glucuronidation

Uridine-5'-diphosphate disodium salt (UDP disodium salt) 是一种选择性 P2Y6受体激动剂，EC50为300 nM，对人 P2Y6受体的 pEC50为6.52。它可刺激炎症介质的产生、吞噬作用和血管收缩，催化多种底物的葡糖醛酸糖化反应，用于核酸生物合成。

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。

BMS-986242 是具有口服具有活力、强效的、选择性的 indoleamine-2,3-dioxygenase 1 抑制剂，可用于研究癌症。

Tacrolimus (Fujimycin) 属于大环内酯类抗生素，可以与 FKBP12 结合形成高亲和力复合物 (Ki=0.2 nM)，抑制钙 钙调蛋白依赖性蛋白磷酸酶的活性。Tacrolimus 是一种免疫抑制剂，通过抑制 IL-2 的释放，全面抑制 T 淋巴细胞的作用。

Cremophor EL 是一种非离子表面活性剂。Cremophor EL 抑制细胞代谢，抑制 UGT1A1 介导的大黄素葡萄糖醛酸化。

Pyrimidine (Metadiazine) 是内源性代谢产物的一种。

Epmedin C (Baohuoside-VI) 是天然化合物，在切除卵巢的小鼠体内与雌性激素作用相似。

Nebicapone is a reversible catechol-O-methyltransferase (COMT) inhibitor and is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of CO

(-)-Sitagliptin carbamoyl glucuronide is a minor phase II metabolite of the dipeptidyl peptidase 4 (DPP-4) inhibitor (-)-sitagliptin . (-)-Sitagliptin carbamoyl glucuronide is formed by N-carbamoyl glucuronidation and has been found in rat and dog plasma following administration of (-)-sitagliptin.

Febuxostat acyl glucuronide is a metabolite of the xanthine oxidoreductase inhibitor febuxostat . Febuxostat acyl glucuronide is formed via glucuronidation of febuxostat by uridine diphosphate-glucuronosyltransferases (UGTs).

4’-hydroxy Atomoxetine glucuronide is a metabolite of the norepinephrine transporter (NET) inhibitor atomoxetine .1It is formed from atomoxetine by glucuronidation of the intermediate metabolite 4-hydroxy atomoxetine.2 1.Todor, I., Popa, A., Neag, M., et al.Evaluation of a potential metabolism-mediated drug-drug interaction between atomoxetine and bupropion in healthy volunteersJ. Pharm. Pharm. Sci.19(2)198-207(2016) 2.Sauer, J.-M., Ring, B.J., and Witcher, J.W.Clinical pharmacokinetics of atomoxetineClin. Pharmacokinet.44(6)571-590(2005)

(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.

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)

1-Salicylate Glucuronide (Salicylic Acid b-D-O-Glucuronide) 是水杨酸在体内经葡萄糖醛酸化作用代谢后的产物，具有促进排泄的功能。

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.

Aurantio-obtusin 是从决明子中分离出的蒽醌类化合物，具有抗炎、抗凝血、抗氧化、抗高血压的活性。它能抑制 IgE 介导的肥大细胞和过敏模型中的过敏反应，具有研究过敏相关疾病的潜力。在大鼠中，它通过内皮细胞 PI3K AKT eNOS 依赖信号通路放松全身动脉，是潜在的新型血管扩张剂。

CN128, an orally bioavailable iron chelator, features a side chain hydroxy group serving as an alternate sacrificial glucuronidation site to mitigate metabolic inactivation at the 3-hydroxy group. When administered at doses of 150 and 450 µmol kg, CN128 enhances iron mobilization by 24.8% in a 59Fe-ferritin-loaded rat model of iron overload.

UGT1A1-IN-1 (化合物2) 为一种非竞争性UGT1A1抑制剂，具有5.02 μM的Ki值，有效阻断UGT1A1介导的1-O-葡糖苷酸化反应。此化合物能与UGT1A1在胆红素相同的配体结合位点上相结合。此外，UGT1A1-IN-1还可用作UGT1A1活性“开启”的荧光探针底物。