9

CP-100356 hydrochloride

9 Publications Verification

Cat. No.: HY-108347

CAS No.: 142715-48-8

Purity: 99.19%

Target:

P-glycoprotein BCRP

Research Areas:

Metabolic Disease

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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4

CP-724714

4 Cited Publications

Cat. No.: HY-14674

CAS No.: 383432-38-0

Purity: 98.72%

Target:

EGFR Apoptosis P-glycoprotein Raf ERK

Research Areas:

Infection Cancer

CP-724714 is an orally active and selective HER2 tyrosine kinase inhibitor with an IC₅₀ of 10 nM. CP-724714 inhibits HER2 receptor autophosphorylation and blocks the downstream Ras-Raf-Mek-Erk signaling pathway, thereby inducing cell cycle arrest and apoptosis in tumor cells. CP-724714 exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC₅₀ of 0.91 μM). CP-724714 is an inhibitor of the hepatic transport receptors OATP1B1/MDR1/BSEP, and can enter hepatocytes via active uptake and trigger the accumulation of drugs and bile acids within hepatocytes. CP-724714 can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection .

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2

Pradigastat

2 Cited Publications

Cat. No.: HY-16278

CAS No.: 956136-95-1

Synonyms: LCQ-908

Target:

Acyltransferase BCRP OAT

Research Areas:

Infection Metabolic Disease

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 .

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1

Estradiol 3-glucuronide sodium

1 Cited Publications

Cat. No.: HY-N7755

CAS No.: 14982-12-8

Target:

Endogenous Metabolite ATP-binding cassette (ABC) transporters OAT

Research Areas:

Others

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 .

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1

Estradiol 3-glucuronide

1 Cited Publications

Cat. No.: HY-W585842

CAS No.: 15270-30-1

Target:

Endogenous Metabolite ATP-binding cassette (ABC) transporters OAT

Research Areas:

Others

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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