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Niflumic acid (Nifluril) 是钙离子激活的氯离子通道阻断剂，用于治疗类风湿性关节炎的镇痛剂和抗炎剂。

Mycophenolic acid (Mycophenolate) 是一种有效的非竞争性肌苷单磷酸脱氢酶 (IMPDH) 抑制剂，EC50为 0.24 µM。它对多种 RNA 病毒具有抗病毒作用。它也是一种免疫抑制剂，具有抗血管生成和抗肿瘤作用。

Jaceosidin 是从毛莲蒿中得到的一种黄酮类天然产物，可激活Bax，下调 Mcl-1 和 c-FLIP 的表达，诱导癌细胞凋亡。它能够降低炎性因子水平，激活 NF-κB，抑制COX-2的表达，具有抗癌和抗炎作用。

α-Angelica lactone 是一种乙烯基亲核试剂，也是一种天然存在的抗癌剂。它可以得到手性的 δ-氨基 γ，γ-二取代丁烯醇内酯羰基衍生物，并在 γ-碳上表现出亲电子俘获。它通过选择性增强谷胱甘肽-S-硫转移酶 (GST) 和 UDP-葡糖苷转移酶 (UGT) 解毒酶发挥强大的化学保护作用。

UGT8-IN-1 is a brain-permeable and orally-active inhibitor that specifically targets the ceramide galactosyltransferase enzyme (UGT8). By inhibiting UGT8, this compound has the potential to be employed in research pertaining to lysosomal storage disorders.

Deferiprone (Deferidone) 是口服活性铁螯合剂，可研究地中海贫血中的输血性铁过载。

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。

Gitogenin 是一种从Tribulus longipetalus 整株中分离出来的天然类固醇，是一种 UDP-葡萄糖醛酸转移酶 1A4 (UGT1A4) 和 α-葡萄糖苷酶的选择性抑制剂，其IC50分别为 0.69 µM (使用三氟拉嗪为底物) 和 37.2 μM，对人类主要细胞色素 P450 亚型的活性无抑制作用。

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。

Demethylzeylasteral (Demethylzeylasteral (T-96)) 分离自雷公藤，具有抗炎、免疫抑制和抗肿瘤活性。它通过阻断 TGF-β 信号通路，抑制三阴性乳腺癌的侵袭，它能显著减轻动脉粥样硬化。

Licochalcone A 是从名药甘草中分离得到的黄酮类天然产物，具有抗癌功效，对UDP-葡萄糖醛酸转移酶 (UGTs) 具有广泛抑制活性。它对 UGT1A1、1A3、1A4、1A6、1A7、1A9 和 2B7 具有强烈的抑制作用，IC50和Ki 值均低于5 μM。

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。

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

Ophiopogonin D'可以以剂量依赖性方式激活 SIRT1。 Ophiopogonin D'也非竞争性地抑制 UGT1A6 和 UGT1A10。

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)。

Hesperetin 是一种天然黄烷酮类物质，是人UGT 的广谱抑制剂，可诱导凋亡。

Cabotegravir (S GSK1265744) 是一种HIV 整合酶抑制剂，可研究艾滋病。它抑制OAT1 和OAT3，IC50值为 0.81 和0.41 μM。

Mertansine 是一种微管蛋白抑制剂，也是一种抗体可缀合的美登木素生物碱。Mertansine 对HCT-15和A431细胞的IC50分别是0.750和0.04nM。

(Rac)-Hesperetin is the racemate form of of Hesperetin. Hesperetin is a natural flavanone compound, and it exhibits potent inhibitory effects against human UGT activity, making it a broad-spectrum inhibitor. Furthermore, Hesperetin induces apoptosis through the activation of p38 MAPK.

Dapagliflozin-3-O-β-D-glucuronide is a metabolite of dapagliflozin . Dapagliflozin is a first generation selective sodium glucose cotransporter (SGLT) 2 inhibitor that blocks glucose transport.[1] Dapagliflozin is metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A9 to dapagliflozin-3-O-β-D-glucuronide, which is 2,600-fold less potent than the parent compound with regard to SGLT2 inhibition.[2]

(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.