Search Result
Results for "
potentiate
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
14
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-14658
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-
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- HY-B0089
-
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BAY g 5421
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Glycosidase
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Infection
Metabolic Disease
Cancer
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Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
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- HY-B1811
-
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Arginine vasopressin; Antidiuretic hormone
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Endogenous Metabolite
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Neurological Disease
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Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
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- HY-15066
-
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FG9065
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iGluR
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Neurological Disease
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CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist . CNQX blocks the expression of fear-potentiated startle in rats .
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- HY-10932
-
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Ro 13-5057
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nAChR
iGluR
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Neurological Disease
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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 .
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- HY-15066A
-
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FG9065 disodium
|
iGluR
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Neurological Disease
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CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist . CNQX disodium blocks the expression of fear-potentiated startle in rats .
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- HY-100957
-
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Nucleoside Transporters
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Cardiovascular Disease
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Dilazep dihydrochloride is an inhibitor of adenosine uptake. Dilazep dihydrochloride has cerebral and coronary vasodilating action through enhancement of effect of adenosine. Dilazep dihydrochloride also inhibits the ischemic damage, platelet aggregation, and membrane transport of nucleosides .
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- HY-101372A
-
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mAChR
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Neurological Disease
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Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms .
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- HY-B1429
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-
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- HY-160424
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Diethylamine NONOate sodium; Diethylamine nitric oxide sodium
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Reactive Oxygen Species (ROS)
Xanthine Oxidase
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Others
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DEANO sodium is notric oxide donor. DEANO sodium potentiates the abilitv of hypoxanthine/xanthine oxidase to induce lipid peroxidation as well as DNA single- and double-strand breaks .
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- HY-15044
-
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PARP
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Neurological Disease
Cancer
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NU1025 is a potent PARP inhibitor with an IC50 of 400 nM and a Ki of 48 nM. NU1025 potentiates the cytotoxicity of ionizing radiation and anticancer agents. NU1025 has anti-cancer and neuroprotective activity .
|
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- HY-112209
-
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mAChR
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Neurological Disease
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VU0467154 is a positive allosteric modulator of the M4 muscarinic acetylcholine receptor (mAChR), potentiating the response to ACh with pEC50s of 7.75, 6.2 and 6 for rat, human and cynomolgus monkey M4 receptor, respectively.
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- HY-124467
-
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Ro 07-4065
|
GABA Receptor
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Neurological Disease
|
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Difludiazepam (Ro 07-4065), a benzodiazepine derivative, is a GABAA receptor ligand with an IC50 of 4.1 nM. Difludiazepam binds to an allosteric site on the GABAA receptor to potentiate the receptor's response to GABA, reducing neuron excitability. Difludiazepam contains halogenated groups at the ortho position of its phenyl ring .
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- HY-100690
-
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DNA/RNA Synthesis
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Cancer
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NSC16168 is a specific inhibitor of ERCC1-XPF, with an IC50 value of 0.42 μM. NSC16168 inhibits DNA repair and potentiates CDDP efficacy in cancer .
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- HY-135572
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-
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- HY-N125722
-
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Aabomycin A1
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ATP Synthase
Antibiotic
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Infection
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Venturicidin A (Aabomycin A1), from actinomycetes, is a membrane-active natural product inhibitor of ATP synthase. Venturicidin A potentiates the aminoglycoside antibiotic gentamicin against multidrug-resistant clinical isolates of Staphylococcus, Enterococcus, and Pseudomonas aeruginosa. Venturicidin A shows noticeable toxicity toward human embryonic-kidney (HEK)cells with an IC50 of 31 μg/mL.
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- HY-N1944A
-
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Bacterial
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Infection
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cis-Nerolidol is a sesquiterpene alcohol that can be found in various plants. cis-Nerolidol exhibits antioxidant and antibacterial activities. cis-Nerolidol can also potentiate the action of antibiotics .
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- HY-119936
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CFTR
Autophagy
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Inflammation/Immunology
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GLPG2451 is a cystic fibrosis transmembrane conductance regulator (CFTR) potentiator, which effectively potentiates low temperature rescued F508del CFTR with an EC50 of 11.1 nM .
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- HY-143312
-
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GLP Receptor
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Metabolic Disease
Inflammation/Immunology
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V-0219 is an orally active glucagon-like peptide-1 receptor (GLP-1R) positive allosteric modulator. V-0219 potentiates GLP-1R stimulation, and enhances GLP-1-induced cAMP production and insulin secretion. V-0219 potentiates glucose-dependent insulin secretion. V-0219 improves glucose handling in normal and diabetic rodents. V-0219 can be used for the research of obesity-associated diabetes .
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- HY-124867
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TSH Receptor
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Endocrinology
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D3-βArr is a positive allosteric modulator for thyrotropin receptor (TSHR), which initiates translocation of β-Arr 1 by direct TSHR activation and potentiates TSH-mediated preosteoblast differentiation in vitro .
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- HY-124702
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Potassium Channel
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Cardiovascular Disease
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ICA-105574 is a potent and efficacious hERG channel activator. The primary mechanism by which ICA-105574 potentiates hERG channel activity is by removing hERG channel inactivation. ICA-105574 steeply potentiates current amplitudes more than 10-fold with an EC50 value of 0.5 +/- 0.1 μM and a Hill slope (n(H)) of 3.3 +/- 0.2. ICA-105574 can prevent arrhythmias induced by cardiac delayed repolarization. ICA-105574 shortens action potential duration in ventricular myocytes concentration-dependently .
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- HY-14612
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mGluR
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Neurological Disease
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CPPHA is potent and selective positive allosteric modulator (PAM) of the mGluR5 and mGluR1 (metabotropic glutamate receptor). CPPHA can potentiate responses of mGluR5 and mGluR1 to activation of these receptors. CPPHA is developed for the research of central nervous system disorders .
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- HY-156009
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Bacterial
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Infection
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CDFI is an inhibitor of the lipid II flippase MurJ. CDFI potentiates the activity of β-lactams against MRSA .
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- HY-W015050
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1-Aminoanthracene
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GABA Receptor
Chloride Channel
Fluorescent Dye
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Neurological Disease
|
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1-Anthramine (1-aminoanthracene) is a fluorescent general anesthetic. potentiates GABAergic transmission with Kd = 0.1 mM, for binding to the general anesthetic site in horse spleen apoferritin (HSAF). 1-Anthramine fluorescence is enhanced when bound to HSAF. 1-Anthramine potentiates chloride currents elicited by GABA. 1-Anthramine can reversibly inhibit the movement of Xenopus laevis, with an EC50 value of 16 μM .
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- HY-W743398
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CS-386
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GABA Receptor
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Neurological Disease
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Mexazolam (CS-386) is an orally active benzodiazepine and anxiolytic. Benzodiazepines bind to specific BZD-type receptors on the GABA-chloride complex and potentiate the inhibitory effects of GABA .
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- HY-143312A
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GLP Receptor
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Metabolic Disease
Inflammation/Immunology
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V-0219 hydrochloride is an orally active glucagon-like peptide-1 receptor (GLP-1R) positive allosteric modulator. V-0219 hydrochloride potentiates GLP-1R stimulation, and enhances GLP-1-induced cAMP production and insulin secretion. V-0219 hydrochloride potentiates glucose-dependent insulin secretion. V-0219 hydrochloride improves glucose handling in normal and diabetic rodents. V-0219 hydrochloride can be used for the research of obesity-associated diabetes .
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- HY-P4685
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Angiotensin Receptor
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Metabolic Disease
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(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated insulin receptor (IR) signaling and glycogen synthesis. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated phosphorylation of Akt and GSK3α/β .
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- HY-P3985
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Bradykinin potentiating peptide B
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Angiotensin-converting Enzyme (ACE)
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Cardiovascular Disease
Others
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Bradykinin potentiator B (Bradykinin potentiating peptide B) is venom of Agkistrodon halys blomhoffi. Bradykinin potentiator B is a potent ACE inhibitor. Bradykinin potentiator inhibits the activity of bradykinin inhibitory peptidase .
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- HY-106892
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348U87
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DNA/RNA Synthesis
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Infection
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BW 348U87 is an inhibitor for ribonucleotide reductase, which exhibits synergistic effect with Acyclovir (HY-17422), potentiate the antiviral activity of Acyclovir against herpes simplex virus (HSV) in athymic nude mouse model .
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- HY-W415004
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Cholinesterase (ChE)
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Neurological Disease
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ACHE-IN-38 (Compound mol-8) inhibits the metabolic breakdown of the neurotransmitter acetylcholine (ACh) by the enzyme acetylcholinesterase (AChE) and hence alleviates memory deficits in patients with Alzheimer’s Disease by potentiating cholinergic transmission .
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- HY-W178327
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Adenosine Receptor
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Cancer
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8-Chloro caffeine binds to adenosine receptors (Ki = 30 µM). 8-Chloro caffeine potentiates UV-induced chromosomal aberrations in Cl-I Chinese hamster embryonic lung cells. 8-Chloro caffeine is a derivative of the methylxanthine alkaloid caffeine .
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- HY-119993
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BMH-23
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DNA/RNA Synthesis
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Cancer
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AR03 (BMH-23) is an apurinic/apyrimidinic endonuclease 1 (Ape1) inhibitor with an IC50 of 2.1 µM. AR03 has low affinity for double-stranded DNA. AR03 potentiates the cytotoxicity of methyl methanesulfonate and temozolomide in SF767 cells .
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- HY-B0089R
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BAY g 5421 (Standard)
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Reference Standards
Glycosidase
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Metabolic Disease
Cancer
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Acarbose (Standard) is the analytical standard of Acarbose. This product is intended for research and analytical applications. Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
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- HY-113654
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TRP Channel
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Others
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AMG 7905 is a hypothermia-inducing transient receptor potential vanilloid type 1 (TRPV1) antagonist. AMG 7905 potentiates TRPV1 channels activation by protons and drives the reflectory inhibition of thermogenesis and tail-skin vasoconstriction, while potently blocking channel activation by capsaicin .
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- HY-134598A
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Epigenetic Reader Domain
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Cancer
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653-47 hydrochloride, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 hydrochloride is also a very weak CREB inhibitor with IC50 of 26.3 μM .
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- HY-131032
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Adenosine Receptor
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Others
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KI-7 is an A2B adenosine receptor positive allosteric modulator. KI-7 potentiates the cAMP accumulation induced by the non-selective A2B adenosine receptor agonist NECA (EC50=445.8 nM). KI-7 also potentiates the cAMP accumulation induced by the selective A2B adenosine receptor agonist BAY 60-6583 as well as by adenosine with EC50s of 2390 nM and 2550 nM, respectively .
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- HY-164704
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- HY-139628
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Bacterial
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Infection
Cancer
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JPD447, a MAC-0547630 derivative, is a novel class of UppS inhibitor to potentiate β-lactam antibiotics.
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- HY-101179
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- HY-N3995
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Apoptosis
Drug Metabolite
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Cancer
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5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis .
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- HY-117517
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Trk Receptor
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Cancer
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NG-012, potentiator of nerve growth factor (NGF), were isolated from the culture broth of Penicillium verruculosum F-4542. NG-012 potentiates the neurite outgrowth induced by NGF in rat pheochromocytoma cell line (PC12) .
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- HY-119226
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mAChR
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Neurological Disease
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VU0152099 is a potent, selective and brain-penetrant mAChR M4 positive allosteric modulator with an EC50 of 0.4 µM for rat M4 receptor. VU0152099 is inactive for other mAChR subtypes or other GPCRs. VU0152099 has no agonist activity but potentiated responses of M4 to acetylcholine .
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- HY-W654264
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Endogenous Metabolite
Integrin
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Cardiovascular Disease
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2-Methylbutyrylcarnitine (chloride) is a gut microbial metabolite which binds to integrin α2β1 in platelets, potentiating cytosolic phospholipase A2 (cPLA2) activation and platelet hyperresponsiveness. 2-Methylbutyrylcarnitine (chloride) enhances platelet hyperreactivity and thrombus formation in mice. 2-Methylbutyrylcarnitine (chloride) is a branched-chain acylcarnitine .
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- HY-100957R
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Nucleoside Transporters
Reference Standards
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Cardiovascular Disease
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Dilazep (dihydrochloride) (Standard) is the analytical standard of Dilazep (dihydrochloride). This product is intended for research and analytical applications. Dilazep dihydrochloride is an inhibitor of adenosine uptake. Dilazep dihydrochloride has cerebral and coronary vasodilating action through enhancement of effect of adenosine. Dilazep dihydrochloride also inhibits the ischemic damage, platelet aggregation, and membrane transport of nucleosides .
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- HY-15276
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PARP
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Cancer
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4-Aminonaphthalimide is a potent PARP inhibitor and potentiates the cytotoxicity of γ-radiation in cancer cells .
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- HY-106822
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AO-33; (±)-Losigamone; LSG
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Sodium Channel
Chloride Channel
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Neurological Disease
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Losigamone (AO-33) is an orally active antiepileptic compound. Losigamone blocks sodium channel. Losigamone stimulates the neuronal chloride channel and enhance chloride influx. Losigamone potentiates GABA-mediated responses and reduces epileptiform activity induced by chloride channel antagonists. Losigamone can be used for epilepsy research .
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- HY-10932R
-
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Ro 13-5057 (Standard)
|
Reference Standards
nAChR
iGluR
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Neurological Disease
|
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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 .
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- HY-P2619
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-
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- HY-114611
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IRE1
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Metabolic Disease
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BDM44768 is an inhibitior of IDE. BDM44768 exacerbates ER stress-induced IRE1 activation and promotes lipid accumulation in hepatocytes. BDM44768 potentiates activation of the IRE1 pathway in the liver and exacerbates liver lipid accumulation in an acute mice model of ER stress .
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- HY-149812
-
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Bacterial
Parasite
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Infection
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Efflux pump-IN-4 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-4 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-4 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
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- HY-P1257
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Insulin Receptor
Neurotensin Receptor
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Metabolic Disease
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Xenin-8, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
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- HY-116859
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- HY-134598
-
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Epigenetic Reader Domain
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Cancer
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653-47, a potentiator, significantly potentiates the cAMP-response element binding protein (CREB) inhibitory activity of 666-15. 653-47 is also a very weak CREB inhibitor with IC50 of 26.3 μM .
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- HY-14611
-
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DFB
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mGluR
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Neurological Disease
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3,3'-Difluorobenzaldazine (DFB) is a selective positive allosteric modulator of mGluR5. 3,3'-Difluorobenzaldazine potentiates 3- to 6-fold action for mGlu5 agonists (Glutamate, Quisqualate, and 3,5-Dihydroxyphenylglycine), with EC50s in the 2 to 5 μM range .
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- HY-W769935
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-
- HY-103341
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-
- HY-149157
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- HY-101353
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(-)-LY 235959
|
iGluR
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Neurological Disease
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LY 235959 is a competitive N-methyl-D-aspartate (NMDA)-receptor antagonist. LY 235959 potentiates the anticonvulsant action of antiepileptics .
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- HY-N15081
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Others
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Cancer
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5-N-Acetylardeemin potentiated the cytotoxicity of the anticancer agent Vinblastine (HY-13780) in multidrug resistant human tumor cells .
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- HY-P3969
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- HY-116629
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Drug Derivative
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Neurological Disease
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Dactylyne is an ethyl dibromochloroether isolated from the sea hare Dactylomela. Dactylyne has the ability to inhibit Pentobarbital (PTB) metabolism and potentiate the effects of other hypnotic drugs .
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- HY-124264
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iGluR
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Neurological Disease
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UBP710 is a selective NMDA receptor modulator. UBP710 displays greater activity in potentiating GluN2B-containing receptors than those containing GluN2A .
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- HY-175470
-
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Amino Acid Derivatives
Lipase
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Others
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Stearidonoyl glycine is an N-acyl amino acid. Stearidonoyl glycine has a weak potentiating effect on some glycine receptor subtypes, among which the potentiation on GlyRα2 is statistically significant .
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- HY-P3578
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Insulin Receptor
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Endocrinology
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Gastric Inhibitory Polypeptide (1-30), porcine lacks the C-terminal 12 amino acid residues of natural gastric inhibitory polypeptide (GIP), exhibits biologic activity by potentiating the release of insulin and somatostatin .
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- HY-134220
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Parasite
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Infection
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Doramectin monosaccharide is an acid degradation product of Doramectin (HY-17035), a disaccharide-containing anthelmintic that potentiates glutamate- and GABA-gated chloride channel opening in nematodes. Doramectin undergoes acid-catalyzed hydrolysis to form doramectin monosaccharide.
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- HY-W003576
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Cholinesterase (ChE)
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Neurological Disease
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ACHE-IN-38 hydrochloride (Compound 13b) inhibits the metabolic breakdown of the neurotransmitter acetylcholine (ACh) by the enzyme acetylcholinesterase (AChE) and hence alleviates memory deficits in patients with Alzheimer’s Disease by potentiating cholinergic transmission .
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- HY-116205
-
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iGluR
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Others
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UBP684 is a novel positive allosteric modulator of NMDA receptors (NMDARs) that enhances receptor function by stabilizing the ligand-binding domains in a closed conformation, resulting in potentiated whole-cell currents and increased mean open time.
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- HY-B0089A
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Bay-g 5421 sulfate
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Glycosidase
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Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Acarbose (BAY g 5421) sulfate, antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose sulfate can potentiate the hypoglycemic effects of sulfonylureas or insulin .
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- HY-102063
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Pyridoxol, cyclic 3,4-hydrogen phosphate
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P2X Receptor
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Neurological Disease
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MRS 2219 (Pyridoxol) is a selective pharmacological probe of P2X1 receptor. MRS 2219 selectively potentiated ATP-evoked responses at P2X1 receptors with an EC50 of 5.9 μM .
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- HY-101179R
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- HY-161870
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Antibiotic
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Infection
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Antibiotic adjuvant 1 (compound 3e) is an antibiotic adjuvant that presents insufficient antibacterial activity (MIC > 128 µg/mL) and potentiate the activity of Cloxacillin (HY-B0466A)(66-fold) with synergistic effect .
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- HY-P4012
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Vasopressin Receptor
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Endocrinology
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[Asu1,6-Arg8]Vasopressin is an vasopressin agonist which potentiates cyclic AMP accumulation and ACTH release induced by corticotropin-releasing factor (CRF) in rat anterior pituitary cells in culture .
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![[Asu1,6-Arg8]Vasopressin](//file.medchemexpress.com/product_pic/hy-p4012.gif)
- HY-159930
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Bacterial
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Infection
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Antibiotic adjuvant 3 (compound 8g) is an antibiotic adjuvant with potent colistin-potentiating activity and low mammalian toxicity. Antibiotic adjuvant 3 has minimum re-sensitizing concentration of 0.25 μg/mL agnist of Escherichia coli AR-0493 .
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- HY-159929
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Bacterial
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Infection
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Antibiotic adjuvant 2 (compound 5q) is an antibiotic adjuvant with potent colistin-potentiating activity and low mammalian toxicity. Antibiotic adjuvant 2 has minimum re-sensitizing concentration of 0.125 μg/mL agnist of Escherichia coli AR-0493 .
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- HY-139803
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Prolyl Endopeptidase (PREP)
Neprilysin
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Cardiovascular Disease
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SCH-39370 is a potent and specific inhibitor of neutral metalloendopeptidase (NEP) from rabbit kidney with an IC50 value of 11.2 nM. SCH-39370 potentiates biological responses to atrial natriuretic factor and lowers blood pressure in desoxycorticosterone acetate-sodium hypertensive rats .
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- HY-106611
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SR 33287
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Phospholipase
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Cancer
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Brinazarone (SR 33287) is an inhibitor for acid lysosomal sphingomyelinase, and leads to cellular lipidosis. Brinazarone potentiates the cytotoxic effects of anti-Thy 1.2 AT15E RTA-IT on T2 cells and anti-CD5 T101 on CEM cells .
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- HY-112658
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Adrenergic Receptor
Adenosine Receptor
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Endocrinology
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p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC50 of 1.5 μM .
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- HY-N1944AR
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Reference Standards
Bacterial
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Infection
|
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cis-Nerolidol (Standard) is the analytical standard of cis-Nerolidol. This product is intended for research and analytical applications. cis-Nerolidol is a sesquiterpene alcohol that can be found in various plants. cis-Nerolidol exhibits antioxidant and antibacterial activities. cis-Nerolidol can also potentiate the action of antibiotics .
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- HY-161413
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Bacterial
|
Infection
Inflammation/Immunology
|
Antibacterial agent 204 (Compd P2-56-3) possesses potentiated Rifampin (RIF) activity against Acinetobacter baumannii and Klebsiella pneumoniae. Antibacterial agent 204 (Compd P2-56-3) disrupts the outer membrane of A. baumannii. T .
|
-
- HY-149810
-
|
|
Bacterial
Parasite
|
Infection
|
|
AcrB-IN-2 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. AcrB-IN-22 inhibits Nile Red (a known substrate of AcrB) efflux.AcrB-IN-2 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
|
-
- HY-100702
-
|
|
Akt
Apoptosis
|
Cancer
|
|
SH-5 is a potent AKT inhibitor. SH-5 potentiates the apoptosis induced by tumor necrosis factor. SH-5 blocks NF-kB activation induced by TNF-a, lipopolysaccharide (HY-D1056), phorbol ester (HY-18739), and cigarette smoke .
|
-
- HY-121323R
-
|
|
Reference Standards
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Acarbose (Standard) is the analytical standard of Acarbose. This product is intended for research and analytical applications. Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
|
-
- HY-113654A
-
|
|
TRP Channel
|
Cardiovascular Disease
|
|
AMG 7905 TFA is a hypothermia-inducing transient receptor potential vanilloid type 1 (TRPV1) antagonist. AMG 7905 TFA potentiates TRPV1 channels activation by protons and drives the reflectory inhibition of thermogenesis and tail-skin vasoconstriction, while potently blocking channel activation by capsaicin .
|
-
- HY-149811
-
|
|
Bacterial
Parasite
|
Infection
|
|
Efflux pump-IN-3 is an AcrB efflux pump inhibitor, with ability to potentiate the effect of antibiotics. Efflux pump-IN-3 inhibits Nile Red (a known substrate of AcrB) efflux. Efflux pump-IN-3 does not disrupts the bacterial outer membrane nor display toxicity in a nematode model .
|
-
- HY-P1257A
-
|
|
Neurotensin Receptor
|
Metabolic Disease
|
|
Xenin-8 TFA, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 TFA stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
|
-
- HY-17460AR
-
|
BMS284756 Mesylate hydrate (Standard)
|
Reference Standards
Bacterial
Topoisomerase
DNA/RNA Synthesis
Antibiotic
|
Infection
|
|
ACHE-IN-38 (hydrochloride) (Standard) is the analytical standard of ACHE-IN-38 (hydrochloride). This product is intended for research and analytical applications. ACHE-IN-38 hydrochloride (Compound 13b) inhibits the metabolic breakdown of the neurotransmitter acetylcholine (ACh) by the enzyme acetylcholinesterase (AChE) and hence alleviates memory deficits in patients with Alzheimer’s Disease by potentiating cholinergic transmission .
|
-
- HY-B0089S
-
|
BAY g 5421-d4
|
Isotope-Labeled Compounds
Glycosidase
|
Metabolic Disease
Cancer
|
|
Acarbose-d4 (BAY g 5421-d4) is deuterium labeled Acarbose. Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
|
-
- HY-115895
-
|
CI-686 free base
|
Dopamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Trebenzomine (CI-686 free base) is a centrally acting psychotropic compound. Trebenzomine has both neuroleptic and stimulant activity. Trebenzomine potentiates Methamphetamine-induced self-stimulation. Trebenzomine reduces septal
hyperirritability, suppression of conditioned avoidance behavior, blocks Apomorphine (HY-12723)-induced emesis in dogs .
|
-
- HY-120547
-
|
|
Adenylate Cyclase
|
Neurological Disease
Metabolic Disease
|
|
UCB-11056 is a modulator of cyclic AMP generation. UCB-11056 can rapidly increase cyclic AMP levels in the rat brain in vivo and potentiate stimulated cyclic AMP formation in vitro. UCB-11056 does not stimulate cAMP formation on its own. UCB-11056 is a potential nootropic drug .
|
-
- HY-W003576R
-
|
|
Cholinesterase (ChE)
Reference Standards
|
Neurological Disease
|
|
ACHE-IN-38 (hydrochloride) (Standard) is the analytical standard of ACHE-IN-38 (hydrochloride). This product is intended for research and analytical applications. ACHE-IN-38 hydrochloride (Compound 13b) inhibits the metabolic breakdown of the neurotransmitter acetylcholine (ACh) by the enzyme acetylcholinesterase (AChE) and hence alleviates memory deficits in patients with Alzheimer’s Disease by potentiating cholinergic transmission .
|
-
- HY-P5172
-
|
|
Sodium Channel
|
Neurological Disease
|
|
MitTx-alpha is a subunit of MitTx. MitTx is a potent, persistent, and selective agonist for acid-sensing ion channels (ASICs). MitTx is highly selective for the ASIC1 subtype at neutral pH; under more acidic conditions (pH<6.5), MitTx massively potentiates (>100-fold) proton-evoked activation of ASIC2a channels .
|
-
- HY-107153
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Amidox is a ribonucleotide reductase inhibitor. Amidox potentiates the action of Arabinofuranosylcytosine in leukemia .
|
-
- HY-100957A
-
|
|
Nucleoside Transporters
|
Cardiovascular Disease
|
|
Dilazep is an inhibitor of adenosine uptake. Dilazep has cerebral and coronary vasodilating action through enhancement of effect of adenosine. Dilazep also inhibits the ischemic damage, platelet aggregation, and membrane transport of nucleosides .
|
-
- 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-129425
-
|
|
PARP
|
Others
|
|
NU1064 (dihydrochloride) is an inhibitor of PARP. NU1064 (dihydrochloride) potentiates the cytotoxicity of DNA-methylating agent (MTIC) in a concentration-dependent manner .
|
-
- HY-119360
-
|
|
Insecticide
|
Others
|
|
Lilly 18947 (free base) is a selective drug-potentiating agent that synergizes carbamate insecticides. Lilly 18947 (free base) inhibits a variety of detoxication mechanisms in mammals .
|
-
- HY-183947
-
|
|
Phosphatase
Drug Derivative
|
Cancer
|
|
4-Bromolevamisole, an analogues of Levamisole (HY-A0106), is a phosphatase inhibitor. 4-Bromolevamisole potentiates the antineoplastic activity of 5-Fluorouracil (HY-90006), its analogues, or prodrugs thereof.4-Bromolevamisole can be used for cancer research .
|
-
- HY-N15436
-
|
|
GABA Receptor
|
Neurological Disease
|
|
5-Deoxykievitone, an isoflavanone found in Phaseolus species, is a GABA receptor modulator. 5-Deoxykievitone potentiates GABA-induced chloride current through α1β2γ2s GABAA receptors. 5-Deoxykievitone can be used for the research of epilepsy and anxiety .
|
-
- HY-204388
-
|
|
iGluR
Calcium Channel
|
Neurological Disease
|
|
TAK-137 is an AMPA receptor potentiator with weak agonistic effect. TAK-137 binds to the AMPA receptor ligand binding domain in a glutamate-dependent manner. TAK-137 potentiates AMPA-induced currents and Ca 2+ influx. TAK-137 can be used for the research of neurological disease .
|
-
- HY-101372AR
-
|
|
mAChR
Reference Standards
|
Neurological Disease
|
|
Oxotremorine M (iodide) (Standard) is the analytical standard of Oxotremorine M (iodide) (HY-101372A). This product is intended for research and analytical applications. Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms .
|
-
- HY-128049
-
|
|
Beta-lactamase
|
Infection
|
|
ML121 is a selective and potent VIM-2 inhibitor with an IC50 of 54 nM and a Ki of 148 nM. ML121 shows inactive in IMP-1 and TEM-1 beta-lactamase assays. ML121 can potentiate the antibiotic activity of Imipenem (HY-B1369A) in VIM-2 transformed E.coli .
|
-
- HY-15519
-
|
|
IAP
FLT3
|
Cancer
|
|
LBW242, a 3-mer and Smac mimetic, is a potent and orally active proapoptotic IAP inhibitor. LBW242 shows effects on mutant FLT3-expressing cells. LBW242 has activity against multiple myeloma, and potentiates TRAIL- and anticancer agent-mediated cell death of ovarian cancer cells .
|
-
- HY-136731
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells .
|
-
- HY-153542
-
|
|
PKG
|
Others
|
|
AP-C6 is a potent inhibitor of guanosine 3′,5′-cyclic monophosphate (cGMP)-dependent protein kinase II (cGKII) with a pIC50 of 6.5. AP-C6 concentration-dependently inhibits human cGKII activity in vitro. AP-C6 potentiate cAMP signaling by PDE inhibition .
|
-
- HY-114555
-
|
|
GlyT
|
Neurological Disease
|
|
TASP0315003 is a glycine transporter 1 (GlyT1) inhibitor. TASP0315003 potentiates NMDA receptor function by increasing synaptic glycine levels. TASP0315003 can improve cognitive dysfunction and the negative symptoms of schizophrenia without having undesirable central nervous system side effects. TASP0315003 can be used for the research of neurological disease .
|
-
- HY-130656
-
|
cis-8-Eicosenoic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
8(Z)-Eicosenoic acid is a cis-unsaturated free fatty acid with a 20-carbon chain. It potentiates acetylcholine (ACh) receptor channel currents without depression and enhances PCKε phosphorylation of a substrate peptide in Xenopus oocytes. 8(Z)-Eicosenoic acid constitutes 6% of the fatty acid pool in seed oil isolated from B. collina.
|
-
- HY-W856819
-
|
|
Opioid Receptor
Cholinesterase (ChE)
Drug Metabolite
nAChR
|
Neurological Disease
|
|
Eseroline is a potent μ-opioid receptor agonist, which is the hydrolytic metabolite of Physostigmine (HY-N6608). Eseroline is a selective and competitive acetylcholinesterase (AChE) inhibitor, with its Ki values for AChE and BuChE being 0.1 μM and 200 μM respectively. Eseroline has nicotinic acetylcholine receptor allosteric enhancing ligand (nAChR-APL) activity, meaning it does not activate the receptor but significantly enhances the signal transduction of Ach triggered by the receptor. Eseroline is neurotoxic, causing cell membrane damage (LDH leakage) and energy metabolism collapse (ATP depletion). Eseroline can be used for the study of Alzheimer's disease .
|
-
- HY-142723
-
|
|
Potassium Channel
|
Neurological Disease
|
|
KCa2 channel modulator 1 (compound 2o) is a potent subtype-selective positive modulator of KCa2 channel. KCa2 channel modulator 1 potentiates human KCa2.3 channels with an EC50 value of 0.19 μM and 0.99 μM on the rat KCa2.2 channel subtype .
|
-
- HY-103367
-
|
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
CHK1-IN-7 (Compound 10c) is a potent human CHK1 inhibitor. CHK1-IN-7 shows no single agent effect, potentiates the antiproliferative effect of Gemcitabine HY-17026 in both prostate and breast cancer cell lines. CHK1-IN-7 can be used for the research of cancer .
|
-
- HY-157838
-
|
|
MAP4K
|
Cancer
|
|
HMC-B17 is a selective, orally bioavailable HPK1 inhibitor (IC50 = 1.39 nM) that potentiates anti-PD-L1 efficacy. HMC-B17 potently enhances the IL-2 secretion in Jurkat cells (EC50 = 11.56 nM). HMC-B17 can be used for the research of cancer .
|
-
- HY-15066R
-
|
FG9065 (Standard)
|
iGluR
Reference Standards
|
Neurological Disease
|
|
CNQX (Standard) is the analytical standard of CNQX. This product is intended for research and analytical applications. CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist . CNQX blocks the expression of fear-potentiated startle in rats .
|
-
- HY-147349
-
|
ANT3310 sodium
|
Beta-lactamase
Bacterial
|
Infection
|
|
Pilabactam (ANT3310) sodium is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC50 values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). Pilabactam sodium potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). Pilabactam sodium can be used in the research of bacterial infection .
|
-
- HY-P5780
-
|
|
Sodium Channel
|
Neurological Disease
|
|
π-TRTX-Hm3a is a 37-amino acid peptide isolated from Togo starburst tarantula (Heteroscodra maculata) venom. π-TRTX-Hm3a pH-dependently inhibits acid-sensing ion channel 1a (ASIC1a) with an IC50 of 1-2 nM and potentiates ASIC1b with an EC50 of 46.5 nM .
|
-
- HY-147349A
-
|
ANT3310
|
Bacterial
Beta-lactamase
|
Infection
|
|
Pilabactam (ANT3310) is a broad-spectrum covalent Serine β-Lactamase inhibitor, with IC50 values ranging from 1 nM to 175 nM (a panel of Serine β-Lactamase). Pilabactam potentiates activity of β-lactam antibiotics against Carbapenem-Resistant Enterobacterales (CRE) and Acinetobacter baumannii (CRAB). Pilabactam can be used in the research of bacterial infection .
|
-
- HY-B1811S1
-
|
Arginine vasopressin-d5; Antidiuretic hormone-d5
|
Isotope-Labeled Compounds
|
Others
|
|
Vasopressin-d5 is anIsotope-labeled compound of Vasopressin. Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of the corticotropin-releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
|
-
- HY-120523
-
|
|
iGluR
|
Neurological Disease
|
|
UBP646 is a potent GluN1/GluN2D receptors potentiator, and also potentiates the other three subtypes, GluN1/GluN2A, GluN1/GluN2B, and GluN1/GluN2C receptors .
|
-
- HY-N6733
-
Aphidicolin
Maximum Cited Publications
15 Publications Verification
|
DNA/RNA Synthesis
HSV
Apoptosis
Antibiotic
Orthopoxvirus
|
Infection
Inflammation/Immunology
|
|
Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering DNA polymerase activity. Aphidicolin is an antibiotic produced by mold Cephalosporium aphidicola, inhibits cellular deoxyribonucleic acid synthesis and the growth of herpes simplex virus. Aphidicolin exhibits anti-orthopoxvirus activity and potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line .
|
-
- HY-N3995S
-
|
|
Isotope-Labeled Compounds
Apoptosis
Drug Metabolite
|
Cancer
|
|
5β-Dihydrocortisol-d6 is the deuterium labeled 5β-Dihydrocortisol. 5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis .
|
-
- HY-177218
-
|
NSC 119910
|
Phospholipase
Opioid Receptor
|
Neurological Disease
|
|
M119 (NSC 119910) is a selective Gβγ-subunit inhibitor. M119 selectively potentiates μ-opioid-dependent antinociception. M119 inhibits μ-receptor-dependent phospholipase (PLC) activation. M119 can enhance opioid analgesia and attenuate its acute tolerance and dependence in mice. M119 can be used for pain research .
|
-
- HY-143498
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
ERCC1-XPF-IN-1 is a potent and high-affinity ERCC1-XPF inhibitor with IC50 value of 0.49 μM. ERCC1-XPF-IN-1 has the capacity to potentiate the cytotoxicity effect of UV radiation and inhibiting DAN repair, by the inhibition of removal of CPDs, and cyclophosphamide toxicity to colorectal cancer cells .
|
-
- HY-W1135319
-
|
|
Casein Kinase
Wee1
IKZF Family
|
Cancer
|
|
SB-405483 is a CRBN orthosteric ligand bindign enhancer. SB-405483 potentiates degradation of CRBN substrates including CK1α, Wee1, IKZF1/3. SB-405483 stabilizes CRBN and reduces CRBN autoubiquitination. SB-405483 can be used for the research of cancer, such as multiple myeloma and acute myeloid leukemia .
|
-
- HY-101377A
-
|
(R)-8-Hydroxy-2-dipropylaminotetralin hydrobromide
|
5-HT Receptor
|
Neurological Disease
|
|
R(+)-8-OH-DPAT ((R)-8-Hydroxy-2-dipropylaminotetralin) hydrobromide is a potent 5-HT1A agonist. R(+)-8-OH-DPAT potentiates SUL (HY-B1059)-induced dopamine (DA) release in the medial prefrontal cortex (mPFC) .
|
-
- HY-B1546
-
|
Benzylamiloride
|
Na+/Ca2+ Exchanger
Sodium Channel
|
Neurological Disease
|
|
Benzamil (Benzylamiloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM .
|
-
- HY-Y0669
-
-
- HY-B1546A
-
|
Benzylamiloride hydrochloride
|
Na+/Ca2+ Exchanger
Sodium Channel
|
Neurological Disease
|
|
Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na +/Ca 2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca 2+-activated currents, with an IC50 of 1.1 μM .
|
-
- HY-G0021
-
|
Norclozapine; Desmethylclozapine; Normethylclozapine
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
|
N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .
|
-
- HY-120139
-
KMH-233
1 Publications Verification
|
Amino acid Transporter
|
Cancer
|
|
KMH-233, a potent, reversible and selective inhibitor of l-type amino acid transporter LAT1/SLC7A5, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM) .
|
-
- HY-167825
-
-
- HY-111655
-
SKA-31
4 Publications Verification
|
Potassium Channel
|
Cardiovascular Disease
|
|
SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure .
|
-
- HY-182581
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
MK-3134 is an orally active, brain-penetrant and selective histamine H3 receptor inverse agonist. MK-3134 modulates histaminergic neurotransmission, decreases constitutive H3 receptor signaling, releases tonic inhibition of neurotransmitter release, potentiates neurotransmission, and may enhance cholinergic neurotransmission. MK-3134 can be used for the research of Alzheimer's disease .
|
-
- HY-107613A
-
|
DKGI-I hydrochloride; Diacylglycerol kinase inhibitor I hydrochloride
|
PKC
5-HT Receptor
|
Infection
Inflammation/Immunology
Cancer
|
|
R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
|
-
- HY-120645
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BMS-986122 is a selective, potent positive allosteric modulator of the mu-opioid receptor (µ-OR). BMS-986122 shows potentiation of orthosteric agonist-mediated β-arrestin recruitment, adenylyl cyclase inhibition, and G protein activation. BMS-986122 potentiates DAMGO-mediated [ 35S]GTPγS binding in mouse brain membranes .
|
-
- HY-107613
-
|
DKGI-I; Diacylglycerol kinase inhibitor I
|
PKC
5-HT Receptor
|
Inflammation/Immunology
|
|
R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
|
-
- HY-143415
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
Metallo-β-lactamase-IN-7 is a potent VIM-Type metallo-β-lactamase inhibitor with IC50s of 0.019 μM, 13.64 μM, 0.38 μM for VIM-2, VIM-1 and VIM-5. Metallo-β-lactamase-IN-7 potentiate antibacterial activity of Meropenem against the Gram-negative bacterial strains .
|
-
- HY-B1811R
-
|
Arginine vasopressin (Standard); Antidiuretic hormone (Standard)
|
Endogenous Metabolite
Reference Standards
|
Neurological Disease
|
|
Vasopressin (Standard) is the analytical standard of Vasopressin. This product is intended for research and analytical applications. Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
|
-
- HY-161681
-
|
|
Guanylate Cyclase
|
Metabolic Disease
|
|
Formycin triphosphate is a fluorescent analogue of ATP which on binding to enzyme active sites exhibits enhanced fluorescence. Formycin triphosphate is an ATP-competitive chicken liver pyruvate carboxylase inhibitor. Formycin triphosphate potentiates atrial natriuretic factor (ANF)-stimulated guanylate cyclase activity with an EC50 at about 90 μM and inhibits ATP-stimulated guanylate cyclase activity with an IC50 at about 100 μM .
|
-
- HY-W014622
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
CRT0044876 is a potent and selective apurinic/apyrimidinic endonuclease 1 (APE1) inhibitor (IC50=~3 μM). CRT0044876 inhibits the AP endonuclease, 3′-phosphodiesterase and 3′-phosphatase activities of APE1, and is a specific inhibitor of the exonuclease III family of enzymes to which APE1 belongs. CRT0044876 potentiates the cytotoxicity of several DNA base-targeting compounds .
|
-
- HY-123778
-
|
|
mAChR
|
Neurological Disease
|
|
VU6007678 (compound 18g) is a central nervous system-penetrant muscarinic acetylcholine receptor(mAChR) potentiator. VU6007678 potentiates acetylcholine-mediated signaling at human M1, M3, M5 and rat M1, M3, M4, M5 muscarinic acetylcholine receptors. VU6007678 is applicable to research related to Alzheimer's disease, schizophrenia, and ischemic stroke .
|
-
- HY-103552
-
|
|
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 .
|
-
- HY-14658R
-
|
|
Ligands for E3 Ligase
Autophagy
Apoptosis
Reference Standards
|
Inflammation/Immunology
Cancer
|
|
Thalidomide (Standard) is the analytical standard of Thalidomide. This product is intended for research and analytical applications. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ∼250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties. Thalidomide can work as molecular glue to potentiate substrate.
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-
- HY-A0009
-
|
Galantamine hydrobromide
|
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
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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-N15846
-
|
|
Drug Derivative
|
Infection
Inflammation/Immunology
|
|
VSA 1, a semisynthetic QS-21 (HY-101092) analog, is a saponin adjuvant. VSA 1 potentiates antigen-specific IgG1 and IgG2a immune responses in BALB/c mice, indicating a mixed Th1/Th2 immune response. VSA 1 significantly improves vaccine efficacy after primary immunization and enhances homologous protection .
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-
- HY-173556
-
|
|
GPR84
|
Inflammation/Immunology
|
|
GPR84 agonist-2 is a selective GPR84 agonist with no activity at free fatty acid receptors. GPR84 agonist-2 enhances GPR84-mediated signaling above basal levels and potentiates agonist-induced GPR84 activation. GPR84 agonist‑2 can be used for research on GPR84-related physiological mechanisms .
|
-
- HY-171302
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GLP-1R/GIPR agonist-2 is a GIPR agonist. GLP-1R/GIPR agonist-2 potentiates GIP(1-42)-induced intracellular cAMP production in cells expressing human GIPR. GLP-1R/GIPR agonist-2 can be used for the research of type II diabetes mellitus .
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-
- HY-179219S
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
RTx-303 is an orally active, selective DNA polymerase θ (Polθ) inhibitor (IC50 = 5.1 nM). RTx-303 exhibits significantly high cellular potency and strongly potentiates PARPi in BRCA1/2 mutant cells and patient-derived xenograft models. RTx-303 can be used for the study of BRCA2-mutated breast cancer .
|
-
- HY-124056
-
|
|
CXCR
|
Cancer
|
|
AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo .
|
-
- HY-108985
-
|
EGYT-3615
|
Others
|
Neurological Disease
|
|
Trazium esilate (EGYT-3615) is an antidepressant, which influences the central dopaminergic system. Trazium esilate synergizes amphetamine, potentiates stereotypy and hypermotility. Trazium esilate blocks Apomorphine (HY-12723)-induced hypothermic and the stereotypy, and Bulbocapnine (HY-W436270)-induced cataleptic state. Trazium esilate enhances the effect of Norepinephrine (HY-13715) on isolated vas deferens of the rat .
|
-
- HY-12390S
-
|
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Lofepramine-d3 (Lopramine-d3) is the deuterium labeled Lofepramine. Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties .
|
-
- HY-101165
-
|
|
iGluR
GABA Receptor
|
Neurological Disease
|
|
Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
|
-
- HY-100403
-
|
|
mGluR
|
Cancer
|
|
Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) .
|
-
- HY-N7426
-
|
3-Deoxy-D-glucosone
|
GLP Receptor
|
Metabolic Disease
|
|
3-Deoxyglucosone (3-Deoxy-D-glucosone) is a reactive intermediate of the Maillard reaction and the polyol pathway. 3-Deoxyglucosone rapidly reacts with protein amino groups to form advanced glycation end products (AGEs), such as imidazolone, it is the most specific AGE for 3-DG. 3-Deoxyglucosone synergizes with low glucose to potentiate GLP-1 secretion and is considered as a biomarker for diabetes .
|
-
- HY-176200
-
|
AF98943
|
mAChR
|
Neurological Disease
|
|
VU6008055 (AF98943) is a brain-penetrant, orally active and selective muscarinic acetylcholine receptor subtype 4 (mAChR4) activator with human EC50 values of 73.4 nM. VU6008055 potentiates mAChR4 receptor activity in the presence of acetylcholine, and exhibits no activity at mAChR1, mAChR3, or mAChR5. VU6008055 can be used for the research of schizophrenia, parkinson’s disease, alzheimer’s disease .
|
-
- HY-182584
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
S 15931 is a 5-HT1A receptor inhibitor. S 15931 inhibits the late-phase hindpaw licking response induced by formalin and the abdominal writhing response induced by acetic acid in Mus musculus. S 15931 abolishes the spontaneous tail-flick response induced by 8-OH-DPAT in Rattus norvegicus and potentiates the analgesic effect of morphine. S 15931 is applicable for pain-related research .
|
-
- HY-16969
-
|
PNB-0408; N-hexanoic-Try-Ile-(6)-amino hexanoic amide; Hexanoyl-Tyr-Ile-Ahx-NH2
|
c-Met/HGFR
|
Neurological Disease
|
|
Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with high affinity (Kd=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa exhibits excellent antidementia activity and improves cognitive function in animal models. Dihexa may have therapeutic potential as a treatment Alzheimer’s disease .
|
-
- HY-118140
-
|
|
Cannabinoid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
ZCZ011 is a potent and brain-penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
|
-
- HY-103520
-
|
|
GABA Receptor
|
Neurological Disease
|
|
DS2 is a selective positive allosteric modulator of δ-GABAA receptor. DS2 selectively potentiates GABA responses mediated by α4β3δ receptor. DS2 does not enhance activity at α4β3γ2 and α1β3γ2 receptors. DS2 relieves pain and has the potential for sleep disorders research .
|
-
- HY-G0021S
-
|
Norclozapine-d8; Desmethylclozapine-d8; Normethylclozapine-d8
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
|
N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .
|
-
- HY-B1671
-
|
|
GABA Receptor
Sodium Channel
Calcium Channel
|
Neurological Disease
Metabolic Disease
|
|
(+)-Kavain, a main kavalactone that can be extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .
|
-
- HY-123489
-
|
THDOC
|
GABA Receptor
|
Neurological Disease
|
|
3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
|
-
- HY-12976
-
|
|
G Protein-coupled Receptor Kinase (GRK)
|
Metabolic Disease
|
|
DS-1558 is an orally active small molecule G protein-coupled receptor 40 agonist. DS-1558 not only increases the glucose-stimulated insulin secretion by glucagon like peptide-1 (GLP-1) but also potentiated the maximum insulinogenic effects of GLP-1 after an intravenous glucose injection in normal Sprague Dawley rats. DS-1558 is promising for research of type 2 diabetes .
|
-
- HY-182631
-
|
|
iGluR
|
Neurological Disease
|
|
CX1763 is an AMPAR allosteric modulator. CX1763 allosterically potentiates glutamate-evoked currents, accelerates channel opening, and increases the surface levels of AMPAR containing Glur2 (R). CX1763 enhances synaptic transmission in the rat hippocampus. CX1763 improves attention in rats and attenuates amphetamine-induced hyperactivity in mice. CX1763 can be used in studies related to attention deficit hyperactivity disorder and opioid-induced respiratory depression .
|
-
- HY-158380
-
|
|
Bacterial
|
Infection
|
|
UH-NIP-16 exhibits antimicrobial activity against Mycobacterium tuberculosis, with MIC50 of 1.86 and 3.05 μM, for pathogenic mycobacterial strains H37Rv and CDC1551. UH-NIP-16 synergizes with Streptomycin (HY-B1906), Isoniazid (HY-B0329), Ethambutol (HY-B0535) and Bedaquiline (HY-14881), potentiates their anti-tuberculosis activities .
|
-
- HY-12757
-
|
|
BCRP
|
Cancer
|
|
YHO-13177, a acrylonitrile derivative, is an orally active, potent and specific inhibitor of breast cancer resistance protein (BCRP) and ABCG2 with an IC50 value of 10 nM. YHO-13177 potentiates the cytotoxicity of SN-38 in HCT116 and A549 cells that express BCRP. YHO-13177 combined with Irinotecan (HY-16562) significantly suppresses the tumor growth in an HCT116/BCRP xenograft model .
|
-
- HY-114833
-
|
(Rac)-Bunolol; dl-Bunolol
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Bunolol ((Rac)-Bunolol) is a β-adrenergic receptor blocker. Bunolol antagonizes the β-receptor agonist activity induced by Isoproterenol (HY-B0468) and Dichloroisoproterenol. Bunolol reduces the heart rate and mean blood pressure of anesthetized dogs. Bunolol decreases spontaneous motor activity and Amphetamine-induced hyperactivity in rats, potentiates Pentobarbital-induced hypnosis in mice, and protects rats from extensor tonic convulsions induced by maximal electroshock .
|
-
- HY-A0009S
-
|
Galantamine-d3 hydrobromide
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-G0021S1
-
|
Norclozapine-d8 hydrochloride; Desmethylclozapine-d8 hydrochloride; Normethylclozapine-d8 hydrochloride
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
|
N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist .
|
-
- HY-103645
-
|
|
Bacterial
Aurora Kinase
Apoptosis
|
Infection
Cancer
|
|
GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway . MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
|
-
- HY-150090
-
|
|
CFTR
|
Inflammation/Immunology
|
|
SRI-41315 induces a prolonged pause at stop codons and suppresses PTCs (premature termination codons) associated with cystic fibrosis in immortalized and primary human bronchial epithelial cells, restoring CFTR (cystic fibrosis transmembrane conductance regulator) expression and function. SRI-41315 suppresses PTCs by reducing the abundance of the termination factor eRF1. SRI-41315 also potentiates aminoglycoside-mediated readthrough, leading to synergistic increases in CFTR activity .
|
-
- HY-N7038
-
|
PHA-M
|
NF-κB
COX
Interleukin Related
Reactive Oxygen Species (ROS)
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Phytohemagglutinin (PHA-M), the major seed lectin of the common bean, Phaseolus vulgaris, is a T-cell activator. Phytohemagglutinin stimulates human mononuclear leukocytes, inducing the expression of ChAT mRNA and potentiating ACh synthesis. Phytohemagglutinin induces dose- and time-dependent toxicity in THP-1 monocytes/macrophages, alters cellular morphology, causes organelle dysfunction, and increases the expression of NF-κB, COX2, IL-1β .
|
-
- HY-B1546AR
-
|
Benzylamiloride hydrochloride (Standard)
|
Na+/Ca2+ Exchanger
Sodium Channel
Reference Standards
|
Neurological Disease
|
|
Benzamil (hydrochloride) (Standard) is the analytical standard of Benzamil (hydrochloride). This product is intended for research and analytical applications. Benzamil hydrochloride (Benzylamiloride hydrochloride), an Amiloride analogue, is a Na+/Ca2+ exchanger (NCX) inhibitor (IC50~100 nM). Benzamil hydrochloride also is a non-selective Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Benzamil hydrochloride inhibits TRPP3-mediated Ca2+-activated currents, with an IC50 of 1.1 μM .
|
-
- HY-G0021R
-
|
Norclozapine (Standard); Desmethylclozapine (Standard); Normethylclozapine (Standard)
|
Reference Standards
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
|
N-Desmethylclozapine (Standard) is the analytical standard of N-Desmethylclozapine. This product is intended for research and analytical applications. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .
|
-
- HY-14292
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
NVP-DPP728 is a potent, reversible and nitrile-dependent dipeptidyl peptidase IV (DPP-IV) inhibitor. NVP-DPP728 can inhibit human DPP-IV amidolytic activity with a Ki of 11 nM. NVP-DPP728 inhibits degradation of glucagon-like peptide-1 (GLP-1) and thereby potentiates insulin release in response to glucose intake. NVP-DPP728 can be used for researching diabetes .
|
-
- HY-120553
-
|
|
Apoptosis
|
Neurological Disease
|
|
B355252, a phenoxy thiophene sulfonamide small molecule, is a potent NGF receptor agonist. B355252 potentiates NGF-induced neurite outgrowth. B355252 protects ischemic neurons from neuronal loss by attenuating DNA damage, reducing ROS production and the LDH level, and preventing neuronal apoptosis. B355252 has anti-apoptotic effects in glutamate-induced excitotoxicity, as well as in a murine hippocampal cell line (HT22) model of Parkinson disease (PD) .
|
-
- HY-120139A
-
|
|
ASCT
|
Cancer
|
|
(R)-KMH-233 is the isomer of KMH-233 (HY-120139), and can be used as an experimental control. KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM) .
|
-
- HY-182280
-
|
|
Insulin Receptor
|
Metabolic Disease
|
|
BDM71230 is an orally active inducer of insulin-degrading enzyme (IDE), with an EC50 of 1.9 μM against human IDE. BDM71230 binds to the interface of IDE dimers and enhances the catalytic activity of IDE via steric effects. BDM71230 can potentiate the hydrolytic effect of IDE on insulin and slightly attenuate the hypoglycemic effect of insulin. BDM71230 serves as a pharmacological tool for investigating IDE function and is applicable to studies related to glucose intolerance .
|
-
- HY-N0165
-
|
|
HIV
Reverse Transcriptase
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
Methyl-Hesperidin is a glycoside compound. Methyl-Hesperidin has hypotensive, coronary dilating, smooth muscle relaxing, capillary stabilizing, choleretic, and anti-ulcer activities. Methyl-Hesperidin act as a competitive substrate to inhibit HIV-1 reverse transcriptase activity. Methyl-Hesperidin potentiates coronary dilating actions of adenine nucleotides and 3'-AMP, enhances depressant action on isolated atria, and prolongs adenosine- and ATP-induced heart block in guinea pigs .
|
-
- HY-N6733R
-
|
|
Reference Standards
DNA/RNA Synthesis
HSV
Apoptosis
Antibiotic
Orthopoxvirus
|
Infection
Inflammation/Immunology
|
|
Aphidicolin (Standard) is the analytical standard of Aphidicolin. This product is intended for research and analytical applications. Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering DNA polymerase activity. Aphidicolin is an antibiotic produced by mold Cephalosporium aphidicola, inhibits cellular deoxyribonucleic acid synthesis and the growth of herpes simplex virus. Aphidicolin exhibits anti-orthopoxvirus activity and potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line .
|
-
- HY-N8280
-
|
|
Fungal
|
Infection
|
|
IKD-8344 is a macrocyclic dilactone originally isolated from an actinomycete species and has diverse biological activities, including anticancer, antimicrobial, and anthelmintic properties. It is cytotoxic to L5178Y murine leukemia cells (IC50=0.54 ng/ml).1 IKD-8344 inhibits growth of the mycelial form of C. albicans (MIC=6.25 μg/mL) and potentiates the activity of polymyxin B against the multidrug-resistant pathogenic bacterium B. cenocepacia.
|
-
- HY-B1671R
-
|
|
Reference Standards
GABA Receptor
Sodium Channel
Calcium Channel
|
Neurological Disease
Metabolic Disease
|
|
(+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .
|
-
- HY-101165R
-
|
|
Reference Standards
iGluR
GABA Receptor
|
Neurological Disease
|
|
Cyclothiazide (Standard) is the analytical standard of Cyclothiazide. This product is intended for research and analytical applications. Cyclothiazide is a positive allosteric modulator of ionotropic AMPA-type glutamate receptors. Cyclothiazide inhibits GABAA receptors. Cyclothiazide is frequently used to produce a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Cyclothiazide can potentiate responses to kainate in hippocampal neurons. Cyclothiazide has effects on glutamatergic neurotransmission. Cyclothiazide also induces epileptiform EEG activity accompanying behavioral seizures .
|
-
- HY-111655R
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
SKA-31 (Standard) is the analytical standard of SKA-31. This product is intended for research and analytical applications. SKA-31 is a potent potassium channel activator with EC50s of 260 nM, 1.9 μM, 2.9 μM, and 2.9 μM for KCa3.1, KCa2.2, KCa2.1 and KCa2.3, respectively. SKA-31 potentiates endothelium-derived hyperpolarizing factor response and lowers blood pressure .
|
-
- HY-183666
-
|
|
nAChR
Serotonin Transporter
|
Neurological Disease
|
|
NS3956 is a blood-brain barrier-permeable human α4β2-nicotinic acetylcholine receptor (nAChR) agonist (Ki = 0.36 nM). NS3956 induces dopamine release, produces analgesic effects, modulates rotational behavior in 6-OHDA-lesioned rats, and potentiates the effects of SSRI/SNRI in the forced swim test in mice. NS3956 can be used in research related to depression, Parkinson's disease, and acute pain .
|
-
- HY-B0590
-
|
Ro 1-9569
|
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
- HY-B0590E
-
|
Ro 1-9569 mesylate
|
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
Tetrabenazine (Ro 1-9569) mesylate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine mesylate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine mesylate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine mesylate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
- HY-162472
-
|
|
ATM/ATR
DNA-PK
|
Cancer
|
|
XRD-0394 is a potent and orally active dual ATM and DNA-PKcs inhibitor with IC50s of 0.39 nM and 0.89 nM, respectively. XRD-0394 shows selectivity over other PIKK and PI3K family members. XRD-0394 significantly enhances tumor cell killing in vitro and in vivo under therapeutic ionizing radiation conditions. XRD-0394 can potentiate the effects of PARP and topoisomerase I inhibitors in vitro .
|
-
- HY-107506
-
|
|
mGluR
|
Neurological Disease
|
|
Ro 67-4853 is a positive allosteric modulator (PAM) of mGluR1 (pEC50=7.16 for rmGlu1a receptor). Ro67-4853 exhibits activity at all group I mGlu receptors including hmGlu1, rmGlu1, and rmGlu5. Ro 67-4853 enhances the potency of L-Glu by interacting with the transmembrane domain (TMD) of the receptor. Ro 67-4853 potentiates sensory synaptic responses to repetitive vibrissa stimulation .
|
-
- HY-107613R
-
|
DKGI-I (Standard); Diacylglycerol kinase inhibitor I (Standard)
|
PKC
5-HT Receptor
Reference Standards
|
Inflammation/Immunology
|
|
R 59-022 (Standard) is the analytical standard of R 59-022. This product is intended for research and analytical applications. R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
|
-
- HY-B0590A
-
|
Ro 1-9569 Racemate
|
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
Tetrabenazine (Ro 1-9569) Racemate is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine Racemate binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine Racemate weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine Racemate can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
- HY-117836
-
|
|
FAK
|
Cancer
|
|
FAK-IN-16 (compound OXA-11) is an orally active, selective focal adhesion kinase (FAK) inhibitor with an IC50 of 1.2 pM. FAK-IN-16 inhibits FAK phosphorylation at pFAK[Y397] and pFAK[Y861]. FAK-IN-16 slows tumor growth and reduces tumor vascularity, invasion. FAK-IN-16 potentiates effects of Cisplatin (HY-17394) on tumor cell proliferation and apoptosis in vitro and anti-tumor actions in mice .
|
-
- HY-A0009R
-
|
Galantamine hydrobromide (Standard)
|
nAChR
Cholinesterase (ChE)
Reference Standards
|
Neurological Disease
|
|
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-134299
-
|
8-(4-Chlorophenylthio)-cAMP-AM
|
Ras
PKA
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
8-CPT-cAMP-AM (8-(4-Chlorophenylthio)-cAMP-AM) is an Epac/PKA activator. 8-CPT-cAMP-AM potentiates glucose-dependent first- and second-phase insulin secretion, induces β-cell depolarization, modulates intracellular calcium via influx and ryanodine-sensitive store mobilization, and facilitates calcium-induced calcium release resistant to PKA inhibition. 8-CPT-cAMP-AM can be used for the research of cardiac hypertrophy, diabetic cardiomyopathy, and melanoma .
|
-
- HY-168491
-
|
|
Phosphodiesterase (PDE)
STING
PD-1/PD-L1
|
Cancer
|
|
Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC50 of 8.05 nM and low oral bioavailability. Enpp-1-IN-25 can effectively activate the intracellular STING pathway by inhibiting cGAMP degradation. Enpp-1-IN-25 can enhance immune cell infiltration in the tumor microenvironment and type I interferon responses, and potentiate the antitumor efficacy of the anti-PD-L1 antibody. Enpp-1-IN-25 can be used in the research of cancer immunotherapy .
|
-
- HY-114583
-
|
|
TRP Channel
|
Neurological Disease
|
|
AMG-8562 is a TRPV1 modulator. AMG-8562 blocks Capsaicin (HY-10448) activation of TRPV1 without affecting heat activation of TRPV1. AMG-8562 potentiates pH 5 activation of TRPV1. AMG-8562 blocks capsaicin-induced flinching behavior in pain models. AMG-8562 produces significant efficacy in CFA- and skin incision-induced thermal hyperalgesia, and in the Acetic acid (HY-Y0319)-induced writhing models .
|
-
- HY-183334
-
|
|
Phosphodiesterase (PDE)
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
TDP1-IN-5 is a tyrosyl-DNA phosphodiesterase 1 (TDP1) inhibitor with an IC50 of 2.2 μM. By targeting TDP1 both intracellularly and extracellularly, TDP1-IN-5 inhibits the NHEJ repair pathway, arrests the cell cycle at the G2/M phase, upregulates PIG3 to enhance ROS, and ultimately significantly potentiates ionizing radiation (IR)-induced DNA damage and apoptosis. TDP1-IN-5 can be used in the research of colorectal cancer .
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-
- HY-18610
-
|
Ro 8-4650 hydrochloride
|
Dopamine Transporter
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Diclofensine (Ro 8-46500) hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression .
|
-
- HY-P1345B
-
-
![[DArg10, DAla20] TLQP-21](//file.medchemexpress.com/product_pic/hy-p1345b.gif)
- HY-107613AR
-
|
DKGI-I hydrochloride (Standard); Diacylglycerol kinase inhibitor I hydrochloride (Standard)
|
Reference Standards
PKC
5-HT Receptor
|
Infection
Inflammation/Immunology
Cancer
|
|
R 59-022 hydrochloride (Standard) is the analytical standard of R 59-022 (hydrochloride) (HY-107613A). This product is intended for research and analytical applications. R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein Kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils .
|
-
- HY-B0996
-
|
NSC-17764
|
Bacterial
Fungal
|
Infection
Inflammation/Immunology
|
|
Hexetidine (NSC-17764) is an orally active antibacterial and antifungal agent with broad antibacterial and antifungal activity. Hexetidine combined with IPBC potentiates strong fungal growth inhibition properties. Hexetidine at concentrations greater than 0.1% can cause oral ulceration. Additionally, Hexetidine improves its plaque inhibiting activities combined with zinc and has been confirmed the effectiveness on purulent wound along with ultrasound. Hexetidine is a promising candidate for research in fungus-related diseases and soft tissue purulent-inflammatory
|
-
- 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-B1803A
-
|
ICI 136753 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Tracazolate (ICI 136753) hydrochloride is a potent GABAA receptor modulator. Tracazolate hydrochloride has selectivity for β3 and potentiates α1β1γ2s (EC50=13.2 μM), α1β3γ2 (EC50=1.5 μM). Tracazolate hydrochloride has the potency (EC50) determined by the nature of the third subunit (γ1-3, δ, ε) within the receptor complex. Tracazolate hydrochloride possesses anxiolytic and anticonvulsant activity .
|
-
- HY-P1210
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
Lys-γ3-MSH(human) is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
|
-
- HY-125604
-
|
|
Beta-lactamase
Bacterial
|
Infection
Inflammation/Immunology
|
|
WCK-4234 is a diazabicyclooctane β-lactamase inhibitor and susceptibility restorer. WCK-4234 lacks direct antibacterial activity. WCK-4234 inhibits class A, C, D β-lactamases and extended-spectrum β-lactamases to potentiate Imipenem (HY-B1369A) and Meropenem (HY-13678) activity against Gram-negative pathogens. WCK-4234 can be used for the research of gram-negative bacterial infections and β-lactamase-mediated carbapenem-resistant bacterial infections .
|
-
- HY-18610A
-
|
Ro 8-4650
|
Dopamine Transporter
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Diclofensine (Ro 8-46500) is an orally active neuronal monoamine uptake inhibitor. Diclofensine blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine can be used in the research of moderate to severe depression .
|
-
- HY-P1210A
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
Lys-γ3-MSH(human) TFA is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) TFA potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) TFA is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) TFA can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
|
-
- HY-168997
-
|
|
Cannabinoid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
CB1R agonist 1 is a potent, CNS-penetrant, and selective Cannabinoid-1 receptor (CB1R) agonist with a Ki of 0.95 nM, modulating Gi/o signaling. CB1R agonist 1 exhibits high selectivity over CB2R and other off-target GPCRs, including GPR55, GPR18, and GPR119. CB1R agonist 1 induces analgesia and hypothermia, and potentiates opioid analgesia in mice. CB1R agonist 1 can be used for the research of pain .
|
-
- HY-177512
-
|
|
FLAP
|
Cancer
|
|
MSC778 is an effective and orally active flap endonuclease 1 (FEN1) inhibitor with an IC50 of 3 nM and a KD of 2.9 nM. MSC778 exhibits 145-fold, 516-fold, and 65-fold selectivity over EXO1, GEN1, and XPG, respectively. MSC778 selectively kills BRCA2-deficient cells and potentiates the activity of Niraparib (HY-10619) to induce tumor stasis in a BRCA2 KO DLD-1 mouse xenograft. MSC778 can be used in the research of colorectal cancer .
|
-
- HY-18610R
-
|
Ro 8-4650 hydrochloride (Standard)
|
Reference Standards
Dopamine Transporter
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Diclofensine (Ro 8-4650) hydrochloride (Standard) is the analytical standard of Diclofensine hydrochloride. This product is intended for research and analytical applications. Diclofensine hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression.
|
-
- HY-180802
-
|
|
Mas-related G-protein-coupled Receptor (MRGPR)
|
Neurological Disease
|
|
BCFTP is a potent, orally active and selective human Mas-related G protein-coupled receptor X1 (MrgprX1)-positive allosteric modulator. BCFTP selectively potentiates MrgprX1 signaling in HEK293 cells. BCFTP alleviates specific neuropathic pain-related behaviors in a humanized MrgprX1 mouse model of chronic constrictive injury (CCI) in a MrgprX1-dependent manner. BCFTP synergistically enhances psychoactive substances analgesia in CCI MrgprX1 mice. BCFTP can be used for neuropathic pain research .
|
-
- HY-B0881
-
|
|
Potassium Channel
|
Metabolic Disease
Cancer
|
|
Acetohexamide is an orally active first-generation sulfonylurea agent used in research related to type 2 diabetes and cancer. Acetohexamide exerts reductase activity in human erythrocytes. Acetohexamide stimulates the pancreas to secrete insulin. Acetohexamide inhibits ATP-sensitive potassium channels in the β cells of the pancreas. Acetohexamide can inhibit the formation of circular chemorepellent induced defects (CCIDs) in lymphendothelial cell (LEC) monolayers. Acetohexamide inhibits markers of epithelial-to-mesenchymal-transition and migration. Acetohexamide suppresses the synthesis of 12(S)-HETE. Acetohexamide can potentiate hypoglycaemic action .
|
-
- HY-B1692
-
|
MSX; MSO
|
Glutaminase
|
Neurological Disease
|
|
L-Methionine-DL-sulfoximine (MSX; MSO), a highly specific and irreversible inhibitor of Glutamine synthetase (GS), is also a potent convulsant which metabolically and morphologically primarily affects astroglia. L-Methionine-DL-sulfoximine has been employed to inhibit the Gln-dependent ammonia-stimulated neuronal toxicity in vitro, potentiating Gln deficit-dependent depression. L-Methionine-DL-sulfoximine tremendously increases the rate of release of fixed nitrogen in cyanobacteria. L-Methionine-DL-sulfoximine is a promising candidate for research in biofertilizers and convulsive seizures (CS) .
|
-
- HY-10289
-
|
RO-4876904
|
Dipeptidyl Peptidase
GLP Receptor
P-glycoprotein
|
Metabolic Disease
|
|
Carmegliptin (RO-4876904) is an orally active and potent DPP IV inhibitor with a human DPP IV IC50 of 6.8 nM. Carmegliptin binds to the S1 pocket of DPP IV, blocks the degradation of GLP 1, potentiates endogenous GLP 1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin acts as a substrate for human P glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin can be used for the research of type 2 diabetes, non insulin dependent diabetes mellitus .
|
-
- HY-100403R
-
|
|
mGluR
Reference Standards
|
Cancer
|
|
Ro 67-7476 (Standard) is the analytical standard of Ro 67-7476 (HY-100403). This product is intended for research and analytical applications. Ro 67-7476 is a potent positive allosteric modulator of mGluR1 and potentiates glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a with an EC50 of 60.1 nM . Ro 67-7476 is a potent P-ERK1/2 agonist and activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50=163.3 nM) .
|
-
- HY-185007
-
|
|
GABA Receptor
|
Neurological Disease
|
|
LI-633 is a selective and orally active GABAA receptor positive allosteric modulator (PAM) with a Ki of 21 nM. LI-633 produces robust potentiation of GABA-induced inward current, with EC50 values ranging from 8 nM (α5β2γ2) to 128 nM (α3β2γ2). LI-633 potentiates muscimol-induced GABAergic currents in rat dorsal root ganglion (DRG) neurons with an EC50 of 70.4 nM. LI-633 can be used for the study of visceral pain .
|
-
- HY-108292
-
|
|
NF-κB
|
Neurological Disease
Cancer
|
|
Propacetamol hydrochloride is an orally active prodrug of paracetamol and an inducer of acute liver injury models, with multiple properties including antinociception, antioxidation and gastroprotection. Propacetamol hydrochloride potentiates Tramadol and attenuates Aspirin (HY-14654)-induced gastric mucosal damage and lipid peroxidation. Under specific conditions, Propacetamol hydrochloride also acts as a hepatotoxic inducer, triggering acute liver injury, oxidative stress and apoptosis, with strain differences in toxicity sensitivity. Propacetamol hydrochloride can be used in the research of acute liver injury, drug-induced hepatotoxicity and gastric mucosal damage .
|
-
- HY-10289A
-
|
RO-4876904 hydrochloride
|
Dipeptidyl Peptidase
GLP Receptor
P-glycoprotein
|
Metabolic Disease
|
|
Carmegliptin hydrochloride (RO-4876904 hydrochloride) is an orally active and potent DPP‑IV inhibitor with a human DPP‑IV IC50 of 6.8 nM. Carmegliptin hydrochloride binds to the S1 pocket of DPP‑IV, blocks the degradation of GLP‑1, potentiates endogenous GLP‑1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin hydrochloride acts as a substrate for human P‑glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin hydrochloride can be used for the research of type 2 diabetes, non‑insulin‑dependent diabetes mellitus .
|
-
- HY-B1811AS1
-
|
Arginine vasopressin-d5 TFA; Antidiuretic hormone-d5 TFA
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Vasopressin-d5 TFA is the TFA salt form of Vasopressin-d5 (HY-B1811S1). Vasopressin-d5 TFA is an isotope-labeled compound of Vasopressin (HY-B1811). Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of the corticotropin-releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
|
-
- HY-116819
-
|
|
GCGR
|
Neurological Disease
Metabolic Disease
|
|
VU0453379 is a blood-brain barrier permeable GLP-1R positive allosteric modulator (PAM) with an EC50 value of 1.3 μM. VU0453379 potentiates the actions of endogenous GLP-1 and synthetic peptide agonists, and promotes GLP-1 receptor internalization. VU0453379 stimulates insulin secretion from primary mouse islets. VU0453379 enhances the function of endogenous GLP-1R and reverses catalepsy in animal models. VU0453379 is useful for research on Parkinson's disease and type 2 diabetes .
|
-
- HY-118301
-
|
|
GABA Receptor
5-HT Receptor
|
Neurological Disease
|
|
ADX71441 is an orally active, blood-brain barrier penetrant positive allosteric modulator of GABAB receptor. ADX71441 potentiates the activity of endogenous GABA at GABAB receptor, with an EC50 of 96 nM. ADX71441 functionally inhibits adenosine transporters and 5-HT2B receptor. ADX71441 produces anxiolytic-like, analgesic, muscle relaxant, hypothermic and overactive bladder inhibitory effects, reduces acute locomotor activity levels, decreases voluntary intake of alcohol and saccharin, attenuates stress-induced neuronal activation, and exhibits anti-hyperalgesic activity .
|
-
- HY-P1345C
-
|
|
Drug Derivative
Complement System
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
[DArg10, Aib20] TLQP-21, TLQP-21 (HY-P1345) analogue, is a C3aRpartial agonist, C3aR functional antagonist (EC50: 854 nM for β-arrestin recruitment). [DArg10, Aib20] TLQP-21 shows no significant calcium flux activity. [DArg10, Aib20] TLQP-21 shows no activity in potentiating adrenergic-induced lipolysis. [DArg10, Aib20] TLQP-21 can be used in the research of inflammatory diseases, metabolic disorders, and neurological conditions .
|
-
![[DArg10, Aib20] TLQP-21](//file.medchemexpress.com/product_pic/hy-p1345c.gif)
- HY-120184
-
|
AZ13713945
|
mAChR
|
Neurological Disease
|
|
VU0467485 (AZ13713945) is a potent, selective, and orally bioavailable muscarinic acetylcholine receptor 4 (M4) positive allosteric modulator (PAM). VU0467485 (AZ13713945) potentiates activity of ACh at M4 with EC50s of 26.6 nM and 78.8 nM at rat and human M4 receptors, respectively. VU0467485 (AZ13713945) shows selectivity for M4 over human and rat M1/2/3/5. VU0467485 (AZ13713945) displays moderate to high CNS penetration. VU0467485 (AZ13713945) has antipsychotic-like activity .
|
-
- HY-125604A
-
|
|
Beta-lactamase
Bacterial
|
Infection
Inflammation/Immunology
|
|
WCK-4234 free base is a diazabicyclooctane β-lactamase inhibitor and susceptibility restorer. WCK-4234 free base lacks direct antibacterial activity. WCK-4234 free base inhibits class A, C, D β-lactamases and extended-spectrum β-lactamases to potentiate Imipenem (HY-B1369A) and Meropenem (HY-13678) activity against Gram-negative pathogens. WCK-4234 free base can be used for the research of gram-negative bacterial infections and β-lactamase-mediated carbapenem-resistant bacterial infections .
|
-
- HY-B0590S
-
|
Ro 1-9569-d6
|
Monoamine Transporter
|
Neurological Disease
|
|
Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
- HY-B0590R
-
|
Ro 1-9569 (Standard)
|
Reference Standards
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
Tetrabenazine (Standard) is the analytical standard of Tetrabenazine (HY-B0590). This product is intended for research and analytical applications. Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
- HY-103645R
-
|
|
Reference Standards
Bacterial
Aurora Kinase
Apoptosis
|
Infection
Cancer
|
|
GW779439X (Standard) is the analytical standard of GW779439X (HY-103645). This product is intended for research and analytical applications. GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway . MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
|
-
- HY-101366
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
A-61603 is a selective α1A/α1a-adrenergic receptor agonist with Ki of 8.89 nM for rat submaxillary gland α1A, Ki of 30.5 nM for cloned bovine α1a. A-61603 potentiates Ca 2+ transients with EC50 of 6.9 nM. A-61603 stimulates phosphoinositide hydrolysis, induces contractile responses in vas deferens, prostate strips, and spleen strips, and exhibits low activity in aortic rings. A-61603 can be used for research on adrenergic function .
|
-
- HY-W016412
-
-
- HY-18610S
-
|
|
Isotope-Labeled Compounds
Dopamine Transporter
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
|
Diclofensine-d3 (Ro-8-4650-d3) hydrochloride is the deuterium labeled Diclofensine hydrochloride. Diclofensine hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression.
|
-
- HY-N0165R
-
|
|
Reference Standards
HIV
Reverse Transcriptase
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
Methyl-Hesperidin (Standard) is the analytical standard of Methyl-Hesperidin (HY-N0165). This product is intended for research and analytical applications. Methyl-Hesperidin is a glycoside compound. Methyl-Hesperidin has hypotensive, coronary dilating, smooth muscle relaxing, capillary stabilizing, choleretic, and anti-ulcer activities. Methyl-Hesperidin act as a competitive substrate to inhibit HIV-1 reverse transcriptase activity. Methyl-Hesperidin potentiates coronary dilating actions of adenine nucleotides and 3'-AMP, enhances depressant action on isolated atria, and prolongs adenosine- and ATP-induced heart block in guinea pigs .
|
-
- HY-B0881R
-
|
|
Reference Standards
Potassium Channel
|
Metabolic Disease
Cancer
|
|
Acetohexamide (Standard) is the analytical standard of Acetohexamide. This product is intended for research and analytical applications. Acetohexamide is an orally active first-generation sulfonylurea agent used in research related to type 2 diabetes and cancer. Acetohexamide exerts reductase activity in human erythrocytes. Acetohexamide stimulates the pancreas to secrete insulin. Acetohexamide inhibits ATP-sensitive potassium channels in the β cells of the pancreas. Acetohexamide can inhibit the formation of circular chemorepellent induced defects (CCIDs) in lymphendothelial cell (LEC) monolayers. Acetohexamide inhibits markers of epithelial-to-mesenchymal-transition and migration. Acetohexamide suppresses the synthesis of 12(S)-HETE. Acetohexamide can potentiate hypoglycaemic action .
|
-
- HY-119468
-
|
|
Dopamine Transporter
|
Neurological Disease
|
|
Medifoxamine is an orally active monoamine reuptake inhibitor and antidepressant. Medifoxamine preferentially inhibits presynaptic dopamine reuptake. Medifoxamine acts as an intraocular pressure-lowering agent to reduce intraocular pressure, and also functions as a miotic agent to decrease pupil diameter. Medifoxamine exhibits characteristic properties of antidepressant compounds, including preventing hypothermia induced by Reserpine (HY-N0480) or Apomorphine (HY-12723), potentiating the toxic effects of Yohimbine (HY-N0127) in mice, and reducing immobility behavior in mice and rats in the "behavioral despair" model. Medifoxamine has no anticholinergic activity. Medifoxamine can be used in research related to depression .
|
-
- HY-182401
-
|
|
ERK
Akt
|
Neurological Disease
|
|
NS-417 free base is an ERK1, ERK2, and Akt kinase activator with neuroprotective, neurite outgrowth potentiating, and dopaminergic cell population enhancing activity. NS-417 free base enhances activation of ERK1, ERK2, and Akt kinase via growth factor stimulation. NS-417 free base rescues cells from growth factor withdrawal-induced death, stimulates neurite outgrowth, increases tyrosine hydroxylase-positive cell counts, and displays neurotrophic-like activity in in vitro models. NS-417 free base can be used for the research of parkinson’s disease .
|
-
- HY-171844
-
|
|
iGluR
|
Neurological Disease
Inflammation/Immunology
|
|
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-P991444
-
|
|
NTPDase
ATP Synthase
|
Inflammation/Immunology
Cancer
|
|
IPH5201 is a selective CD39 inhibitor and a humanized IgG1 monoclonal antibody. IPH5201 selectively binds to and inhibits the enzymatic activity of both membrane-bound and soluble CD39, blocking ATP hydrolysis. IPH5201 enhances the phenotypic maturation and activation of dendritic cells and macrophages. IPH5201 potentiates the anti-tumor effect of Oxaliplatin (HY-17371). IPH5201 shows preliminary evidence of disease stabilization in advanced solid tumor models when used as a single agent or in combination with Durvalumab (HY-P9919). IPH5201 can be used for the research of advanced solid tumors .
|
-
- HY-109008
-
|
OP0595 free acid
|
Beta-lactamase
Bacterial
|
Infection
|
|
Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and C β-lactamases. Nacubactam acts as a penicillin binding protein (PBP) 2-active antibacterial, and gives β-lactamase-independent potentiation of β-lactams targeting other PBPs. Nacubactam potentiates the antimicrobial activities of Piperacillin (HY-B1923), Cefepime (HY-B0692), and Meropenem (HY-13678) against CTX-M-15-positive Escherichia coli and KPC-positive Klebsiella pneumoniae .
|
-
- HY-180398
-
|
|
PPAR
PGC-1α
|
Metabolic Disease
|
|
PA-082 is a selective PPAR-γ modulator that functions as a partial agonist. PA-082 causes partial recruitment of SRC1, TIF2, SRC3 and full recruitment of PGC1-α to PPAR-γ ligand-binding domain. PA-082 prevents triglyceride accumulation during de novo adipogenesis and antagonizes Rosiglitazone (HY-17386)-induced lipid accumulation. PA-082 potentiates insulin-stimulated glucose uptake in adipocytes and protects against TNFα-induced insulin resistance. PA-082 can be used for the research of type 2 diabetes .
|
-
- HY-150105
-
|
BMF-219; Menin-MLL inhibitor 21
|
Epigenetic Reader Domain
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Icovamenib (BMF-219) is a selective, orally active, irreversible Menin inhibitor. Icovamenib forms a stable and irreversible covalent bond with Menin. Icovamenib promotes selective and controlled proliferation of beta cells and improvement of beta cell function in ex vivo human islet cultures. Icovamenib enhances glycemic control in animal diabetic models. Icovamenib induces a dose-dependent enhancement in insulin secretion potentiated by the GLP-1 RA. Icovamenib can be used for the study of multiple hematologic malignancies, solid tumors, and diabetes mellitus, such as diffuse large B-cell lymphoma (DLBCL), multiple myeloma (MM) and chronic lymphocytic leukemia and type 2 diabetes .
|
-
- HY-182850
-
|
|
CXCR
|
Metabolic Disease
|
|
UCUF-965 is a CXCR4 positive allosteric modulator. UCUF-965 potentiates CXCL12-induced β-arrestin recruitment and cAMP signaling, activates lymphoblast migration, induces calcium flux, and does not bind CXCR4’s orthosteric CXCL12 site. UCUF-965 reduces miR-15b and miR-29a levels, increases miR-146a levels in fibroblasts. UCUF-965 enhances angiogenesis and reduces wound healing time in diabetic mice. UCUF-965 can be used for the research of diabetic wound healing impairment .
|
-
- HY-175670
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy .
|
-
- HY-179573
-
|
|
iGluR
|
Neurological Disease
|
|
UCM-A86 is a selective positive allosteric modulator of GluN1/GluN3 NMDA receptors with EC50 values of 21 µM and 19 µM at GluN1/GluN3A and GluN1/GluN3B receptors, respectively. UCM-A86 selectively potentiates responses from GluN1/GluN3A/B over GluN1/GluN2A-D receptors. UCM-A86 can be used in the research of central nervous system diseases .
|
-
- HY-B0590S3
-
|
TBZ-d7-d7; Ro 1-9569-d7
|
Isotope-Labeled Compounds
Monoamine Transporter
Dopamine Receptor
|
Neurological Disease
|
|
Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
- HY-16639
-
|
|
GPR35
Neurotensin Receptor
|
Neurological Disease
Endocrinology
|
|
ML314 is a potent, BBB-penetrant and β-arrestin biased molecule agonist of NTR1 (EC50 = 1.9 μM). ML314 shows good selectivity against NTR2 and GPR35, but does not stimulate Ca2+ mobilization. ML314 can attenuate amphetamine-like hyperlocomotion in dopamine transporter knockout mice. ML314 attenuates methamphetamine-associated hyperlocomotion and potentiates the psychostimulant inhibitory effects of a ghrelin antagonist in wild type mouse model. ML314 also acts as an allosteric enhancer of endogenous neurotensin. ML314 antagonizes G protein signaling. ML314 can be studied in research for methamphetamine abuse conditions .
|
-
- HY-P2196A
-
|
|
Apelin Receptor (APJ)
|
Cancer
|
|
ELA-32(human) TFA is a potent, high affinity apelin receptor agonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells.
|
-
- 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-W013150
-
|
|
GABA Receptor
|
Neurological Disease
|
|
Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions .
|
-
- HY-109008R
-
|
OP0595 free acid (Standard)
|
Beta-lactamase
Reference Standards
Bacterial
|
Infection
|
|
Nacubactam (Standard) is the analytical standard of Nacubactam (HY-109008). This product is intended for research and analytical applications. Nacubactam (OP0595 free acid) is a potent non-β-lactam-β-lactamase inhibitor with activity against class A and C β-lactamases. Nacubactam acts as a penicillin binding protein (PBP) 2-active antibacterial, and gives β-lactamase-independent potentiation of β-lactams targeting other PBPs. Nacubactam potentiates the antimicrobial activities of Piperacillin (HY-B1923), Cefepime (HY-B0692), and Meropenem (HY-13678) against CTX-M-15-positive Escherichia coli and KPC-positive Klebsiella pneumoniae .
|
-
- HY-W013150R
-
|
|
Reference Standards
GABA Receptor
|
Neurological Disease
|
|
Alpidem (Standard) is the analytical standard of Alpidem (HY-W013150). This product is intended for research and analytical applications. Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.
|
-
- HY-123489S
-
|
THDOC-d3
|
GABA Receptor
|
Neurological Disease
|
|
3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
|
-
- HY-173163
-
|
|
Bacterial
|
Infection
|
|
(E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) (Compound 4a) is a Gram-negative outer membrane permeabilizer with synergistic antibacterial activity through the blockage on LptA/LptC interaction via targeting Met47 in LptA. (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) potentiates pol B against both wild-typed and MDR A. baumannii and E. coli strains. (E)-2,6-Di-tert-butyl-4-(4-(diethylamino)styryl)pyrylium (trifluoromethanesulfonate) can be used as antibiotic adjuvants against MDR Gram-negative bacteria .
|
-
- HY-W013150S
-
|
|
Isotope-Labeled Compounds
GABA Receptor
|
Neurological Disease
|
|
Alpidem-d14 is the deuterium labeled Alpidem (HY-W013150) . Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.
|
-
- HY-120105
-
|
|
DNA/RNA Synthesis
Apoptosis
MDM-2/p53
Bcl-2 Family
Caspase
PARP
|
Cancer
|
|
NSC666715 is a DNA polymerase β (Pol-β) inhibitor. NSC666715 directly and specifically interacts with Pol-β, interferes with its binding to damaged DNA, blocks its dRP lyase activity, and inhibits Pol-β-mediated SN- and LP-BER. NSC666715 induces AP site accumulation and S-phase cell cycle arrest, and triggers senescence and apoptosis (apoptosis) via the p53/p21 pathway in colorectal cancer cells. NSC666715 enhances TMZ (HY-17364)-induced DNA damage, senescence and apoptosis, and potentiates the cytotoxicity of TMZ. NSC666715 inhibits tumor growth in colon cancer xenograft models. NSC666715 can be used in research related to colorectal cancer .
|
-
- HY-N17845
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
3,3'-Dihydroxy-2,6-bis(4-hydroxybenzyl)-5-methoxybibenzyl, a stilbenoid compound, is a tubulin inhibitor with an IC50 of 10 μM. 3,3'-Dihydroxy-2,6-bis(4-hydroxybenzyl)-5-methoxybibenzyl inhibits tubulin polymerization. 3,3'-Dihydroxy-2,6-bis(4-hydroxybenzyl)-5-methoxybibenzyl functions as a potentiator that potentiates SN-38 (HY-13704) cytotoxicity in BCRP-transduced cancer cells. 3,3'-Dihydroxy-2,6-bis(4-hydroxybenzyl)-5-methoxybibenzyl can be used for the study of breast cancer .
|
-
- HY-180245
-
|
|
STAT
Ferroptosis
Apoptosis
Glutathione Peroxidase
Bcl-2 Family
Reactive Oxygen Species (ROS)
|
Cancer
|
|
STAT3-IN-51 is a STAT3 inhibitor that directly binds to the STAT3 SH2 domain. STAT3-IN-51 induces apoptosis, ferroptosis, and immunogenic cell death (ICD) to potentiate anti-tumor immunity. STAT3-IN-51 inhibits STAT3 activation (phosphorylation, p-STAT3) and its downstream signaling. STAT3-IN-51 induces ROS generation, decreases Bcl-2 expression, disruptes mitochondrial function, suppresses GPX4 activity, and promotes lipid peroxidation. STAT3-IN-51 can be used for the study of colorectal carcinoma, breast adenocarcinoma, non-small cell lung cancer (NSCLC) and Cisplatin (HY-17394)-resistant pulmonary adenocarcinoma .
|
-
- HY-182707
-
|
|
nAChR
Interleukin Related
TNF Receptor
NF-κB
|
Neurological Disease
|
|
JWX-A0108 is a selective human α7 nAChR positive allosteric modulator with an EC50 of 4.35 μM. JWX-A0108 potentiates α7 nAChR currents only in the presence of acetylcholine, with no direct activating effect or alteration of desensitization. JWX-A0108 enhances hippocampal GABAergic synaptic transmission by increasing spontaneous inhibitory postsynaptic currents. JWX-A0108 reduces the brain expression levels of IL-1β, TNF-α, and IL-6 by blocking the NF-κB signaling pathway, and reduces microglial activation by downregulating Iba1. JWX-A0108 effectively improves cognitive deficits, neuroinflammation, and hippocampal neuronal damage in mouse models of schizophrenia and Alzheimer's disease. JWX-A0108 can be used for research related to schizophrenia and Alzheimer's disease .
|
-
- HY-171936
-
|
GM1 (d18:1/C18:0) ammonium; C18 Ganglioside GM1 (d18:1/18:0) ammonium
|
Endogenous Metabolite
|
Neurological Disease
|
|
Ganglioside GM1 (ammonium) is a monosialylated ganglioside and the prototypic ganglioside for those containing one sialic acid residue. Ganglioside GM1 (ammonium) is one of the most abundant gangliosides in the brain which provides neuroprotection. Ganglioside GM1 (ammonium) exhibits anti-inflammatory property. Ganglioside GM1 (ammonium) has a well-balanced amphiphilic behavior. Ganglioside GM1 (ammonium) can reduce the fluidity of the plasma membrane that implies a retention and enrichment of the ganglioside in specific membrane domains that are called lipid rafts. Ganglioside GM1 (ammonium) can modify the process of differentiation, amplifies responses to neurotrophic factors, protects against excitatory amino acid-related neurotoxicity. Ganglioside GM1 (ammonium) can alleviate acute nerve cell damage through blocking cytotoxicity and potentiating neurotophic factors. Ganglioside GM1 (ammonium) can be studied in neurodegenerative diseases such as Alzheimer’s disease .
|
-
- HY-179372
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin polymerization-IN-84 inhibits tubulin polymerization by targeting the colchicine-binding pocket, with anIC50 = 10.9 μM. Tubulin polymerization-IN-84 shows antiproliferative activity against Jurkat, B16-F10, HCT116, and MDA-MB-231 cells (IC50 = 60 nM, 380 nM, 138 nM, and 1.054 μM). Tubulin polymerization-IN-84 induces G2/M-phase arrest and apoptosis in B16-F10 cells. Tubulin polymerization-IN-84 suppresses tumor growth in a B16-F10 melanoma model and potentiates anti-tumor immunity in combination with a PD-L1 mAb for the research of T-cell acute lymphoblastic leukemia, melanoma, colon cancer, and breast cancer.
|
-
- HY-123597
-
|
DDUG; NCI C04808
|
Autophagy
Checkpoint Kinase (Chk)
|
Cancer
|
|
NSC 109555 is an ATP-competitive inhibitor of checkpoint kinase 2 (Chk2; IC50=200 nM in a cell-free kinase assay). It is selective for Chk2 over Chk1 and 16 kinases in a panel but does inhibit Brk, c-Met, IGFR, and LCK with IC50 values of 210, 6,000, 7,400, and 7,100 nM, respectively. NSC 109555 inhibits Chk2 autophosphorylation and phosphorylation of the Chk2 substrate histone H1 in vitro (IC50=240 nM). It inhibits the growth of, and induces autophagy in, L1210 leukemia cells in vitro.2 NSC 109555 (1,250 nM) potentiates gemcitabine-induced cytotoxicity in MIA PaCa-2, CFPAC-1, PANC-1, and BxPC-3 pancreatic cancer cells, as well as reduces gemcitabine-induced increases in Chk2 phosphorylation and enhances gemcitabine-induced production of reactive oxygen species (ROS) in MIA PaCa-2 cells.
|
-
- HY-182091
-
|
|
5-HT Receptor
Dopamine Receptor
Dopamine Transporter
Adrenergic Receptor
Calcium Channel
|
Neurological Disease
|
|
CYD-1-79 is a selective positive allosteric modulator of 5-HT2C receptor. CYD-1-79 potentiates 5-HT-evoked intracellular calcium release via a topographically distinct allosteric site. CYD-1-79 shows significant inhibition of binding at dopamine D3 receptor, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 modulates 5-HT2C receptor-mediated spontaneous ambulation in rodents and synergizes with a low dose of a 5-HT2C receptor agonist. CYD-1-79 attenuates relapse vulnerability of psychoactive substance in a rodent self-administration model. CYD-1-79 can be used for the research of neurological disease .
|
-
- HY-112288
-
C188-9
Maximum Cited Publications
32 Publications Verification
TTI-101
|
STAT
Apoptosis
DNA Methyltransferase
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
C188-9 (TTI-101) is a STAT3 inhibitor with a Kd value of 4.7 nM. C188-9 targets the SH2 domain of STAT3, blocks the processes of STAT3 ligand binding, receptor recruitment, homodimerization and phosphorylation, and regulates STAT3-mediated genes associated with tumorigenesis and radioresistance. C188-9 regulates STAT1-mediated genes related to radioresistance and reduces the activation level of STAT1. C188-9 downregulates the expression of DNMT1, enhances DAC-induced demethylation and re-expression of RASSF1A, and simultaneously potentiates the anti-tumor effect of DAC on pancreatic cancer cells. C188-9 inhibits both anchorage-dependent and anchorage-independent growth of cancer cells, induces Apoptosis, blocks the growth of tumor xenografts, and suppresses muscle atrophy. C188-9 maintains muscle mass, increases body weight and improves grip strength in tumor-bearing mice. C188-9 can be used in research related to head and neck squamous cell carcinoma, pancreatic cancer, sepsis-related skeletal muscle wasting, non-small cell lung cancer, acute myeloid leukemia and cancer cachexia .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-Y0669
-
|
|
Biochemical Assay Reagents
|
|
Pipecolic acid is an orally bioavailable, blood-brain barrier-permeable metabolite of lysine with antioxidant, inhibitor, and inducer activity. Pipecolic acid modulates the YAP-GPX4 signaling pathway, reduces retinal vascular tube formation, and mitigates ferroptosis. Pipecolic acid potentiates voltage-sensitive Ca 2+ channel currents and induces neuronal apoptosis. Pipecolic acid can be used for the research of diabetic retinopathy .
|
-
- HY-W016412
-
|
CoQ0
|
Biochemical Assay Reagents
|
|
Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-B1811
-
|
Arginine vasopressin; Antidiuretic hormone
|
Endogenous Metabolite
|
Neurological Disease
|
|
Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
|
-
- HY-P2196A
-
|
|
Apelin Receptor (APJ)
|
Cancer
|
|
ELA-32(human) TFA is a potent, high affinity apelin receptor agonist (IC50=0.27 nM; Kd=0.51 nM). ELA-32(human) TFA exhibits no binding GPR15 and GPR25. ELA-32(human) TFA activates the PI3K/AKT pathway and promotes self-renewal of hESCs via cell-cycle progression and protein translation. ELA-32(human) TFA also potentiates the TGFβ pathway, priming hESCs toward the endoderm lineage. ELA-32(human) TFA stimulates angiogenesis in HUVEC cells.
|
-
- HY-P4685
-
|
|
Angiotensin Receptor
|
Metabolic Disease
|
|
(Sar1,Ile4,8)-Angiotensin II is a functionally selective angiotensin II type 1 receptor (AT1R) agonist. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated insulin receptor (IR) signaling and glycogen synthesis. (Sar1,Ile4,8)-Angiotensin II potentiates insulin-stimulated phosphorylation of Akt and GSK3α/β .
|
-
- HY-P3985
-
|
Bradykinin potentiating peptide B
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Others
|
|
Bradykinin potentiator B (Bradykinin potentiating peptide B) is venom of Agkistrodon halys blomhoffi. Bradykinin potentiator B is a potent ACE inhibitor. Bradykinin potentiator inhibits the activity of bradykinin inhibitory peptidase .
|
-
- HY-P2619
-
-
- HY-P1257
-
|
|
Insulin Receptor
Neurotensin Receptor
|
Metabolic Disease
|
|
Xenin-8, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
|
-
- HY-B1811R
-
|
Arginine vasopressin (Standard); Antidiuretic hormone (Standard)
|
Endogenous Metabolite
Reference Standards
|
Neurological Disease
|
|
Vasopressin (Standard) is the analytical standard of Vasopressin. This product is intended for research and analytical applications. Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
|
-
- HY-P3969
-
-
- HY-P3578
-
|
|
Insulin Receptor
|
Endocrinology
|
|
Gastric Inhibitory Polypeptide (1-30), porcine lacks the C-terminal 12 amino acid residues of natural gastric inhibitory polypeptide (GIP), exhibits biologic activity by potentiating the release of insulin and somatostatin .
|
-
- HY-P4012
-
|
|
Vasopressin Receptor
|
Endocrinology
|
|
[Asu1,6-Arg8]Vasopressin is an vasopressin agonist which potentiates cyclic AMP accumulation and ACTH release induced by corticotropin-releasing factor (CRF) in rat anterior pituitary cells in culture .
|
-
- HY-P1257A
-
|
|
Neurotensin Receptor
|
Metabolic Disease
|
|
Xenin-8 TFA, a C-terminal octapeptide, is a biologically active fragment of Xenin. Xenin is a 25-amino acid peptide of the neurotensin/xenopsin family. Xenin-8 TFA stimulates basal insulin secretion and potentiates the insulin response to glucose in a dose-dependent manner (EC50=0.16 nM) .
|
-
- HY-P5172
-
|
|
Sodium Channel
|
Neurological Disease
|
|
MitTx-alpha is a subunit of MitTx. MitTx is a potent, persistent, and selective agonist for acid-sensing ion channels (ASICs). MitTx is highly selective for the ASIC1 subtype at neutral pH; under more acidic conditions (pH<6.5), MitTx massively potentiates (>100-fold) proton-evoked activation of ASIC2a channels .
|
-
- HY-P5780
-
|
|
Sodium Channel
|
Neurological Disease
|
|
π-TRTX-Hm3a is a 37-amino acid peptide isolated from Togo starburst tarantula (Heteroscodra maculata) venom. π-TRTX-Hm3a pH-dependently inhibits acid-sensing ion channel 1a (ASIC1a) with an IC50 of 1-2 nM and potentiates ASIC1b with an EC50 of 46.5 nM .
|
-
- HY-P1210
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
Lys-γ3-MSH(human) is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
|
-
- HY-P1210A
-
|
|
Melanocortin Receptor
|
Endocrinology
|
|
Lys-γ3-MSH(human) TFA is a melanocortin peptide derived from the C-terminal of the fragment of pro-opiomelanocortin (POMC). Lys-γ3-MSH(human) TFA potentiates the steroidogenic response of the rat adrenal to adrenocorticotrophin (ACTH). Lys-γ3-MSH(human) TFA is a potent stimulator of lipolysis with an apparent EC50 of 3.56 nM. Lys-γ3-MSH(human) TFA can activate hormone sensitive lipase (HSL) and Perilipin A resulting in lipolysis .
|
-
- HY-P1345B
-
-
- HY-P1345C
-
|
|
Drug Derivative
Complement System
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
[DArg10, Aib20] TLQP-21, TLQP-21 (HY-P1345) analogue, is a C3aRpartial agonist, C3aR functional antagonist (EC50: 854 nM for β-arrestin recruitment). [DArg10, Aib20] TLQP-21 shows no significant calcium flux activity. [DArg10, Aib20] TLQP-21 shows no activity in potentiating adrenergic-induced lipolysis. [DArg10, Aib20] TLQP-21 can be used in the research of inflammatory diseases, metabolic disorders, and neurological conditions .
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| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P991444
-
|
|
NTPDase
ATP Synthase
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Inflammation/Immunology
Cancer
|
|
IPH5201 is a selective CD39 inhibitor and a humanized IgG1 monoclonal antibody. IPH5201 selectively binds to and inhibits the enzymatic activity of both membrane-bound and soluble CD39, blocking ATP hydrolysis. IPH5201 enhances the phenotypic maturation and activation of dendritic cells and macrophages. IPH5201 potentiates the anti-tumor effect of Oxaliplatin (HY-17371). IPH5201 shows preliminary evidence of disease stabilization in advanced solid tumor models when used as a single agent or in combination with Durvalumab (HY-P9919). IPH5201 can be used for the research of advanced solid tumors .
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(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N7038
-
-
-
- HY-N6733
-
-
-
- HY-B0089
-
-
-
- HY-B1811
-
-
-
- HY-N7426
-
-
-
- HY-A0009
-
|
Galantamine hydrobromide
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Alkaloids
Other Alkaloids
Plants
Amaryllidaceae
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Cholinesterase (ChE)
nAChR
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
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-
-
- HY-N0165
-
-
-
- HY-B1671
-
-
-
- HY-N125722
-
-
-
- HY-N1944A
-
-
-
- HY-B0089R
-
-
-
- HY-N3995
-
-
-
- HY-117517
-
-
-
- HY-W654264
-
-
-
- HY-167825
-
-
-
- HY-B1811R
-
|
Arginine vasopressin (Standard); Antidiuretic hormone (Standard)
|
Structural Classification
Cyclopeptides
Endogenous metabolite
Source Classification
|
Endogenous Metabolite
Reference Standards
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|
Vasopressin (Standard) is the analytical standard of Vasopressin. This product is intended for research and analytical applications. Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis, and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of corticotropin releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
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-
-
- HY-N15846
-
|
|
Structural Classification
Lipid
|
Drug Derivative
|
|
VSA 1, a semisynthetic QS-21 (HY-101092) analog, is a saponin adjuvant. VSA 1 potentiates antigen-specific IgG1 and IgG2a immune responses in BALB/c mice, indicating a mixed Th1/Th2 immune response. VSA 1 significantly improves vaccine efficacy after primary immunization and enhances homologous protection .
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-
-
- HY-N6733R
-
-
-
- HY-A0009R
-
|
Galantamine hydrobromide (Standard)
|
Structural Classification
Alkaloids
Other Alkaloids
Plants
Amaryllidaceae
Source Classification
|
nAChR
Cholinesterase (ChE)
Reference Standards
|
|
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
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-
-
- HY-N15081
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-
-
- HY-B0089A
-
-
-
- HY-N1944AR
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-
-
- HY-B1671R
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-
-
- HY-N15436
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-
-
- HY-N0165R
-
|
|
Structural Classification
Flavonoids
other families
Flavonones
Phenols
Polyphenols
Plants
Source Classification
|
Reference Standards
HIV
Reverse Transcriptase
|
|
Methyl-Hesperidin (Standard) is the analytical standard of Methyl-Hesperidin (HY-N0165). This product is intended for research and analytical applications. Methyl-Hesperidin is a glycoside compound. Methyl-Hesperidin has hypotensive, coronary dilating, smooth muscle relaxing, capillary stabilizing, choleretic, and anti-ulcer activities. Methyl-Hesperidin act as a competitive substrate to inhibit HIV-1 reverse transcriptase activity. Methyl-Hesperidin potentiates coronary dilating actions of adenine nucleotides and 3'-AMP, enhances depressant action on isolated atria, and prolongs adenosine- and ATP-induced heart block in guinea pigs .
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-
-
- HY-N17845
-
|
|
Bletilla striata (Thunb. ex Murray) Rchb. f.
Structural Classification
Simple Phenylpropanols
Orchidaceae
Phenylpropanoids
Plants
Source Classification
|
Microtubule/Tubulin
|
|
3,3'-Dihydroxy-2,6-bis(4-hydroxybenzyl)-5-methoxybibenzyl, a stilbenoid compound, is a tubulin inhibitor with an IC50 of 10 μM. 3,3'-Dihydroxy-2,6-bis(4-hydroxybenzyl)-5-methoxybibenzyl inhibits tubulin polymerization. 3,3'-Dihydroxy-2,6-bis(4-hydroxybenzyl)-5-methoxybibenzyl functions as a potentiator that potentiates SN-38 (HY-13704) cytotoxicity in BCRP-transduced cancer cells. 3,3'-Dihydroxy-2,6-bis(4-hydroxybenzyl)-5-methoxybibenzyl can be used for the study of breast cancer .
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-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0590S
-
|
|
|
Tetrabenazine-d6 (Deutetrabenazine) is a deuterium-labled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
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-
-
- HY-B1811AS1
-
|
|
|
Vasopressin-d5 TFA is the TFA salt form of Vasopressin-d5 (HY-B1811S1). Vasopressin-d5 TFA is an isotope-labeled compound of Vasopressin (HY-B1811). Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of the corticotropin-releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
|
-
-
- HY-179219S
-
|
|
|
RTx-303 is an orally active, selective DNA polymerase θ (Polθ) inhibitor (IC50 = 5.1 nM). RTx-303 exhibits significantly high cellular potency and strongly potentiates PARPi in BRCA1/2 mutant cells and patient-derived xenograft models. RTx-303 can be used for the study of BRCA2-mutated breast cancer .
|
-
-
- HY-G0021S1
-
|
|
|
N-Desmethylclozapine-d8 (hydrochloride) is the deuterium labeled N-Desmethylclozapine hydrochloride. N-Desmethylclozapine hydrochloride is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine hydrochloride is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine hydrochloride is also a δ-opioid agonist .
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-
-
- HY-G0021S
-
|
|
|
N-Desmethylclozapine-d8 is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic agent Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist .
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-
-
- HY-B0089S
-
|
|
|
Acarbose-d4 (BAY g 5421-d4) is deuterium labeled Acarbose. Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
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-
-
- HY-B1811S1
-
|
|
|
Vasopressin-d5 is anIsotope-labeled compound of Vasopressin. Vasopressin is a cyclic nonapeptide that is synthesized centrally in the hypothalamus. Vasopressin participates in the hypothalamic-pituitary-adrenal axis and regulates pituitary corticotropin secretion by potentiating the stimulatory effects of the corticotropin-releasing factor. Vasopressin also can act as a neurotransmitter, exerting its action by binding to specific G protein-coupled receptors .
|
-
-
- HY-N3995S
-
|
|
|
5β-Dihydrocortisol-d6 is the deuterium labeled 5β-Dihydrocortisol. 5β-Dihydrocortisol, a metabolite of Cortisol, is a potential mineralocorticoid. 5β-Dihydrocortisol can potentiate glucocorticoid activity in raising the intraocular pressure. 5β-Dihydrocortisol causes breast cancer cell apoptosis .
|
-
-
- HY-12390S
-
|
|
|
Lofepramine-d3 (Lopramine-d3) is the deuterium labeled Lofepramine. Lofepramine (Lopramine) is a potent tricyclic antidepressant and is extensively metabolised to Desipramine. The antidepressant activity of Lofepramine stems from the facilitation of noradrenergic neurotransmission by uptake inhibition. Lofepramine may also potentiate serotoninergic neurotransmission by inhibition of the neuronal uptake of serotonin and the enzyme tryptophan pyrrolase. Lofepramine has significant anxiolytic efficacy in addition to its antidepressant properties .
|
-
-
- HY-A0009S
-
|
|
|
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
-
- HY-18610S
-
|
|
|
Diclofensine-d3 (Ro-8-4650-d3) hydrochloride is the deuterium labeled Diclofensine hydrochloride. Diclofensine hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression.
|
-
-
- HY-B0590S3
-
|
|
|
Tetrabenazine-d7 (TBZ-d7-d7) is deuterium labeled Tetrabenazine (HY-B0590). Tetrabenazine (Ro 1-9569) is a brain-penetrant and orally active VMAT2-selective ligand with human VMAT2 Ki 100 nM. Tetrabenazine binds VMAT2 to block monoamine uptake into synaptic vesicles, potentiates cytoplasmic monoamine degradation. Tetrabenazine weakly blocks dopamine D2 receptors, and increases dopamine turnover via elevated cerebrospinal fluid homovanillic acid. Tetrabenazine can be used for the research of Huntington’s disease, tardive dyskinesia, and Tourette’s syndrome .
|
-
-
- HY-123489S
-
|
|
|
3α,21-Dihydroxy-5α-pregnan-20-one-d3 is the deuterium labeled 3α,21-Dihydroxy-5α-pregnan-20-one. 3α,21-Dihydroxy-5α-pregnan-20-one (THDOC), an endogenous neurosteroid, is a positive modulator of GABAA receptors. 3α,21-Dihydroxy-5α-pregnan-20-one potentiates neuronal response to low concentrations of GABA at α4β1δ GABAA receptors in vitro.
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-
-
- HY-W013150S
-
|
|
|
Alpidem-d14 is the deuterium labeled Alpidem (HY-W013150) . Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions.
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-116629
-
|
|
|
Alkynes
|
|
Dactylyne is an ethyl dibromochloroether isolated from the sea hare Dactylomela. Dactylyne has the ability to inhibit Pentobarbital (PTB) metabolism and potentiate the effects of other hypnotic drugs .
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![[Asu1,6-Arg8]Vasopressin](http://file.medchemexpress.com/product_pic/hy-p4012.gif)
![[DArg10, DAla20] TLQP-21](http://file.medchemexpress.com/product_pic/hy-p1345b.gif)
![[DArg10, Aib20] TLQP-21](http://file.medchemexpress.com/product_pic/hy-p1345c.gif)
