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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
53 Results for "
CYP 2C8
" in MedChemExpress (MCE) Product Catalog:
Products (53)
53 Results for "CYP 2C8" in MCE Product Catalog:
36
36 Publications Verification
Cat. No.: HY-17356
CAS No.: 49562-28-9
Target:
Research Areas:
Fenofibrate is a selective PPARα agonist with an EC50 of 30 μM. Fenofibrate also inhibits human cytochrome P450 isoforms, with IC50s of 0.2, 0.7, 9.7, 4.8 and 142.1 μM for CYP2C19, CYP2B6, CYP2C9, CYP2C8, and CYP3A4, respectively.
13
Rebastinib (DCC-2036) is an orally active, non-ATP-competitive Bcr-Abl inhibitor, with IC50 values of 0.8 nM and 4 nM against Abl1 WT and Abl1 T315I, respectively. Rebastinib potently inhibits CYP2C8 (IC50 = 0.0533 μM) and CYP2C9 (IC50 = 2.54 μM). Rebastinib allosterically inhibits Tie2 with an IC50 of 0.63 nM. Rebastinib inhibits the transcriptional activity of FoxO1. Rebastinib inhibits SRC family kinases, KDR and FLT3 kinases. Rebastinib induces Apoptosis. Rebastinib exerts anti-tumor activity in breast cancer. Rebastinib exerts anti-angiogenic effects. Rebastinib increases myotube diameter and improves reduced contractility. Rebastinib can be used in research related to triple-negative breast cancer, luminal breast cancer, pancreatic neuroendocrine tumors, muscle atrophy, cancer cachexia, chronic myeloid leukemia, and B-lymphocytic leukemia .
7
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Gemfibrozil is an activator of PPAR-α, used as a lipid-lowering agent; Gemfibrozil is also a nonselective inhibitor of several P450 isoforms, with Ki values for CYP2C9, 2C19, 2C8, and 1A2 of 5.8, 24, 69, and 82 μM, respectively.
6
6 Cited Publications
Cat. No.: HY-N0319
CAS No.: 115841-09-3
Category:
Plant Ketones, Aldehydes, Acids Phenols Polyphenols Salvia miltiorrhiza Bunge Extract Disease Research Fields Cancer Labiatae Extract
Target:
1
1 Cited Publications
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Gemfibrozil 1-O-β-Glucuronide, a metabolite of Gemfibrozil (CI-719; HY-B0258), is a potent and competitive P450 (CYP) isoform CYP2C8 inhibitor with an IC50 of 4.07 μM .
1
1 Cited Publications
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Research Areas:
ACP-5862 is a major active, circulating, pyrrolidine ring-opened metabolite of Acalabrutinib with an IC50 of 5.0 nM for Bruton tyrosine kinase (BTK). ACP‐5862 is a weak time‐dependent inactivator of CYP3A4 and CYP2C8. Acalabrutinib is an orally active, irreversible, and highly selective BTK inhibitor, with an IC50 of 3 nM and EC50 of 8 nM .
1
1 Cited Publications
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LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A .
1
1 Cited Publications
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N-Desmethyl-Apalutamide, the major active metabolite of Apalutamide (HY-16060), is a selective competitive inhibitor of androgen receptor. N-Desmethyl-Apalutamide is catalyzed by CYP3A4 and CYP2C8 enzymes. The plasma protein binding rate of N-Desmethyl-Apalutamide reaches 95%, with albumin as the primary binding protein. N-Desmethyl-Apalutamide is suitable for prostate cancer-related research .
1
1 Cited Publications
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MS-PPOH is a potent and selective cytochrome P450 (CYP) epoxygenase inhibitor . MS-PPOH inhibits CYP2C8 and CYP2C9 with IC50s of 15 and 11 μM, respectively . MS-PPOH is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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6α-Hydroxy paclitaxel is one of the main metabolites of Paclitaxel (PTX) (HY-B0015), and it is generated by the liver cytochrome P450 enzyme CYP2C8. 6α-Hydroxy paclitaxel has bone marrow toxicity, but it can enhance the cytotoxicity of PTX against leukemia cells without causing cell toxicity. 6α-Hydroxy paclitaxel can be used in leukemia research .
Category:
Umbelliferae/Apiaceae Extract Other Monoterpenes Plant Foeniculum vulgare Mill. Extract Terpenoids Other Diseases Disease Research Fields
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Synonyms: ACT-539313
Research Areas:
Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder .
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4-Hydroxytolbutamide (Hydroxytolbutamide) is a metabolite of Tolbutamide. 4-Hydroxytolbutamide is metabolized by CYP2C8 and CYP2C9. Tolbutamide is a first generation potassium channel blocker and a sulfonylurea oral antidiabetic .
Cat. No.: HY-W013268
CAS No.: 790676-40-3
Synonyms: (+)-N-3-Benzylnirvanol
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(S)-(+)-N-3-Benzylnirvanol ((+)-N-3-Benzylnirvanol) is a selective and competitive cytochrome P450 (CYP) isoform CYP2C19 inhibitor with a Ki of 250 nM. (S)-(+)-N-3-Benzylnirvanol has low activity against CYP1A2, CYP2A6, CYP2C8, CYP2C9, CYP2D6, CYP2E1, and CYP3A4 .
Synonyms: DBF
Target:
Research Areas:
3'-Hydroxy Repaglinide is the major CYP2C8 metabolite of Repaglinide (HY-15209). Repaglinide is a carbamoylmethylbenzoic acid (CMBA) derivative that acts on type 2 diabetes .
Cat. No.: HY-124542
CAS No.: 69002-84-2
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Research Areas:
5-Hydroxydiclofenac is a major metabolite of Diclofenac (HY-15036). 5-Hydroxydiclofenac is formed by the cytochrome P450 (CYP) isoforms CYP3A4, CYP2C189, CYP2C19, and CYP2C8. 5-Hydroxydiclofenac shows apoptotic effects in hepatocytes .
Cat. No.: HY-17356S
CAS No.: 1092484-56-4
Cat. No.: HY-B0258S
CAS No.: 1184986-45-5
Synonyms: CI-719-d6
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
