udp-glucuronosyltransferase

RO6889678 是高效的 HBV 衣壳结构抑制剂，其吸收、分布、代谢和排泄特征较为复杂。它可通过 CYP3A4 介导的氧化作用进行代谢，以及通过 UDP-葡萄糖醛酸基转移酶 UGT1A3 和 UGT1A1 介导的直接葡萄糖醛酸化作用进行代谢。它是一种诱导剂，可作用于人肝细胞中 CYP3A4 和共调节蛋白。

Bis(4-nitrophenyl) phosphate （BNPP) 抑制UDP-半乳糖，可用于研究糖基转移酶膜拓扑结构。

3-Methyl-2-nitrophenol是一种低特异性的UDP-glucuronosyltransferase底物，广泛应用于生物化学实验和药物合成研究。

(R,S)-Carvedilol glucuronide is a racemic mixture of the carvedilol metabolites (R)-carvedilol glucuronide and (S)-carvedilol glucuronide. (R)-Carvedilol glucuronide is formed via glucuronidation of (R)-carvedilol by the UDP-glucuronosyltransferase (UGT) isoforms UGT1A1 and UGT2B4. (S)-Carvedilol glucuronide is formed via glucuronidation of (S)-carvedilol by UGT2B4 and UGT2B7.

Dabigatran acyl-β-D-glucuronide is a major active metabolite of the thrombin inhibitor dabigatran . The prodrug of dabigatran, dabigatran etexilate , is hydrolyzed by plasma esterases to form dabigatran, which is metabolized primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT2B15 to form dabigatran acyl-β-D-glucuronide. Dabigatran acyl-β-D-glucuronide increases activated partial thromboplastin time (aPTT) in isolated human platelet-poor plasma equipotently to dabigatran.

all-trans Retinoyl β-D-glucuronide is a metabolite of all-trans retinoic acid formed by the UDP-glucuronosyltransferase (UGT) system. It is rapidly converted to all-trans retinoic acid following in vitro or in vivo administration.

Silodosin glucuronide is an active metabolite of the α1A-adrenergic receptor antagonist silodosin . It is formed from silodosin by the UDP-glucuronosyltransferase (UGT) isoform UGT2B7. Silodosin glucuronide is toxic to rats with an LD50 value of 0.347 mg kg.

Dolutegravir O-β-D-glucuronide is a metabolite of the HIV integrase inhibitor dolutegravir .1It is formed from dolutegravir primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A1in vivobut is also metabolized by UGT1A9 in human liver and kidney microsomes and UGT1A3 in human intestinal microsomes.2,1 1.Liu, S.N., Lu, J.B., Watson, C.J.W., et al.Mechanistic assessment of extrahepatic contributions to glucuronidation of integrase strand transfer inhibitorsDrug Metab. Dispos.47(5)535-544(2019) 2.Reese, M.J., Savina, P.M., Generaux, G.T., et al.In vitro investigations into the roles of drug transporters and metabolizing enzymes in the disposition and drug interactions of dolutegravir, a HIV integrase inhibitorDrug Metab. Dispos.41(2)353-361(2013)

Estriol 3-β-D-glucuronide is a metabolite of estriol . It is formed from estriol by the UDP-glucuronosyltransferase (UGT) isoform UGT1A10. Estriol 3-β-D-glucuronide binds to basolateral and canalicular liver plasma membranes with Kd values of 85 and 164 μM, respectively. It competitively inhibits the hydrolysis of 4-methylumbelliferyl-β-D-glucuronide and is a substrate for hydrolysis by Klotho-human IgG1 Fc protein (KLFc).

Etodolac acyl glucuronide is a phase II metabolite of the non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor etodolac .1It is formedviaglucuronidation of etodolac by the UDP-glucuronosyltransferase (UGT) isoforms UGT1A9, UGT1A10, and UGT2B7. 1.Kutsuno, Y., Itoh, T., Tukey, R.H., et al.Glucuronidation of drugs and drug-induced toxicity in humanized UDP-glucuronosyltransferase 1 miceDrug Metab. Dispos.42(7)1146-1152(2014)

Propofol β-D-Glucuronide（2,6 -二异丙基Β- D -吡喃葡萄糖酸）异丙酚硫酸盐（一种短效麻醉剂）主要的无活性代谢产物，由UDP-葡萄糖醛酸转移酶（UGT）介导生成，可用于研究睡眠剥夺（SD）。

Chlorzoxazone N-glucuronide is a phase II metabolite of the skeletal muscle relaxant chlorzoxazone . Chlorzoxazone N-glucuronide is formed via glucuronidation of chlorzoxazone by the UDP-glucuronosyltransferase (UGT) isoform UGT1A9.

UDP-Glucuronic acid is a nucleoside diphosphate sugar that is a source of glucuronic acid for polysaccharide biosynthesis. This compound can be used for the formation of many glucuronides with various aglycones.1 1.Green, M.D., and Tephly, T.R.Glucuronidation of amine substrates by purified and expressed UDP-glucuronosyltransferase proteinsDrug Metab. Dispos.26(9)860-867(1998)

Uridine-5'-diphosphoglucuronic acid is a nucleoside diphosphate sugar that is a source of glucuronic acid for polysaccharide biosynthesis. This compound can be used for the formation of many glucuronides with various aglycones.1 1.Green, M.D., and Tephly, T.R.Glucuronidation of amine substrates by purified and expressed UDP-glucuronosyltransferase proteinsDrug Metab. Dispos.26(9)860-867(1998)

Corylifol A (Corylinin) 是补骨脂中的一种天然产物，可抑制IL-6 诱导的STAT3激活和磷酸化，IC50值为0.81 μM。

Faldaprevir sodium is a potent NS3 NS4A protease inhibitor potentially for the treatment of HCV infection. Faldaprevir is known to inhibit P-glycoprotein, CYP3A4, and UDP-glucuronosyltransferase 1A1.

Dabigatran acyl-β-D-glucuronide是凝血酶抑制剂dabigatran的一种活性代谢产物，主要通过UDP-葡萄糖醛酸转移酶(UGT)的UGT2B15亚型形成。在人体去除血小板的贫血浆中，Dabigatran acyl-β-D-glucuronide (0.46 µM) 能增加活化部分凝血活酶时间(aPTT)。

Chenodeoxycholic acid 24-acyl-β-D-glucuronide (CDCA-24G), a metabolite of CDCA, is synthesized from CDCA via the action of the UDP-glucuronosyltransferase (UG UT) isoform UGT1A3.

1,2,3,6-Tetragalloylglucose (TeGG) 是 UDP-葡萄糖醛酸转移酶 1 家族成员，是多肽A1 的抑制剂(Ki:1.68 μM)。

Naringenin-7-O-β-D-glucuronide, a metabolite of the flavonoid naringenin, is predominantly synthesized through the action of UDP-glucuronosyltransferase (UGT) isoforms UGT1A1, UGT1A3, UGT1A6, and UGT1A9.