OAT Inhibitor

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.

Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC₅₀ values of 2.5 nM, 0.41 μM and 0.81 μM for HIV_ADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir can be used to research AIDS.

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.

5-Fluoromethylornithine (5-FMOrn) dihydrochloride is a specific irreversible inhibitor of L-ornithine:2-oxoacid aminotransferase (OAT). 5-Fluoromethylornithine dihydrochloride can be used in the study of gyrate atrophy of choroid and retina.

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.

SOAT-IN-3 is a selective inhibitor of sodium-dependent organic anion transporter (SOAT/SLC10A6). SOAT-IN-3 reduces intracellular estradiol synthesis, the process of dehydroepiandrosterone (DHEA) production from DHEAS, and DHEAS-induced cancer cell proliferation. SOAT-IN-3 shows no cytotoxicity against breast cancer cells at the tested concentrations. SOAT-IN-3 can be used in the research of breast cancer.

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.

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.

Indican (Indoxyl-β-D-glucoside), a glycoside of indoxyl, is a precursor of the dyesindigo and indirubin. Indican has a major metabolite, indoxyl sulfate (IS). IS, an uremic toxin, is a substrate/inhibitor of organic anion transporter (OAT) 1, OAT 3 and multidrug resistance-associated protein (MRP) 4.

Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with K_m values of 0.85 and 2 µM, respectively.

Hydrastine ((-)-β-Hydrastine; (1R,9S)-β-Hydrastine) is a selective competitive inhibitor of tyrosine hydroxylase (TH), inhibiting dopamine biosynthesis (IC₅₀=20.7 μM, PC12 cells). Hydrastine also inhibits the organic cation transporter OCT1 (IC₅₀=6.6 μM). Hydrastine may cause neuronal toxicity through mitochondrial dysfunction rather than oxidative stress damage, and can aggravate cell apoptosis when combined with L-DOPA. Hydrastine can be used to study Parkinson's disease-related dopaminergic neuronal damage.

Cyazofamid exerts its bactericidal effect by impairing ATP production. Cyazofamid inhibits organic cation transporter 3 (OCT3) and OAT1, with IC₅₀ values ​​of 1.54 and 17.3 μM, respectively.

6-Hydroxyindole is an orally active, endogenous long-acting OATP1B1 inhibitor. 6-Hydroxyindole does not alter the cell surface expression or subcellular localization of OATP1B1. 6-Hydroxyindole protects cells against Ferroptosis. 6-Hydroxyindole possesses intrinsic radical-trapping antioxidant activity. 6-Hydroxyindole serves as a component of oxidative hair dyes. 6-Hydroxyindole can be used in research related to renal failure and neurodegenerative diseases.

Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC₅₀ values of 2.5 nM, 0.41 μM and 0.81 μM for HIV_ADA, OAT3 and OAT1, respectively. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir sodium can be used to research AIDS.

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.

18β-Glycyrrhetyl-3-O-sulfate (Glycyrrhetic acid 3-O-(hydrogen sulfate)) is a potent type 2 11β-hydroxysteroid dehydrogenase (11β-HSD2) inhibitor with an IC₅₀ of 0.10 µM using rat kidney microsome. 18β-Glycyrrhetyl-3-O-sulfate is the major metabolite of Glycyrrhetinic acid (GA). 18β-Glycyrrhetyl-3-O-sulfate is the substrate of organic anion transporter (OAT) 1 and OAT3. 18β-Glycyrrhetyl-3-O-sulfate has anti-inflammatory effects and has the potential for pseudohyperaldosteronism research.

Lesinurad sodium is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with K_m values of 0.85 and 2 μM, respectively.

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.

Epaminurad (UR-1102) is an orally active, potent and selective URAT1 (urate transporter 1) inhibitor, with a K_i of 0.057 μM. Epaminurad quite modestly inhibits OAT1 and OAT3 (organic anion transporter). Epaminurad is a uricosuric agent. Epaminurad can be used for gout and hyperuricemia research.

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.