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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
30 Results for "
OATP1B1
" in MedChemExpress (MCE) Product Catalog:
Products (30)
30 Results for "OATP1B1" in MCE Product Catalog:
48
48 Publications Verification
Synonyms: BMS-790052; EBP 883
Daclatasvir (BMS-790052) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir is also a organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
48
48 Publications Verification
Synonyms: BMS-790052 dihydrochloride; EBP 883 dihydrochloride
Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 μM and 3.27 μM, respectively .
9
9 Cited Publications
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CP-100356 hydrochloride is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 hydrochloride is also a weak inhibitor of OATP1B1 (IC50=∼66 µM). CP-100356 hydrochloride is devoid of inhibition against MRP2 and major human P450 enzymes (IC50>15 µM) .
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Pradigastat (LCQ-908) is a selective and orally effective diacylglyceryl acyltransferase 1 (DGAT1) inhibitor with IC50 at 0.157 µM. Pradigastat is primarily used to study diseases associated with abnormal triglyceride metabolism. Pradigastat has anti-obesity and anti-diabetic effects. Pradigastat inhibited BCRP, OATP1B1, OATP1B3 and OAT3 activities with IC50 of 5 µM, 1.66µM, 3.34µM and 0.973µM, respectively. In addition, Pradigastat has antiviral activity and can inhibit hepatitis C virus replication in vitro .
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
Cat. No.: HY-N7755
CAS No.: 14982-12-8
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Estradiol 3-glucuronide sodium is an estrogen metabolite, which is a glucuronide conjugate formed by the catalysis of uridine diphosphate glucuronosyltransferase in tissues such as the liver from Estradiol (HY-B0141). Estradiol 3-glucuronide sodium is a potent substrate of Mrp2, with an S50 of 55.7 μM. Estradiol 3-glucuronide sodium achieves hepatobiliary transport in hepatocytes through basolateral uptake via OATP1B1, OATP1B3 and OATP2B1, as well as apical efflux via MRP2 and BCRP .
1
1 Cited Publications
Cat. No.: HY-W585842
CAS No.: 15270-30-1
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Estradiol 3-glucuronide is an estrogen metabolite, which is a glucuronide conjugate formed from Estradiol (HY-B0141) via catalysis by uridine diphosphate glucuronosyltransferases in tissues such as the liver. Estradiol 3-glucuronide is a potent substrate of Mrp2, with an S50 value of 55.7 μM. Estradiol 3-glucuronide achieves hepatobiliary transport in hepatocytes through basolateral uptake via OATP1B1, OATP1B3 and OATP2B1, as well as apical efflux via MRP2 and BCRP .
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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 .
Cat. No.: HY-N3504
CAS No.: 65604-80-0
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PF-06456384 trihydrochloride is an extremely potent and selective Nav1.7 sodium channel blocker (IC50: 0.01 nM for hNaV1.7; 75 nM for rNaV1.7; <0.1 nM for mNaV1.7). PF-06456384 trihydrochloride shows no significant analgesic efficacy in the mouse Formalin pain model .
Cat. No.: HY-164774
CAS No.: 2758659-09-3
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(4S)-GLP-1 receptor agonist 14 is a potent and orally active GLP-1 receptor agonist with an EC50 ≤ 20 nM. (4S)-GLP-1 receptor agonist 14 can be used for research on diabetes, obesity, metabolic diseases, cardiovascular diseases, liver diseases, nonalcoholic steatohepatitis (NASH), and other diseases associated with GLP-1 receptor .
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2-Hydroxy atorvastatin calcium salt is an orally active OATP1B1 substrate and inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase (3-hydroxy-3-methylglutaryl-coenzyme A reductase). 2-Hydroxy atorvastatin calcium salt enters cells via OATP1B1-mediated cellular uptake and inhibits de novo hepatic cholesterol synthesis. As an active metabolite of Atorvastatin (HY-B0589), 2-Hydroxy atorvastatin calcium salt contributes to the inhibitory activity against plasma HMG-CoA reductase. 2-Hydroxy atorvastatin calcium salt can be biotransformed into an inactive lactone form, which can be hydrolyzed back to its active acid form chemically or enzymatically. 2-Hydroxy atorvastatin (calcium salt) can be used in the research of hypercholesterolemia .
Cat. No.: HY-W002438
CAS No.: 2380-86-1
Cat. No.: HY-178767
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ECC-5004 (Compound 1) is a GLP-1 receptor agonist with an EC50 of 0-20 nM. ECC-5004 exhibits strong inhibitory effects on OATP1B1, with an IC50 < 1 μM. ECC-5004 can be used to study diseases such as diabetes, obesity, and non-alcoholic fatty liver disease .
Cat. No.: HY-10465R
CAS No.: 1009119-65-6
Synonyms: BMS-790052 dihydrochloride (Standard); EBP 883 dihydrochloride (Standard)
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Daclatasvir (dihydrochloride) (Standard) is the analytical standard of Daclatasvir (dihydrochloride). This product is intended for research and analytical applications. Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is a potent and orally active HCV NS5A protein inhibitor with EC50s range of 9-146 pM for multiple HCV replicon genotypes. Daclatasvir dihydrochloride is also an organic anion transporting polypeptide 1B (OATP1B) and OATP1B3 inhibitor with IC50s of 1.5 µM and 3.27 µM, respectively .
Cat. No.: HY-108347A
CAS No.: 142716-85-6
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CP-100356 is an orally active dual MDR1 (P-gp)/BCRP inhibitor, with an IC50s of 0.5 and 1.5 µM for inhibiting MDR1-mediated Calcein-AM transport and BCRP-mediated Prazosin transport, respectively. CP-100356 is also a weak inhibitor of OATP1B1 (IC50 = ∼66 µM). CP-100356 is devoid of inhibition against MRP2 and major human P450 enzymes (IC50 > 15 µM) .
Cat. No.: HY-155668
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HMG-CoA Reductase-IN-1 is a HMG-CoA reductase inhibitor. HMG-CoA Reductase-IN-1has high HMGR inhibitory activity and OATP1B1 affinity with pIC50 and pKm values of 8.54 and 1.98, respectively. HMG-CoA Reductase-IN-1 can be used for the research of hypercholesterolemia .
Cat. No.: HY-W002438R
CAS No.: 2380-86-1
Cat. No.: HY-N8497
CAS No.: 105350-54-7
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Cat. No.: HY-138142
CAS No.: 13879-04-4
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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
