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17

抑制剂 & 化合物

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天然产物

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Cat. No. Product Name Target Signaling Pathways
T9054 RO6889678

HBV Microbiology/Virology
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。
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.
T19685 Faldaprevir

BI-201335,BI201335,BI 201335

Faldaprevir is an effective NS3/NS4A protease inhibitor potentially for the treatment of HCV infection. Faldaprevir is known to inhibit P-glycoprotein, CYP3A4, and UDP-glucuronosyltransferase 1A1.
T71215 Faldaprevir sodium

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.
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)
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.
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.
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.
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)
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).
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...
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.
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.
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)。
T37004 Estradiol 3-sulfate 17β-Glucuronide (potassium salt)

Estradiol 3-sulfate is a sulfated form of the steroid hormone 17β-estradiol , and is common in fetal plasma and in the breast tissues of patients with mammary carcinoma. Sulfated estrogens, including estradiol 3-sulfate, can be converted back to the parent compound by sulfatases. Estradiol 3-sulfate 17β-glucuronide is a metabolite of estradiol 3-sulfate that has been modified by a UDP-glucuronosyltransferase. Glucuronidation of estrogens enhances their utilization by anion transporters, most com...
T37900 UDP-Glucuronic Acid (sodium salt hydrate)

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)
T37902 Uridine-5'-diphosphoglucuronic Acid (sodium salt hydrate)

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)

化合物

RO6889678
Cat.No: T9054
Synonym:
Target: HBV
Acetaminophen Glucuronide (sodium salt)
Cat.No: T36826
Synonym:
Target:
Faldaprevir
Cat.No: T19685
Synonym: BI-201335,BI201335,BI 201335
Target:
Faldaprevir sodium
Cat.No: T71215
Synonym:
Target:
Etodolac Acyl Glucuronide
Cat.No: T37117
Synonym:
Target:
all-trans Retinoyl β-D-Glucuronide
Cat.No: T35952
Synonym:
Target:
Chlorzoxazone N-Glucuronide
Cat.No: T37852
Synonym:
Target:
Silodosin Glucuronide (sodium salt)
Cat.No: T36071
Synonym:
Target:
1-Salicylate Glucuronide
Cat.No: T37484
Synonym:
Target:
Estriol 3-β-D-Glucuronide (sodium salt)
Cat.No: T37005
Synonym:
Target:
Dolutegravir O-β-D-Glucuronide
Cat.No: T36794
Synonym:
Target:
Dabigatran Acyl-β-D-Glucuronide
Cat.No: T35939
Synonym:
Target:
(R,S)-Carvedilol Glucuronide
Cat.No: T35845
Synonym:
Target:
Dabigatran Acyl-β-D-Glucuronide TFA
Cat.No: T83873
Synonym: Dabigatran β-1-O-Acyl Glucuronide
Target:
Estradiol 3-sulfate 17β-Glucuronide (potassium salt)
Cat.No: T37004
Synonym:
Target:
UDP-Glucuronic Acid (sodium salt hydrate)
Cat.No: T37900
Synonym:
Target:
Uridine-5'-diphosphoglucuronic Acid (sodium salt hydrate)
Cat.No: T37902
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
TN1160 1,2,3,6-Tetragalloylglucose

1,2,3,6-Tetra-O-galloyl-β-D-glucose,1,2,3,6-四-O-没食子酰-Β-D-葡萄糖,TeGG

LDL; UGT Metabolism
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)。
T4S0145 Corylifol A

Corylinin,补骨脂异黄酮A

hCE; STAT; UGT JAK/STAT signaling; Metabolism; Stem Cells
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。
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

1,2,3,6-Tetragalloylglucose
Cat.No: TN1160
Synonym: 1,2,3,6-Tetra-O-galloyl-β-D-glucose,1,2,3,6-四-O-没食子酰-Β-D-葡萄糖,TeGG
Target: LDL, UGT
Corylifol A
Cat.No: T4S0145
Synonym: Corylinin,补骨脂异黄酮A
Target: hCE, STAT, UGT
Epiglobulol
Cat.No: TN5356
Synonym:
Target:
TargetMol Loading
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