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Results for "

CYP+Inhibitors

" in MedChemExpress (MCE) Product Catalog:

6

Inhibitors & Agonists

1

Peptides

2

Natural
Products

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N8382
    Chalepensin

    		Cytochrome P450 Parasite Insecticide Infection
    Chalepensin is a nematicide and CYP inhibitor. Chalepensin inhibits CYP2A6, CYP1A1, CYP1A2, CYP2A13, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 to varying degrees, with IC50 values of 82.3 μM, 2.86 μM, 3.01 μM, 0.21 μM, 6.58 μM, 1.67 μM, 61.1 μM, and 61.7 μM, respectively. Chalepensin potently and selectively kills third-stage infective larvae of Strongyloides venezuelensis .
    Chalepensin
  • HY-150080
    GSK3739936

    BMS-986180

    		 HIV HIV Integrase Infection
    GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
    GSK3739936
  • HY-N8094
    Kushenol M

    		Cytochrome P450 Others
    Kushenol M is a flavonoid from Sophora flavescens. Kushenol M is a cytochrome P450 (CYP) inhibitor, with IC50 values of 1.29 μM for CYP3A4 in human liver microsomes .
    Kushenol M
  • HY-182582
    ZY12201

    		G protein-coupled Bile Acid Receptor 1 Cytochrome P450 Metabolic Disease
    ZY12201 is a selective and orally active TGR5 agonist and pan-CYP inhibitor. ZY12201 lowers glucose levels. ZY12201 induces enzymes regulated through Aryl Hydrocarbon Receptor, Constitutive Androstane Receptor, and Pregnane X Receptor. ZY12201 can be used for the research of type 2 diabetes .
    ZY12201
  • HY-P11489
    RN-0001

    		Cyclophilin Reactive Oxygen Species (ROS) NF-κB Caspase Apoptosis Metabolic Disease
    RN-0001 is a cyclophilin (Cyp) inhibitor with Ki values of 4.1 nM and 12.0 nM against CypA and CypD, respectively, and an EC50 of 916 nM for CypD. RN-0001 binds directly to CypD, inhibits the peptidyl-prolyl cis-trans isomerase activities of CypD and CypA, and prevents CypD-dependent mitochondrial permeability transition pore opening. RN-0001 improves mitochondrial function, reduces ROS production, inhibits the expression of lipogenic markers, blocks the nuclear translocation of NF-κB p65, and decreases the release of activated caspase-3 and cytochrome c. RN-0001 can be used in the research of alcohol-associated liver disease .
    RN-0001
  • HY-182271
    GPR61 Inverse agonist 3

    		Orphan GPCR GABA Receptor Phosphodiesterase (PDE) Metabolic Disease
    GPR61 Inverse agonist 3 is a selective and brain-penetrant GPR61 inverse agonist with human IC50 of 4.0 nM, mouse IC50 of 8.8 nM, human Ki of 0.34 nM, mouse Ki of 1.1 nM. GPR61 Inverse agonist 3 disrupts GPR61-Gαs protein interactions to abolish GPR61 constitutive activity. GPR61 Inverse agonist 3 moderately inhibits GABAA chloride channel and PDE3A1 with IC50 values of 4.6 and 8.9 μM. GPR61 Inverse agonist 3 shows no functional effect on food intake in adult mice co-administered with a pan-CYP inhibitor. GPR61 Inverse agonist 3 can be used for the research of cachexia/sarcopenia .
    GPR61 Inverse agonist 3

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