inhibits growth hormone release from rat primary pituitary cell (IC50=0.05 nM) and glucagon and insulin release from isolated mouse pancreatic islet cell (IC50=0.05 nM and 12 nM) .
|
-
- HY-P10767
-
|
|
Neurotensin Receptor
|
Neurological Disease
|
|
MD01-67 is a selective macrocyclic compound targeting the neurotensin receptor type 2 (NTS2), with Ki of 2.9 nM. MD01-67 exhibits analgesic and tactile hypersensitivity reducing activity in rats acute/persistent/chronic inflammatory pain models .
|
-
- HY-151360
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
NHE3-IN-3 (Compound 1) is a Na +/H + exchanger isoform 3 (NHE3) inhibitor with pIC50 of 6.2 and 6.6 against human and rat NHE3, respectively. NHE3-IN-3 shows high (98%) oral bioavailability in Sprague–Dawley rats .
|
-
- 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-151066
-
|
|
PD-1/PD-L1
|
Cancer
|
|
BMS-1233 is an orally active inhibitor for programmed cell death-ligand 1 (PD-L1), with IC50 of 14.5 nM. BMS-1233 promotes cell death of HepG2 in a Jurkat T cell and HepG2 cell co-culture model, exhibits antitumor activity against melanoma in mouse model .
|
-
- 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-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-117443
-
|
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
IWP-051 is an agonist for soluble guanylate cyclase with an EC50 of 290 nM. IWP-051 stimulates the generation of cGMP, and exhibits the synergistic effect with NO. IWP-051 exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-N13714
-
-
- HY-50692
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
CAY10734 is the agonist for sphingosine-1-phosphate receptor 1 (S1P1) with an IC50 of 1.3 nM. CAY10734 promotes the recirculation of peripheral blood lymphocytes, and is a potential immunosuppressant .
|
-
- HY-P1134
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Galanin (1-15) (porcine, rat) is the N-terminal 15 amino acids peptide fragment of the neuropeptide galanin. Galanin (1-15) (porcine, rat) interacts with the 5-HT1A receptor in the dorsal hippocampus of the rat brain, reduces the affinity of 5-HT1A receptors, and regulates the serotonin neuronal networks .
|
-
- 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-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-163998
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
TLR4-IN-1 (compound 3k) inhibits the cell viability of RAW264.7 with an IC50 of 1.02 μM. TLR4-IN-1 inhibits the release of cytokine TNF-α, IL-1β and IL-6, and exhibits anti-inflammatory efficacy in rats rheumatoid arthritis models .
|
-
- HY-161784
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor modulator-5 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA receptor), with EC50 of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modulator-5 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modulator-5 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression .
|
-
- 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-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 .
|
-
- HY-B1573A
-
|
AY-23,028; dl-Butaclamol hydrochloride
|
Adrenergic Receptor
Dopamine Receptor
|
Neurological Disease
|
|
(±)-Butaclamol hydrochloride (AY-23,028) is the antagonist for adrenergic receptor and dopamine receptor. (±)-Butaclamol hydrochloride antagonizes amphetamine or Apomorphine (HY-12723)-induced stereotyped behaviors and emesis, inhibits discriminative avoidance behavior, and induces catalepsy in rats models .
|
-
- HY-168068
-
|
|
Drug Derivative
|
Neurological Disease
|
|
Res-Glu3 is the derivative of Resveratrol (HY-16561). Res-Glu3 mitigates the ROS accumulation, and exhibits neuroprotective efficacy against H2O2-caused cellular damage in PC12. Res-Glu3 exhibits antioxidant activity in rats ischemia reperfusion models .
|
-
- HY-162963
-
|
|
PPAR
|
Inflammation/Immunology
|
|
PPARδ agonist 11 (Compound 11) is a selective agonist for PPARδ with an EC50 of 20 nM. PPARδ agonist 11 reduces the levels of nitrite oxide (NO), proinflammatory cytokines TNFα and IL-6 in LPS (HY-D1056)-stimulated RAW264.7 cell, and exhibits anti-inflammatory efficacy via NF-κB pathway. PPARδ agonist 11 exhibits good stability in human liver microsomes and plasma. PPARδ agonist 11 ameliorates Carrageenan (HY-125474)-induced foot edema .
|
-
- HY-170586
-
-
- HY-161925
-
|
|
TGF-β Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
sTGFBR3 antagonist 1 (Compound p24) is an antagonist for soluble transforming growth factor beta receptor 3 (sTGFBR3), thus activates TGF-β signaling pathway, and inhibits IκBα/NF-κB signaling pathway. sTGFBR3 antagonist 1 inhibits NO-release in LPS (HY-D1056) -induced BV2 cells with an IC50 of 0.52 μM. sTGFBR3 antagonist 1 exhibits anti-inflammatory and neuroprotective activities with blood brain barrier (BBB) permeability. sTGFBR3 antagonist 1 can be used in Alzheimer’s Disease research .
|
-
- HY-75368
-
|
|
LRRK2
|
Neurological Disease
|
|
SRI-31255 is an orally active LRRK2 inhibitor with IC50 values of 520 and 427 nM for human wild-type (WT) and mutant G2019S, respectively. SRI-31255 exerts neuroprotective effects by binding to the ATP-binding pocket of LRRK2, inhibiting kinase activity. SRI-31255 can be used as a lead compound for the development of LRRK2-targeted drugs for the treatment of Parkinson's disease .
|
-
- 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-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-120476
-
|
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
|
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 .
|
-
- HY-169177
-
|
|
JNK
|
Inflammation/Immunology
|
|
JNK-1-IN-4 (Compound E1) is an inhibitor for JNK, that inhibits JNK-1, JNK-2 and JNK-3 with IC50s of 2.7, 19.0 and 9.0 nM, respectively. JNK-1-IN-4 inhibits the phosphorylation of c-Jun, and reduces the expression of TGF-β1-induced EMT marker proteins, such as fibronectin and α-SMA. JNK-1-IN-4 exhibits good pharmacokinetic characteristics with a bioavailability of 69%. JNK-1-IN-4 exhibits anti-fibrotic effect in Bleomycin (HY-17565)-induced mice idiopathic pulmonary fibrosis models .
|
-
- 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-164010
-
-
- HY-W686216
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
VK-28 is a blood-brain barrier-permeable iron chelator. VK-28 inhibits mitochondrial membrane lipid peroxidation and the iron-dependent generation of reactive hydroxyl radicals. VK-28 exhibits neuroprotective activity and protects rats against 6-OHDA-induced striatal dopaminergic damage. VK-28 can be used in studies related to Parkinson's disease .
|
-
- HY-10704R
-
|
PTP1B inhibitor (Standard)
|
Reference Standards
Phosphatase
NF-κB
|
Neurological Disease
Inflammation/Immunology
|
|
PTP1B-IN-1 (Standard) (PTP1B inhibitor (Standard)) is the analytical standard of PTP1B-IN-1 (HY-10704). This product is intended for research and analytical applications. PTP1B-IN-1 (Compound 7a) is a small molecule inhibitor of PTP1B with an IC50 value of 1.6 mM. It is often used as the mother core for derivatives of analogues .
|
-
- HY-153506
-
|
|
VAP-1
|
Inflammation/Immunology
|
|
VAP-1-IN-2 is an orally active VAP-1 inhibitor with an IC50 value of 0.025 μM against human VAP-1 and 0.015 μM against rat VAP-1. VAP-1-IN-2 inhibits urinary protein excretion and the progression of proteinuria in diabetic rats. VAP-1-IN-2 inhibits VAP-1 activity in rats . VAP-1-IN-2 can be used in research related to diabetes and nephropathy .
|
-
- HY-U00069
-
|
|
Monoamine Transporter
|
Neurological Disease
Inflammation/Immunology
|
|
Thionisoxetine is a norepinephrine transporter inhibitor with a Ki value of 0.2 nM in rats, and exhibits anti-hyperalgesic and analgesic activities. Thionisoxetine reverses thermal hyperalgesia and mechanical allodynia in rats. Thionisoxetine can be used in studies related to persistent inflammatory pain .
|
-
- HY-10716AR
-
|
|
Reference Standards
GlyT
|
Neurological Disease
|
|
PF-03463275 (Standard) is the analytical standard of PF-03463275 (HY-10716A). This product is intended for research and analytical applications. PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research .
|
-
- HY-182585
-
-
- HY-P10587B
-
|
JNJ-77242113 (hydrochloride); JNJ-2113 (hydrochloride); PN-235 (hydrochloride)
|
Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) hydrochloride is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra hydrochloride 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 hydrochloride exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra hydrochloride can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
-
- HY-182697
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
RTICBM-74 is a blood-brain barrier-permeable, selective CB1 allosteric modulator with IC50 values of 23 nM (calcium mobilization assay) and 153 nM ([ 35S]GTPγS assay). RTICBM-74 inhibits CB1 receptor signaling. RTICBM-74 reduces alcohol intake in rats. RTICBM-74 can be used for the research of alcohol use disorder .
|
-
- HY-180401
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
DMP 811 is a potent, orally active and selective angiotensin II subtype receptor AT1 antagonist. DMP 811 exhibits selectivity for AT1 (IC50 = 6 nM) over AT2 (IC50 >10 μM). DMP 811 exhibits potent antihypertensive activity in rats and dogs. DMP 811 can be used for the research of hypertension .
|
-
- HY-18654A
-
|
|
mGluR
|
Neurological Disease
|
|
ADX88178 TFA is an orally active, blood-brain barrier-penetrant, selective positive allosteric modulator of mGluR4, with an EC50 of 3.5 nM against hmGluR4. ADX88178 TFA modulates mGlu4 activity, enhances glutamate-mediated receptor activation, and increases the apparent affinity of glutamate for the receptor. ADX88178 TFA reverses haloperidol-induced catalepsy, potentiates the effects of levodopa (L-DOPA) and quinpirole, but fails to alleviate established abnormal involuntary movements, does not exacerbate L-DOPA-induced dyskinesia, and does not affect forelimb akinesia when administered alone. ADX88178 TFA can be used in research related to L-DOPA-induced dyskinesia and Parkinson's disease .
|
-
- HY-15080
-
|
LY 293606
|
iGluR
|
Cardiovascular Disease
Neurological Disease
|
|
GYKI 53405 is a non-competitive, orally active AMPA receptor antagonist. GYKI 53405 shows no significant binding affinity for GABAA, GABAB or benzodiazepine receptors. GYKI 53405 increases self-grooming behavior, induces wet dog-like shakes, reduces spontaneous activity, produces anxiolytic-like behavior, reverses the anxiogenic effect induced by mCPP, inhibits locomotor activity, suppresses sound-induced and maximal electroshock-induced seizures, prolongs survival in global cerebral ischemia models, and exhibits sustained anticonvulsant effects at doses below the sedation threshold. GYKI 53405 can be used in research related to absence epilepsy, anxiety disorders and global cerebral ischemia .
|
-
- 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-Y1191
-
|
EEDQ
|
Biochemical Assay Reagents
|
|
EEDQ is a carboxylate activator and irreversible antagonist of 5HT2c receptors. EEDQ reduces [ 3H]β-CIT binding to the dopamine transporter (DAT) in rat caudate-putamen (CPu) homogenates (IC50 = 78.3 μM). EEDQ inhibits contralateral rotation behavior .
|
-
- 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 .
|
-
- 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-159062
-
|
|
Biochemical Assay Reagents
|
|
Goji Extract is a natural product with anti-aging, antioxidant, and neuroprotective effects. The antioxidant effect of Goji Extract has a positive impact on erectile dysfunction and can be used in research to improve erectile function .
|
-
- HY-N1964A
-
|
|
Biochemical Assay Reagents
|
|
Gibberellic acid, suitable for plant cell culture (GA3, suitable for plant cell culture) is a natural plant growth regulator with oral bioactivity. Gibberellic acid, suitable for plant cell culture governs multiple plant developmental events, including seed germination, cell elongation, floral organ formation, and rice spikelet fertility. Gibberellic acid, suitable for plant cell culture optimizes root morphology and secondary metabolite production in Echinacea purpurea hairy roots, and serves as a bioactive seed priming agent to improve chilling stress tolerance in chickpea. Gibberellic acid, suitable for plant cell culture mediates modulation of enzyme activity and secondary metabolism in plants and exerts tissue-specific regulatory effects on antioxidant systems and lipid peroxidation in rats. Gibberellic acid, suitable for plant cell culture can be used in studies of plant growth, metabolism, and abiotic stress responses .
|
| Cat. No. |
상품명 |
Target |
Research Area |
-
- 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-P3641A
-
|
|
GnRH Receptor
|
Neurological Disease
Metabolic Disease
|
|
Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
|
-
- HY-100801A
-
|
|
Peptides
|
Others
|
|
DL-threo-3-Hydroxyaspartic acid is a glutamate uptake inhibitor that can block glutamate transport in cannulated sprague dawley rat .
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-
- HY-P5875A
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
P4pal10 TFA is the TFA salt form of P4pal10 (HY-P5875). P4pal10 TFA is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 TFA inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 TFA reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 TFA ameliorates the injury in rats myocardial ischemia/reperfusion (I/R) models .
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-
- 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 .
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-
- HY-P3641
-
|
|
GnRH Receptor
|
Neurological Disease
Metabolic Disease
|
|
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
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-
- HY-P5130
-
|
|
Endothelin Receptor
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Cardiovascular Disease
|
|
Big endothelin-1 (rat 1-39) is a 39-residues peptide. Big endothelin-1 (rat 1-39) induces diuretic and natriuretic response in conscious Sprague-Dawley rats. Big endothelin-1 (rat 1-39) raises blood pressure in mice .
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-
- HY-P10767
-
|
|
Neurotensin Receptor
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Neurological Disease
|
|
MD01-67 is a selective macrocyclic compound targeting the neurotensin receptor type 2 (NTS2), with Ki of 2.9 nM. MD01-67 exhibits analgesic and tactile hypersensitivity reducing activity in rats acute/persistent/chronic inflammatory pain models .
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-
- 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 .
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-
- HY-P10587A
-
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JNJ-77242113 acetate; JNJ-2113 acetate; PN-235 acetate
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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 .
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-
- HY-P1134
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|
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5-HT Receptor
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Neurological Disease
|
|
Galanin (1-15) (porcine, rat) is the N-terminal 15 amino acids peptide fragment of the neuropeptide galanin. Galanin (1-15) (porcine, rat) interacts with the 5-HT1A receptor in the dorsal hippocampus of the rat brain, reduces the affinity of 5-HT1A receptors, and regulates the serotonin neuronal networks .
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-
- HY-P10587B
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|
JNJ-77242113 (hydrochloride); JNJ-2113 (hydrochloride); PN-235 (hydrochloride)
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Interleukin Related
STAT
IFNAR
|
Inflammation/Immunology
|
|
Icotrokinra (JNJ-77242113) hydrochloride is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra hydrochloride 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 hydrochloride exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra hydrochloride can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
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| Cat. No. |
상품명 |
Target |
Research Area |
Image |
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- HY-P99221
-
|
RN-624; PF 4383119
|
Trk Receptor
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Neurological Disease
Inflammation/Immunology
Cancer
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|
Tanezumab (RN-624) is a humanized anti-NGF mAb with high affinity and specificity. Tanezumab blocks NGF binding to its receptors, p75 and TrkA, in the peripheral nervous system. Tanezumab can be used in studies of acute and chronic pain such as osteoarthritis, knee and neuralgia, as well as post-herpetic neuralgia .
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-
(5)
-
- HY-P991272
-
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PF-05230900
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Interleukin Related
|
Inflammation/Immunology
|
|
ATR-107 (PF-05230900) is a humanized monoclonal antibody inhibitor that targets the interleukin-21 receptor (IL-21R). The Ka value of ATR-107 is 2-4 nM in cynomolgus monkeys, 16 nM in mice, and 71 nM in rats. ATR-107 can be used in research related to systemic lupus erythematosus and air pouch inflammation .
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-
(5)
| Cat. No. |
상품명 |
Category |
Target |
Chemical Structure |
-
- HY-N0730
-
-
-
- HY-133668
-
|
|
Other disease
Disease markers
Endogenous metabolite
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Drug Metabolite
Cytochrome P450
PPAR
|
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Monoethyl phthalate is an orally active PDX-1 activator and the major hydrolytic metabolite of Diethyl phthalate (HY-Y0284) in vivo, with reproductive toxicity. Monoethyl phthalate targets aromatase (aromatase/CYP19A1) and PPAR to induce cell proliferation. The plasma protein binding rate of Monoethyl phthalate in rats and humans is lower than that of Diethyl phthalate. It exhibits significant enterohepatic circulation in rats and mainly accumulates in liver tissues. Monoethyl phthalate shows no estrogenic activity in estrogen-dependent human breast cancer cells. Monoethyl phthalate can be used in studies of reproductive toxicity and related environmental endocrine disruption mechanisms .
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-
-
- HY-129630
-
-
-
- HY-N0493
-
|
|
Structural Classification
Flavonoids
Classification of Application Fields
Flavones
Campylotropis hirtella (Franch.) Schindl.
Phenols
Polyphenols
Plants
Compositae
Inflammation/Immunology
Disease Research Fields
Source Classification
|
COX
Lipoxygenase
NF-κB
p38 MAPK
ERK
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
PI3K
Apoptosis
Autophagy
|
|
Pectolinarigenin is an orally active dual inhibitor of COX-2/5-LOX with anti-inflammatory, antioxidant, antitumor and neuroprotective activities. Pectolinarigenin exerts neuroprotective and anti-inflammatory effects on astrocyte inflammation via the NFκB and MAPK pathways. Pectolinarigenin inhibits LPS-induced phosphorylation of ERK1/2, N-FκB and p38MAPK, directly inhibits the enzymatic activity or binding of COX-2, 5-LOX and HIF-1α, and reduces the level of XIAP. Pectolinarigenin modifies Keap1 to promote nuclear accumulation of Nrf2, induces ARE-mediated antioxidant enzyme expression, and possesses direct free radical scavenging activity. Pectolinarigenin reduces the release of NO, proinflammatory mediators and leukotrienes, and increases the level of IL-10. Pectolinarigenin induces G2/M cell cycle arrest, apoptosis (Apoptosis) and autophagy (Autophagy) via the PI3K/AKT/mTOR signaling pathway. Pectolinarigenin reduces renal crystal deposition and inhibits melanin synthesis. Pectolinarigenin inhibits inflammation and alleviates allergy in mouse models of inflammation. Pectolinarigenin alleviates renal injury, inflammation and oxidative stress in mice by inhibiting HIF-1α activity. Pectolinarigenin can be used for the research of neurodegenerative diseases, inflammatory/allergic diseases, calcium oxalate nephrocalcinosis, gastric cancer, melasma, post-inflammatory diseases and chloasma .
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-
-
- HY-113093
-
-
-
- HY-128749
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-
-
- HY-114557
-
|
3,5-Diiodo-L-thyronine
|
Structural Classification
Monophenols
Classification of Application Fields
Ketones, Aldehydes, Acids
Phenols
Metabolic Disease
Endogenous metabolite
Disease Research Fields
Source Classification
|
JNK
NF-κB
Sirtuin
PGC-1α
COX
TGF-β Receptor
Collagen
|
|
NSC 90469 (3,5-Diiodo-L-thyronine) is an orally active thyroid hormone derivative. NSC 90469 inhibits JNK phosphorylation and NF-κB acetylation, blocks SIRT1 protein expression, induces elevated PGC-1α levels, and stimulates COX activity. NSC 90469 enhances UCP1-mediated thermogenesis, increases hepatic Dio1 activity, inhibits TSH levels and hypothalamic-pituitary-thyroid axis function, enhances lipid metabolism, and regulates energy metabolism via the mitochondrial pathway. NSC 90469 prevents blood glucose reduction, reduces urinary albumin excretion, inhibits renal matrix expansion, decreases TGF-β1 expression, and reduces renal fibronectin and type Ⅳ collagen deposition. NSC 90469 also increases energy expenditure and prevents diet-induced overweight. NSC 90469 can be used in studies related to diabetic nephropathy, hypothyroidism, non-alcoholic fatty liver disease, and diet-induced obesity .
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-
-
- HY-W008270
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-
-
- HY-N2512
-
-
-
- HY-N0909
-
-
-
- HY-125539
-
|
|
Structural Classification
Natural Products
Microorganisms
Source Classification
|
Antibiotic
Phosphatase
Fungal
|
|
Roridin E is a glucose-6-phosphatase (G6Pase) inhibitor and antibiotic, and is a metabolic byproduct of Roridin A (HY-N9599). Roridin E induces significant oxidative stress, characterized by depletion of glutathione in vivo, induction of hepatic lipid peroxidation, and inhibition of renal superoxide dismutase activity. Roridin E reduces blood glucose levels in rats, but exhibits acute toxicity (which is enhanced when co-administered with linoleic acid (HY-N0729)) and causes hepatotoxicity in male albino mice. Roridin E induces a decrease in total blood protein and increases in the levels of total lipids, γ-glutamyltransferase, alkaline phosphatase, and 5'-nucleotidase. Roridin E can be isolated from molds, and possesses cytostatic and antifungal activities similar to those of Verrucarin A (HY-107426) and Roridin A. Roridin E exhibits in vivo activity in rodents and is commonly used in hepatotoxicity-related studies .
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-
-
- HY-N4031
-
-
-
- HY-B1341
-
|
Enidrel; SC-4642; NSC 15432
|
Structural Classification
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Endocrinology
Steroids
Source Classification
|
Endogenous Metabolite
Progesterone Receptor
|
|
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-135319
-
|
|
Structural Classification
Phenols
Polyphenols
Camellia sinensis (L.) O. Ktze.
Plants
Source Classification
Theaceae
|
Bacterial
Antibiotic
ERK
JNK
NF-κB
ROR
Apoptosis
Caspase
GSK-3
Akt
PI3K
|
|
Strictinin is an orally active phenolic compound. Strictinin reduces xanthine oxidase activity, uric acid production, and the activation of ERK1/2, JNK, NF-κB, and NLRP3 inflammasome components in hepatocytes treated with Xanthine (HY-W017389). Strictinin decreases elevated serum uric acid levels and enhanced xanthine oxidase activity in mice treated with potassium oxonate. Strictinin acts as a ROR1 inhibitor and exhibits anticancer activity against highly aggressive non-androgen-dependent prostate cancer. Strictinin induces cancer cell apoptosis (apoptosis), arrests cell cycle, and inhibits cancer cell migration, invasion, and epithelial-mesenchymal transition. Strictinin modulates gut microbiota, inhibits bacterial growth and biofilm formation, accelerates small intestinal transit, and blocks viral entry and replication. Strictinin can be used in research related to hyperuricemia, androgen receptor-negative non-androgen-dependent prostate cancer, triple-negative breast cancer, bacterial infections, constipation, coronavirus infections, dental caries, and infections caused by influenza A, influenza B, and human parainfluenza virus type 1 .
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-
-
- HY-N2196
-
-
-
- HY-N11925
-
-
-
- HY-N13714
-
-
| Cat. No. |
상품명 |
|
Classification |
-
- HY-B1341
-
|
Enidrel; SC-4642; NSC 15432
|
|
Alkynes
|
|
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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