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14

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T40046	UGT8-IN-1 UGT8-IN-1
	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.
T36826	Acetaminophen Glucuronide (sodium salt)
	Acetaminophen glucuronide is an inactive metabolite of the analgesic and antipyretic agent acetaminophen . It is formed via glucuronidation of acetaminophen by the UDP-glucuronosyltransferase (UGT) isoforms UGT1A6, UGT1A9, UGT1A1, and UGT2B15.
T35952	all-trans Retinoyl β-D-Glucuronide
	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.
T37484	1-Salicylate Glucuronide
	1-Salicylate glucuronide is a metabolite of salicylic acid and aspirin .1It is formed from salicylic acid primarily by the UDP-glucuronosyltransferase (UGT) isoform UGT1A9 but also by a variety of other UGT isoforms and from aspirinviasalicylic acid as an intermediate. 1.Kuehl, G.E., Bigler, J., Potter, J.D., et al.Glucuronidation of the aspirin metabolite salicylic acid by expressed UDP-glucuronosyltransferases and human liver microsomesDrug Metab. Dispos.34(2)199-202(2006)
T37117	Etodolac Acyl Glucuronide
	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)
T36794	Dolutegravir O-β-D-Glucuronide
	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...
T37852	Chlorzoxazone N-Glucuronide
	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.
T35939	Dabigatran Acyl-β-D-Glucuronide
	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.
T36071	Silodosin Glucuronide (sodium salt)
	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.
T62328	Cabotegravir sodium
	Cabotegravir sodium 是一种 HIV 整合酶的高效抑制剂，能够作用于 HIVADA (IC50: 2.5 nM)。Cabotegravir sodium 主要由尿苷二磷酸葡萄糖醛酸转移酶 (UGT) 1A1 代谢，与其他抗逆转录病毒药物 (ARVs) 相互作用的可能性较小。
T35619	Dapagliflozin-3-O-β-D-Glucuronide
	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]
T35845	(R,S)-Carvedilol Glucuronide
	(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.
T37005	Estriol 3-β-D-Glucuronide (sodium salt)
	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).
T83873	Dabigatran Acyl-β-D-Glucuronide TFA Dabigatran β-1-O-Acyl Glucuronide
	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)。

化合物

Cat.No: T40046

Synonym: UGT8-IN-1

Acetaminophen Glucuronide (sodium salt)

Cat.No: T36826

all-trans Retinoyl β-D-Glucuronide

Cat.No: T35952

1-Salicylate Glucuronide

Cat.No: T37484

Etodolac Acyl Glucuronide

Cat.No: T37117

Dolutegravir O-β-D-Glucuronide

Cat.No: T36794

Chlorzoxazone N-Glucuronide

Cat.No: T37852

Dabigatran Acyl-β-D-Glucuronide

Cat.No: T35939

Silodosin Glucuronide (sodium salt)

Cat.No: T36071

Cabotegravir sodium

Cat.No: T62328

Dapagliflozin-3-O-β-D-Glucuronide

Cat.No: T35619

(R,S)-Carvedilol Glucuronide

Cat.No: T35845

Estriol 3-β-D-Glucuronide (sodium salt)

Cat.No: T37005

Dabigatran Acyl-β-D-Glucuronide TFA

Cat.No: T83873

Synonym: Dabigatran β-1-O-Acyl Glucuronide

Cat. No.	Product Name	Target	Signaling Pathways
T7995	α-Angelica lactone α-当归内酯,当归内酯,Alpha-Angelica Lactone	Others; GST	Others; oxidation-reduction
	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。
T3880	Silydianin 水飞蓟宁,Silidianin	Phosphatase	Metabolism
	Silydianin (Silidianin) 是一种水飞蓟的活性成分，具有抗胶原酶和抗弹性酶作用，对氧化产物的体外产生和释放具有抑制作用。它是一种天然蛋白酪氨酸磷酸酶 1B 抑制剂，其IC50=17.38 μM。
T2565	Hesperetin 橙皮素	Apoptosis; p38 MAPK; 5-HT Receptor; Autophagy; TGF-beta/Smad	Apoptosis; Autophagy; GPCR/G Protein; MAPK; Neuroscience; Stem Cells
	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。
T3824	Jaceosidin	Apoptosis; BCL; COX; UGT	Apoptosis; Immunology/Inflammation; Metabolism; Neuroscience
	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。
T12667	(Rac)-Hesperetin	Others	Others
	(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.
TN5356	Epiglobulol
	Epiglobulol shows antibacterial activities, it can strongly inhibit the growth of foodborne microorganisms. Epiglobulol can inhibit the recombinant human UDP-glucuronosyltransferase (UGT) 2B7, it may serve as valuable lead structures for the design of pot

天然产物

α-Angelica lactone

Cat.No: T7995

Synonym: α-当归内酯,当归内酯,Alpha-Angelica Lactone

Target: Others, GST

Cat.No: T3880

Synonym: 水飞蓟宁,Silidianin

Target: Phosphatase

Cat.No: T2565

Synonym: 橙皮素

Target: Apoptosis, p38 MAPK, 5-HT Receptor, Autophagy, TGF-beta/Smad

Cat.No: T3824

Target: Apoptosis, BCL, COX, UGT

(Rac)-Hesperetin

Cat.No: T12667

Target: Others

Cat.No: TN5356

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