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.

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.

6-Chloro-3-indolyl-β-D-Glucuronide (cyclohexylammonium salt) is a chromogenic substrate for β-glucuronidase and can be utilized in the histochemical analysis of β-glucuronidase activity.

Oroxylin A 7-O-β-d-glucuronide was a new alkaloid which found in the bulbs of Lycoris radiata.

Luteolin-3-O-beta-D-glucuronide effectively inhibits nitrite production in macrophages.

Glycyrrhetic acid 3-O-β-D-glucuronide is a potent sweetener (relative sweetness to sucrose: x 941).

DiosMetin 7-O-β-D-Glucuronide, an antioxidant constituent found in the fruits of Luffa cylindrical, supplies antioxidant benefits when sponge gourds are consumed.

Mycophenolic acid glucuronide is the glucuronide metabolite of mycophenolic acid in human plasma.

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.

Tolmetin β-D-Glucuronide has reactive properties with human serum albumin, allowing identification of the binding site and reaction mechanism by tandem mass spectrometry.

(±)-4-hydroxy Propranolol β-D-glucuronide is a metabolite of (±)-4-hydroxy propranolol , which is a metabolite of propranolol. The apparent half-life of (±)-4-hydroxy propranolol β-D-glucuronide is similar to propranolol and 4-hydroxy propranolol. Propranolol is a β-adrenergic antagonist, and the active enantiomer, (S)-(-)-propranolol , has log Kd values of -8.16, -9.08, and -6.93 for β1, β2, and β3, respectively.

Propofol β-D-glucuronide is a metabolite of propofol sulfate, a short-acting anesthetic agent. The metabolite is generated through the glucuronidation of propofol by uridine diphosphate glucuronosyltransferases, and propofol metabolism appears to occur more rapidly in women than in men. [1] [2]

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)

Perindopril acyl-β-D-glucuronide is a metabolite of the ACE inhibitor perindopril [1].

Naringenin-7-O-beta-D-glucuronide is a natural product

4-Methylumbelliferyl β-D-glucuronide is a useful organic compound for research related to life sciences. The catalog number is T65323 and the CAS number is 6160-80-1.

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).

Isoscutellarein 8-O-β-D-glucuronide, a flavonoid antioxidant, can be isolated from the seeds of Theobroma grandiflorum [1] [2].

Ezetimibe-d4 Phenoxy ß-D-Glucuronide is a deuterated compound of Ezetimibe Phenoxy ß-D-Glucuronide. Ezetimibe Phenoxy ß-D-Glucuronide has a CAS number of 190448-57-8.

Eriodictyol 7-O-β-D-glucuronide ethyl ester is a natural product for research related to life sciences. The catalog number is TN5523 and the CAS number is 847025-48-3.

Diclofenac Acyl Glucuronide is a major biliary metabolite of Diclofenac (GLXC-07892), a nonsteroidal antiinflammatory drug and COX inhibitor.

Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-beta-O-glucuronide) exhibits antioxidant activity. Flavonoid glucuronides can be deconjugated by microsomal α²-glucuronidase from various human cells.

β-D-Glucuronide-pNP-carbonate is an ADC linker used in the synthesis of antibody-drug conjugates (ADCs).

Resveratrol-4'-O-D-Glucuronide has anti-fat accumulation properties, is metabolized by resveratrol, and can be used in metabolism-related studies.

Ethyl-β-D-glucuronide-d5 is a deuterated compound of Ethyl-β-D-glucuronide. Ethyl-β-D-glucuronide has a CAS number of 17685-04-0. Ethyl glucuronide is an endogenous metabolite.

Naringenin 7-O-β-D-glucuronide methyl ester is a natural product for research related to life sciences. The catalog number is TN5524 and the CAS number is 1985597-72-5.

Celecoxib carboxylic acid acyl-β-D-glucuronide is a phase II metabolite of celecoxib . Celecoxib is an anti-inflammatory compound from the diaryl heterocycle class that selectively inhibits cyclooxygenase-2 (COX-2; IC50s = 22.9 and 0.05 μM for COX-1 and COX-2, respectively). Celecoxib carboxylic acid acyl-β-D-glucuronide is a minor metabolite, accounting for 2% of the administered dose in human urine and rat bile.

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]

5-Hydroxy tryptophol β-D glucuronide-d4 is a deuterated compound of 5-Hydroxy tryptophol β-D glucuronide.

Curcumin-β-D-glucuronide, a principal metabolite detected in hepatic tissue and portal blood following oral consumption of Curcumin, is utilized in colon cancer research [1] [2].

Propofol-d17 β-D glucuronide is a deuterated compound of Propofol7 β-D glucuronide.

Estriol 16α-(β-D-glucuronide), an endogenous metabolite found in urine, is utilized in pregnancy research [1] [2].

Wogonin 7-O-beta-D-glucuronide methyl ester, a natural product, is isolated from [Huanglian Jiedutang].

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).

Raloxifene 6,4'-Bis-β-D-glucuronide, a metabolite of Raloxifene, acts as a selective antagonist of the estrogen receptor used for osteoporosis prevention.

Compound 5, DDC 3′-O-β-D-glucuronide, is a drug metabolite with properties that inhibit the fibrillization and oligomerization of Aβ42, suggesting its potential utility in Alzheimer's disease research [1].

Levothyroxine acyl glucuronide (Thyroxine Acyl-β-D-glucuronide) is the acyl glucuronide conjugate of thyroxine (T4), an endogenous metabolite.

Chenodeoxycholic acid 24-acyl-β-D-glucuronide (CDCA-24G), a metabolite of CDCA, is synthesized from CDCA via the action of the UDP-glucuronosyltransferase (UG UT) isoform UGT1A3.

Indomethacin acyl glucuronide, a metabolite of the COX inhibitor indomethacin (1), embodies an essential byproduct formed during the metabolic processing of indomethacin.

Estradiol 17-(β-D-glucuronide) (E217G) is an estrogen metabolite formed in the liver and subsequently excreted in bile.1It acts as a substrate of the multidrug resistance protein 2 (MRP2; Km= 75 μM), and through MRP2-mediated transport, functions as a cholestatic agent, decreasing bile flow.1,2In addition to binding to the MRP2 transport site, E217G has been shown to bind to an allosteric site that through positive cooperativity activates its own transportviaMRP2 and the transport of other MRP2 substrates, including the non-cholestatic estrogen metabolite, estradiol 3-(β-D-glucuronide) .2,3E217G has also been reported to be transported by MDR1, MRP1, MRP3, MRP4, MRP7, ABCG2 (a breast cancer resistance protein transporter), and the rat organic anion-transporting polypeptides 1-4.2 1.Loe, D.W., Almquist, K.C., Cole, S.P., et al.ATP-dependent 17β-estradiol 17-(β-D-glucuronide) transport by multidrug resistance protein (MRP). Inhibition by cholestatic steroidsThe Journal of Biological Chemisty271(16)9683-9689(1996) 2.Gerk, P.M., Li, W., and Vore, M.Estradiol 3-glucuronide is transported by the multidrug resistance-associated protein 2 but does not activate the allosteric site bound by estradiol 17-glucuronideDrug Metabolism and Disposition32(10)1139-1145(2004) 3.Gerk, P.M., Li, W., Megaraj, W., et al.Human multidrug resistance protein 2 transports the therapeutic bile salt tauroursodeoxycholateJournal of Pharmacology and Experimental Therapeutics320(2)893-899(2007)

Ethynyl estradiol 3-β-D-glucuronide is a metabolite of ethynyl estradiol that can be detected in urine.1,2It is used as a marker of estrogen contamination in fresh and saltwater.2 1.Hadd, H.E., Slikker, W., Jr., and Helton, E.D.The synthesis and characterization of the glucopyranosiduronic acids of 17a-ethynylestradiol-17bJ. Steroid Biochem.13(9)1107-1114(1980) 2.Griffith, D.R., Soule, M.C.K., Eglinton, T.I., et al.Steroidal estrogen sources in a sewage-impacted coastal oceanEnviron. Sci.: Processes Impacts18(8)931-1106(2016)

2,3,4-Tri-O-acetyl-β-D-glucuronide methyl ester is a synthetic intermediate in the synthesis of prodrug forms of the antitumor antibiotic daunomycin .1 1.Leenders, R.G.G., and Scheeren, H.W.Synthesis and evaluation of novel daunomycin-phosphate-sulfate-β-glucuronide and -β-glucoside prodrugs for application in ADEPTBioorg. Med. Chem. Lett.5(24)2975-2980(1995)

Simvastatin Acyl-β-D-glucuronide, a metabolite formed from Simvastatin, acts as a competitive inhibitor of HMG-CoA reductase, showcasing a potent Ki of 0.2 nM.

6-hydroxyapigenin-6-O-β-D-glucoside-7-O-β-D-glucuronide is a natural product from Carthamus tinctorius Linn.

Ferulic acid acyl-β-D-glucoside, a metabolite of Ferulic Acid, is a novel inhibitor of fibroblast growth factor receptor 1 (FGFR1). It exhibits IC50 values of 3.78 µM and 12.5 µM for FGFR1 and FGFR2, respectively.

Telmisartan acyl-β-D-glucuronide is a major metabolite of the angiotensin II receptor antagonist telmisartan . It does not bind human serum albumin and is cleared from rat plasma with a clearance rate of 180 ml/min/kg following intravenous administration.

Oroxylin A 7-O-β-D-glucuronide methyl ester, a natural product, can be isolated from the roots of *Scutellaria baicalensis* Georgi [1].