26 Results for "

OATP2B1

" in MedChemExpress (MCE) Product Catalog:
Products (26)

26 Results for "OATP2B1" in MCE Product Catalog:

143
143 Publications Verification
Cat. No.: HY-50896
CAS No.: 183321-74-6
Synonyms: CP-358774; NSC 718781; OSI-774
Target:  

EGFR OAT ERK GSK-3 β-catenin

Research Areas:  

Endocrinology Cancer

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 .
loading...
    loading...
143
143 Publications Verification
Cat. No.: HY-12008
CAS No.: 183319-69-9
Purity:  99.94%
Synonyms: CP-358774 hydrochloride; NSC 718781 hydrochloride; OSI-774 hydrochloride
Target:  

EGFR OAT ERK GSK-3 β-catenin

Research Areas:  

Endocrinology Cancer

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 .
loading...
    loading...
8
8 Cited Publications
Cat. No.: HY-N3513
CAS No.: 62949-79-5
Synonyms: Kuwanon C
Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8?±1.5 μM.
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-N7755
CAS No.: 14982-12-8
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 .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-W585842
CAS No.: 15270-30-1
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 .
loading...
    loading...
Cat. No.: HY-B0396
CAS No.: 161715-24-8
Synonyms: L084
Target:  

Antibiotic Bacterial OAT

Research Areas:  

Infection

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 .
loading...
    loading...
Cat. No.: HY-50896R
CAS No.: 183321-74-6
Synonyms: CP-358774 (Standard); NSC 718781 (Standard); OSI-774 (Standard)
Erlotinib Standard (CP-358774 Standard) is the analytical standard of Erlotinib (HY-50896). This product is intended for research and analytical applications. 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 .
loading...
    loading...
Cat. No.: HY-118952A
CAS No.: 1834610-75-1
Purity:  99.38%
Target:  

Sodium Channel

Research Areas:  

Neurological Disease

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 .
loading...
    loading...
Cat. No.: HY-126848
CAS No.: 64118-81-6
Purity:  95.6%
Synonyms: D-1-O-G
Diclofenac acyl glucuronide (D-1-O-G) is an orally active glucuronide metabolite of Diclofenac (HY-15036). Diclofenac acyl glucuronide exhibits SOD inhibitory activity, COX-1 inhibitory activity (IC50 = 0.620 μM), and COX-2 inhibitory activity (IC50 = 2.91 μM). Diclofenac acyl glucuronide induces reactive oxygen species (ROS) production and acts as a substrate of OATP2B1. Diclofenac acyl glucuronide induces small intestinal ulcers . Diclofenac acyl glucuronide can be used in research related to intestinal diseases and small intestinal ulcers .
loading...
    loading...
Cat. No.: HY-12008R
CAS No.: 183319-69-9
Synonyms: CP-358774 hydrochloride (Standard); NSC 718781 hydrochloride (Standard); OSI-774 hydrochloride (Standard)
Erlotinib Hydrochloride Standard (CP-358774 hydrochloride Standard) is the analytical standard of Erlotinib Hydrochloride (HY-12008). This product is intended for research and analytical applications. 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 .
loading...
    loading...
Cat. No.: HY-50896S
CAS No.: 1034651-23-4
Synonyms: CP-358774-d6; NSC 718781-d6; OSI-774-d6
Erlotinib-d6 (CP-358774-d6) 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 .
loading...
    loading...
Cat. No.: HY-12008S1
CAS No.: 1210610-07-3
Synonyms: CP-358774-13C6 hydrochloride; NSC 718781-13C6 hydrochloride; OSI-774-13C6 hydrochloride
Erlotinib- 13C6 hydrochloride (CP-358774- 13C6 hydrochloride) is the 13C-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 .
loading...
    loading...
Cat. No.: HY-12008A
CAS No.: 248594-19-6
Synonyms: CP-358774 mesylate; NSC 718781 mesylate; OSI-774 mesylate
Target:  

EGFR OAT ERK GSK-3 β-catenin

Research Areas:  

Endocrinology Cancer

Erlotinib (CP-358774) mesylate is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib mesylate 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 mesylate blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib mesylate 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 mesylate is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib mesylate can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis .
loading...
    loading...
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 .
loading...
    loading...
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 .
loading...
    loading...
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 .
loading...
    loading...
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 .
loading...
    loading...
Cat. No.: HY-N3513R
CAS No.: 62949-79-5
Synonyms: Kuwanon C (Standard)
Mulberrin (Standard) is the analytical standard of Mulberrin. This product is intended for research and analytical applications. Mulberrin is a strong inhibitor of organic anion-transporting polypeptide 2B1 (OATP2B1)-mediated estrone-3-sulfate (E3S) uptake with an IC50 value being 1.8 ±1.5 μM.
loading...
    loading...
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 .
loading...
    loading...
Cat. No.: HY-14752
CAS No.: 753449-67-1
Synonyms: SB 751689
Target:  

CaSR

Research Areas:  

Metabolic Disease Endocrinology

Ronacaleret (SB 751689) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands. Ronacaleret (SB 751689) is used for the study of postmenopausal osteoporosis .
loading...
    loading...