oatp1b1

Rifampicin (Rifamycin AMP) is a broad-spectrum antibiotic. Rifampicin has a strong antibacterial effect against Mycobacterium tuberculosis and is also effective against gram-positive and gram-negative bacteria and viruses.

Daclatasvir dihydrochloride (BMS-790052 dihydrochloride) is an orally available antiviral agent that inhibits the NS5A region of the hepatitis C virus (HCV) and is used in combination with other oral antivirals to treat chronic hepatitis C. Elevations in serum enzyme levels during daclatasvir therapy are uncommon, and it has not been convincingly implicated in cases of clinically apparent liver injury with jaundice.

Daclatasvir (EBP 883) (BMS-790052) is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture. Phase 3.

CP-100356 hydrochloride is an orally active, low micromolar dual inhibitor of MDR1 (P-gp) and BCRP, a nucleotide-derived substrate analogue that inhibits MDR1-mediated Calcein-AM and BCRP-mediated Prazosin transporters. Additionally, CP-100356 inhibits OATP1B1 and induces stomatal opening in the dark.

Leoidin is a depsidone originally isolated from L. gangaleoides that has antibacterial and enzyme inhibitory activities.1,2,3 It is active against the bacteria E. faecalis, H. influenzae, M. catarrhalis, S. aureus, and S. pneumoniae (MICs = 8, 32, 1, 128, and 64 μg/ml, respectively).2 Leoidin inhibits phenylalanyl-tRNA synthetase (PheRS) isolated from P. aeruginosa (IC50 = 42 μM). It also inhibits organic anion-transporting polypeptide 1B1 (OATP1B1) and OATP1B3 with Ki values of 0.08 and 1.84 μM, respectively, in CHO cells expressing the human transporters.3

Silydianin (Silidianin) exerts inhibition of UGT in human liver. Silydianin exerts inhibition of OATP1B1, OATP1B3 (unknown origin) expressed in HEK293 cells. Silydianin exerts inhibition of OATP2B1 (unknown origin) expressed in MDCK2 cells.

Euphol acetate, a triterpene found in Euphorbia broteri, has demonstrated inhibitory effects on the hepatic transport proteins known as organic anion-transporting polypeptide 1/3 (OATP1B1/3).

HMG-CoA Reductase-IN-1, an inhibitor of HMG-CoA reductase, demonstrates strong inhibitory activity on HMGR and affinity for OATP1B1, with pIC50 and pKm values of 8.54 and 1.98, respectively. It is utilized in hypercholesterolemia research [1].