79 Results for "

OATPs

" in MedChemExpress (MCE) Product Catalog:
Products (79)

79 Results for "OATPs" in MCE Product Catalog:

Cat. No.: HY-12008S
CAS No.: 1189953-78-3
Purity:  98.13%
Synonyms: CP-358774-d6 hydrochloride; NSC 718781-d6 hydrochloride; OSI-774-d6 hydrochloride
Erlotinib-d6 hydrochloride (CP-358774-d6 hydrochloride) is the deuterated-labeled Erlotinib Hydrochloride (HY-12008). Erlotinib (CP-358774) Hydrochloride is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib Hydrochloride also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib Hydrochloride blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib Hydrochloride inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib Hydrochloride is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib Hydrochloride can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis .
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Cat. No.: HY-50896S1
CAS No.: 1211107-68-4
Synonyms: CP-358774-13C6; NSC 718781-13C6; OSI-774-13C6
Erlotinib- 13C6 (CP-358774- 13C6) is the 13C-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions .
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Cat. No.: HY-50896S2
CAS No.: 1130852-41-3
Synonyms: CP-358774-d4; NSC 718781-d4; OSI-774-d4
Erlotinib-d4 (CP-358774-d4) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions .
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Cat. No.: HY-50896S3
CAS No.: 1266656-97-6
Synonyms: CP-358774-d8; NSC 718781-d8; OSI-774-d8
Erlotinib-d8 (CP-358774-d8) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis .
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Cat. No.: HY-16278R
CAS No.: 956136-95-1
Synonyms: LCQ-908 (Standard)
Pradigastat (Standard) is the analytical standard of Pradigastat. This product is intended for research and analytical applications. 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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Cat. No.: HY-161821
Research Areas:  

Cancer

Antitumor agent-173 (Compound 4b) is a prodrug of Cycloicaritin (HY-N1940). Antitumor agent-173 is a substrate for OATP2B1. Antitumor agent-173 selectively inhibits the growth of tumor Antitumor agent-173 significantly increases the oral bioavailability of Cycloicaritin and exerts good antitumor activity and safety .
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Cat. No.: HY-163146
Target:  

Fluorescent Dye

Research Areas:  

Cancer

TME-HYM (PH Probe) is a novel fluorescent probe based on acidic tumor microenvironment (TME) activation and organic anion transporting polypeptide (OATPs, overexpressed on cancer cells), and can be selective uptaken. TME-HYM (PH Probe) can selectively lit up cancer cells and tumor tissues, offering dual tumor selectivity for precise visualization of tumor mass .
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Cat. No.: HY-173231
CAS No.: 1402818-99-8
Target:  

URAT1

Research Areas:  

Metabolic Disease

hURAT1 inhibitor 2 (Compound 5) is an inhibitor of hURAT1 (uric acid transporter 1, SLC22A12) with an IC50 of 18 nM. hURAT1 inhibitor 2 also has a certain inhibitory effect on OATP1B1, with an IC50 value of 0.73 μM. hURAT1 inhibitor 2 can be used in the research of diseases related to abnormal uric acid metabolism, such as hyperuricemia and gout .
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Cat. No.: HY-155062
IR-251 is a mitochondrion-targeting NIR fluorescent probe. IR-251 targets mitochondria via OATPs and causes mitochondrial damage in tumor cells. IR-251 IR-251 induced ROS overproduction by inhibiting PPARγ, and then inhibiting the β-catenin signaling pathway and downstream protein molecules related to the cell cycle and metastasis. IR-251 inhibits tumor proliferation and metastasis .
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Cat. No.: HY-B0396R
CAS No.: 161715-24-8
Synonyms: L084 (Standard)
Research Areas:  

Infection

Tebipenem pivoxil (Standard) (L084 (Standard)) is the analytical standard of Tebipenem pivoxil (HY-B0396). This product is intended for research and analytical applications. 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 .
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Cat. No.: HY-D3239
Synonyms: AF405; Alexa Fluor 405 succinimidyl ester
AF405 NHS Ester (AF405) is a Fluorescent probe substrate, as well as a substrate for OATP1B1, OATP1B3 and OATP2B1 .
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Cat. No.: HY-115292S
CAS No.: 2747915-76-8
Synonyms: Tenivastatin-d6 sodium; Simvastatin impurity A-d6 sodium
Simvastatin hydroxy acid-d6 sodium (Tenivastatin-d6 sodium) is the deuterium labeled Simvastatin hydroxy acid sodium (HY-115292). Simvastatin hydroxy acid (Tenivastatin) sodium is a potent HMG-CoA reductase (HMGCR) inhibitor. Simvastatin hydroxy acid sodium reduces Indoxyl sulfate-mediated reactive oxygen species (ROS) production in human cardiomyocytes. Simvastatin hydroxy acid sodium can also modulates OATP3A1 expression in cardiomyocytes and HEK293 cells transfected with the OATP3A1 gene .
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Cat. No.: HY-D3433
CAS No.: 222159-75-3
Synonyms: CDCSF
Target:  

Fluorescent Dye

Research Areas:  

Others

5-Carboxy-2′,7′-dichlorosulfonefluorescein (CDCSF) is a fluorescein derivative-based fluorescent probe. 5-Carboxy-2′,7′-dichlorosulfonefluorescein serves as a fluorescent substrate for the organic anion transporting polypeptide OATP2B1, and is specifically recognized and transported into cells by OATP2B1 under acidic pH conditions, making it suitable for in vitro high-throughput screening of drug-drug interactions (DDI) and food-drug interactions (FDI) (Ex/Em = 485/535 nm) .
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Cat. No.: HY-N15205
CAS No.: 159278-74-7
Rhinacanthin C is an orally active naphthoquinone ester and P-gp inhibitor (IC50 = 5.20 μM). Rhinacanthin C exerts effects in ameliorating hepatic steatosis, insulin resistance, and inflammation by inhibiting P-gp, BCRP, OATP1B1/1B3, and multiple CYP enzymes, downregulating lipid synthesis-related factors such as ACC and FAS, and upregulating AMPKα phosphorylation and SIRT1. Rhinacanthin C can be used in research on non-alcoholic fatty liver disease, diabetes, abnormal osteolysis, Alzheimer's disease, and inflammation .
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Cat. No.: HY-14674A
CAS No.: 543681-31-8
Research Areas:  

Infection Cancer

CP-724714 succinate is an orally active and selective HER2 tyrosine kinase inhibitor with an IC50 of 10 nM. CP-724714 succinate 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 succinate exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC50 of 0.91 μM). CP-724714 succinate 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 succinate can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection .
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Cat. No.: HY-113293S1
Estrone sulfate-d4 TEA is the deuterium labeled Estrone sulfate TEA. Estrone sulfate is an inactive endogenous estrogen that can be converted into Estrone (HY-B0234) and Estradiol (HY-B0141). Estrone sulfate is also a substrate of the OATP1B3 transporter. Estrone sulfate can be converted into Estrone and Estradiol in normal mammary parenchymal cells. Estrone sulfate stimulates the growth of nitrosomethylurea-induced mammary tumors in ovariectomized rats and the colony formation of dispersed nitrosomethylurea mammary cells, with conversion into Estrone and Estradiol occurring both in vivo and in vitro during this process. Estrone sulfate is applicable to breast cancer-related research .
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Cat. No.: HY-108347R
CAS No.: 142715-48-8
Research Areas:  

Metabolic Disease

CP-100356 hydrochloride (Standard) is the analytical standard of CP-100356 (hydrochloride) (HY-108347). This product is intended for research and analytical applications. 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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Cat. No.: HY-184557
CAS No.: 2223036-84-6
DZ-1-DHA is a conjugate of DHA (HY-B2167) and DZ-1 dye. DZ-1-DHA mediates selective cellular uptake via binding to overexpressed OATP1A2. DZ-1-DHA induces the cleavage of Caspase-3, Caspase-8, Caspase-9 and PARP-1. DZ-1-DHA induces Apoptosis and Ferroptosis. DZ-1-DHA induces ROS production through a Fenton-like mechanism, causes mitochondrial membrane depolarization, and triggers lipid peroxidation. DZ-1-DHA can be used in studies related to colorectal cancer liver metastasis .
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Cat. No.: HY-B0396B
CAS No.: 1381788-20-0
Synonyms: L084 hydrobromide
Target:  

Antibiotic Bacterial OAT

Research Areas:  

Infection

Tebipenem pivoxil hydrobromide (L084 hydrobromide) is an orally active carbapenem Antibiotic. Tebipenem pivoxil hydrobromide acts as a substrate of OATP1A2 with high affinity for this transporter (Km = 41.1 μM) . Tebipenem pivoxil hydrobromide achieves intestinal absorption via carrier-mediated uptake and simple diffusion. Tebipenem pivoxil hydrobromide inhibits the growth of Gram-positive bacteria, Gram-negative bacteria, multidrug-resistant bacteria, and pathogens producing extended-spectrum β-lactamases. Tebipenem pivoxil hydrobromide eliminates intestinal infection pathogens and reduces mortality in septic mice. Tebipenem pivoxil hydrobromide can be used in research related to bacterial pneumonia, severe gastrointestinal infections, bacterial sepsis, complicated urinary tract infections, and acute pyelonephritis .
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