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).
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.
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.
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)
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.
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.
Methyl-PEG4-acyl chloride is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules. This linker enables selective protein degradation by leveraging the ubiquitin-proteasome system within cells.
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.
Indomethacin acyl glucuronide, a metabolite of the COX inhibitor indomethacin (1), embodies an essential byproduct formed during the metabolic processing of indomethacin.
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.
Acyl Carrier Protein (ACP) (65-74) is an active fragment of ACP, a component of plastid-located plant fatty acid synthetase. It covalently binds acyl groups via the prosthetic group, 4-phosphopantetheine.