gt1a

Grazoprevir (MK-5172) is a nitrogenous macrocyclic compound used as an inhibitor of the hepatitis C virus NS3/4A protease. Grazoprevir is commonly combined with elbasvir for treating chronic HCV genotype 1 or 4 infections in adults.

Ledipasvir (GS-5885) is a Hepatitis C Virus NS5A Inhibitor. The mechanism of action of ledipasvir is as a P-Glycoprotein Inhibitor, and Breast Cancer Resistance Protein Inhibitor.

UGT1A1-IN-1 (Compound 2) is a non-competitive inhibitor of UGT1A1 (UDP-glucuronosyltransferase 1A1). It inhibits the 1-O-glucuronidation process mediated by UGT1A1 with an IC50 of 1.33 μM and a Ki value of 5.02 μM. UGT1A1-IN-1 binds to UGT1A1 at the same ligand-binding site as Bilirubin. Additionally, it displays favorable reactivity in human liver microsomes (HLM) and serves as a practical, high-affinity fluorescent probe substrate for UGT1A1, facilitating the study of bilirubin metabolism disorders and enzyme activity.

Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.

Cremophor EL is a nonionic surfactant. cremophor EL inhibits cellular metabolism and suppresses UGT1A1-mediated rhodopsin glucuronidation.

Cabotegravir (S/GSK1265744) (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor and inhibits the HIV-1 integrase catalyzed strand transfer reaction (IC50: 3.0 nM).

Ledipasvir D-tartrate (GS-5885 D-tartrate) is an HCV NS5A inhibitor that suppresses viral overphosphorylation and replication, and is used for the treatment of hepatitis C virus.

Grazoprevir is a drug approved for the treatment of hepatitis C. Grazoprevir is a second-generation hepatitis C virus protease inhibitor acting at the NS3/4a protease targets.

Grazoprevir, a second generation hepatitis C virus protease inhibitor acting at the NS3/4a protease targets, has good activity against a range of hepatitis C virus genotype variants, including some that are resistant to most currently used antiviral medic

Ledipasvir (acetone) (GS-5885 acetone) is an HCV NS5A polymerase inhibitor, used for the treatment of hepatitis C virus infection.

UK-157147 is a substrate for UGT1A1 (Km: 105 μM).

Mertansine is a tubulin inhibitor and an antibody-conjugable maytansinoid alkaloid. The IC50 of Mertansine against HCT-15 and A431 cells is 0.750 and 0.04nM.

Demethylzeylasteral (T-96), isolated from Tripterygium wilfordii, has anti-inflammatory, immunosuppressive and anti-tumor activities. It inhibits the invasion of triple-negative breast cancer by blocking the TGF-β signaling pathway, and it can significantly reduce atherosclerosis.

Licochalcone A is a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch with obvious anti-cancer effects.

1. Gitogenin, tigogenin, and solasodine are novel selective inhibitors of UGT1A4, and do not inhibit the activities of major human CYP isoforms. 2. Gitogenin and (25S)-5α-furastan-3β, 22, 26-triol are the inhibitors of enzyme α-glucosidase with IC50 value

1. Corylifol A (Corylinin) displays cytotoxic activity against HepG2 and Hep3B hepatocellular carcinoma cell lines, with IC50 values of 4.6 and 13.5 ug/ml, respectively. 2. Corylifol A and Biochanin A can be the potential uncouplers of neuronal nitric oxide synthase-postsynaptic density protein-95. 3. Corylifol A and bavachin are strong inhibitors of UDP-glucuronosyltransferase 1A1 (UGT1A1) with the inhibition kinetic parameters (Ki) values lower than 1 uM.4. Corylifol A and bakuchiol are naturally occurring potent inhibitors of hCE2, with low Ki values ranging from 0.62uM to 3.89 uM. 5. Corylifol A shows an inhibitory effect on IL-6-induced STAT3 promoter activity in Hep3B cells with IC50 values of 0.81 ± 0.15 uμ, it also inhibits STAT3 phosphorylation induced by IL-6 in Hep3B cells, suggests that corylifol A has antiinflammatory activity.

RO6889678 is HBV inhibitor with a complex ADME profile.

Ophiopogonin D' can activate SIRT1 in a dose-dependent manner. Ophiopogonin D' also noncompetitively inhibits UGT1A6 and UGT1A10.

1,2,3,6-Tetragalloylglucose (TeGG) has antioxidative activity, it also shows the most potent anticomplement activity (IC50 = 34 microM). 1,2,3,6-Tetragalloylglucose is also a potent inhibitor of UDP glucuronosyltransferase 1 A1 (UGT1A1, Ki = 1.68 μM).

5-Hydroxytryptophol-O-glucuronide is an authentic glucuronide standard and probe metabolite. It is utilized to assess the activity of human UGT1A6 in in vitro systems such as human liver microsomes and recombinant UGT1A6.

ABT-072, also known as potassium trihydrate, is a highly effective non-nucleoside inhibitor of the HCV NS5B polymerase, administered orally. This compound exhibits potent activity against HCV GT1a (with an EC50 of 1 nM) and HCV GT1b (with an EC50 of 0.3 nM).

GSK5852 (GSK2485852) is an HCV NS5B RdRp polymerase inhibitor, inhibiting NS5B with an IC50 of 50 nM. It exhibits antiviral effects against the hepatitis C virus (HCV) with EC50 values of 3.0 nM for GT1a and 1.7 nM for GT1b.

HCV-IN-39 (Compound 18a) is a potent, orally active nucleoside inhibitor of hepatitis C virus (HCV), effective against the GT1a replicon (EC50: 0.259 μM), GT1b replicon (EC50: 0.434 μM), and GT1b CES1 replicon (EC50: 0.069 μM).

NS5A-IN-4 (Compound 1.12) is a pan-genotypic, orally active inhibitor of the hepatitis C virus (HCV) NS5A, with IC50 values of 1.2, 2296, 4.6, 362, 10.3, and 693 pM against genotypes gT1b, gT1a, gT2a, gT3a, gT4a, and gT5a, respectively [1].