OAT Substrate

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 (K_m = 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.

AF405 NHS Ester (AF405) is a Fluorescent probe substrate, as well as a substrate for OATP1B1, OATP1B3 and OATP2B1.

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.

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.

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.

PF-05221304 tromethamine is an orally active, liver-directed and dual ACC1/ACC2 inhibitor with IC₅₀s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2. PF-05221304 tromethamine is a substrate for organic anion transport polypeptides. PF-05221304 tromethamine directly improves a variety of non-alcoholic fatty liver (NAFL) and non-alcoholic steatohepatitis (NASH) pathogenic factors.