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UGT

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UGT8-IN-1
T400462414349-93-0
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.
    7-10 days
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    Hesperetin
    T2565520-33-2
    Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.
    • $38
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    TargetMol | Citations Cited
    Silodosin Glucuronide (sodium salt)
    T36071879292-24-7
    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.
    • $838
    35 days
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    (R,S)-Carvedilol Glucuronide
    T35845114869-83-9
    (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.
    • $1,210
    35 days
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    Acetaminophen Glucuronide (sodium salt)
    T36826120595-80-4
    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.
    • $110
    35 days
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    Dabigatran Acyl-β-D-Glucuronide
    T359391015167-40-4
    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.
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      all-trans Retinoyl β-D-Glucuronide
      T35952401-10-5
      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.
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      Etodolac Acyl Glucuronide
      T3711779541-43-8
      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)
      • $485
      35 days
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      Naringenin-7-O-β-D-Glucuronide
      TN72621237479-07-0
      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.
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      Chlorzoxazone N-Glucuronide
      T37852
      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.
      • $233
      35 days
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      Silydianin
      T388029782-68-1
      Silydianin (Silidianin) exerts inhibition of UGT in human liver. Silydianin exerts inhibition of OATP1B1, OATP1B3 (unknown origin) expressed in HEK293 cells. Silydianin exerts inhibition of OATP2B1 (unknown origin) expressed in MDCK2 cells.
      • $39
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      α-Angelica lactone
      T7995591-12-8
      α-Angelica lactone has cardiotonic activity, may exert their effects by providing an increased contraction-dependent calcium pool to be released upon systolic depolarization.
      • $29
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      1-Salicylate Glucuronide
      T374847695-70-7
      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)
      • $170
      35 days
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      Dolutegravir O-β-D-Glucuronide
      T367941485692-21-4
      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)
      • $1,530
      35 days
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      rac-Hesperetin-13C-d3
      TMIJ-0108
      rac-Hesperetin-13C-d3 the 13C and deuterated compound of rac-Hesperetin. rac-Hesperetin has a CAS number of 69097-99-0. (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.
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      20 days
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      (Rac)-Hesperetin
      T1266769097-99-0
      (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.
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      7-10 days
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      Jaceosidin
      T382418085-97-7
      Jaceosidin has anti-oxidative activity. Jaceosidin has anti-inflammatory activity, also a microglial inhibitor with anti-neuroinflammation activity. aceosidin has anticancer activity, modulates the ERK/ATM/Chk1/2 pathway, leading to inactivation of the Cd
      • $52
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      Cabotegravir sodium
      T623281051375-13-3
      Cabotegravir sodium is a potent inhibitor of HIV integrase and is able to act on HIVADA (IC50: 2.5 nM). cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1 and is less likely to interact with other antiretroviral drugs (ARVs). Antileishmanial agent-12
      • $31
      7-10 days
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      Estriol 3-β-D-Glucuronide (sodium salt)
      T3700515087-06-6
      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).
      • $540
      35 days
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      Epiglobulol
      TN535688728-58-9
      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
      • $260
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      Dapagliflozin-3-O-β-D-Glucuronide
      T356191351438-75-9
      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]
      • $353
      35 days
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      Dabigatran Acyl-β-D-Glucuronide TFA
      T83873
      Dabigatran acyl-β-D-glucuronide, an active metabolite of the thrombin inhibitor dabigatran, is synthesized predominantly through the action of the UDP-glucuronosyltransferase isoform UGT2B15. This compound, at a concentration of 0.46 µM, effectively prolongs activated partial thromboplastin time (aPTT) in isolated human platelet-poor plasma.
      • $1,690
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