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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
46 Results for "
OATP1
" in MedChemExpress (MCE) Product Catalog:
Products (46)
46 Results for "OATP1" 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 [1] .
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 [1] .
9
9 Cited Publications
Target:
Forschungsgebiete:
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) [1].
5
Target:
Forschungsgebiete:
Nadolol (SQ-11725) is a non-selective and orally active β-adrenergic receptors blocker and is a substrate of organic anion transporting polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research [1] .
3
3 Cited Publications
3
3 Cited Publications
2
Target:
Forschungsgebiete:
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
1 Cited Publications
Art. -Nr.: HY-N7755
CAS. Nr.: 14982-12-8
Forschungsgebiete:
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
1 Cited Publications
Art. -Nr.: HY-W585842
CAS. Nr.: 15270-30-1
Forschungsgebiete:
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 [1] .
Art. -Nr.: HY-B0396
CAS. Nr.: 161715-24-8
Synonyms: L084
Target:
Forschungsgebiete:
Tebipenem pivoxil (L084 hydrobromide) is an orally active carbapenem Antibiotic. Tebipenem pivoxil acts as a substrate of OATP1A2 with high affinity for this transporter (Km = 41.1 μM) . Tebipenem pivoxil achieves intestinal absorption via carrier-mediated uptake and simple diffusion. Tebipenem pivoxil inhibits the growth of Gram-positive bacteria, Gram-negative bacteria, multidrug-resistant bacteria, and pathogens producing extended-spectrum β-lactamases. Tebipenem pivoxil eliminates intestinal infection pathogens and reduces mortality in septic mice. Tebipenem pivoxil can be used in research related to bacterial pneumonia, severe gastrointestinal infections, bacterial sepsis, complicated urinary tract infections, and acute pyelonephritis [1] .
Art. -Nr.: HY-W011819
CAS. Nr.: 821-38-5
Target:
Art. -Nr.: HY-N3504
CAS. Nr.: 65604-80-0
Forschungsgebiete:
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 [1] .
Art. -Nr.: HY-W002438
CAS. Nr.: 2380-86-1
Art. -Nr.: HY-RS13358
Target:
Forschungsgebiete:
SLCO4A1 Human Pre-designed siRNA Set A contains three designed siRNAs for SLCO4A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
Art. -Nr.: HY-16443
CAS. Nr.: 173534-37-7
Target:
Forschungsgebiete:
S-4048 is a glucose-6-phosphate translocase modulator and hypoglycemic agent. S-4048 is taken up by hepatocytes via OATP-1 and is rapidly eliminated via the hepatobiliary system in rats. S-4048 blocks glucose-6-phosphate translocase, prevents glucose-6-phosphate from entering the endoplasmic reticulum, and thereby interferes with the glucose-6-phosphatase system (i.e., the final step of hepatic gluconeogenesis and glycogenolysis) to regulate hepatic glucose production. S-4048 completely inhibits glucose production from pyruvate in GLUT2-deficient hepatocytes without affecting the release of cytoplasmic glucose. S-4048 effectively reduces blood glucose levels in rats and has been used in studies related to type 2 diabetes [1] .
Art. -Nr.: HY-10465R
CAS. Nr.: 1009119-65-6
Synonyms: BMS-790052 dihydrochloride (Standard); EBP 883 dihydrochloride (Standard)
Target:
Forschungsgebiete:
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 [1] .
Art. -Nr.: HY-178767
Target:
Forschungsgebiete:
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 [1].
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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
