glucuronidation

Uridine-5'-diphosphate disodium salt (UDP disodium salt) is a specific agonist of the P2Y6 receptors (EC50 = 13 nM for human P2Y6), stimulating the production of inflammatory mediators, phagocytosis, and vasoconstriction. Uridine-5'-diphosphate disodium salt also acts as an antagonist of P2Y14.

BMS-986242 is an orally active, potent, and selective indoleamine-2,3-dioxygenase 1 (IDO1) inhibitor, suitable for cancer research.

RO6889678 is HBV inhibitor with a complex ADME profile.

Tacrolimus (FK506, Fujimycin) is a macrolide immunosuppressant that binds to FKBP12 to form a high-affinity complex (Ki = 0.2 nM), which inhibits calcineurin phosphatase activity, thereby suppressing T lymphocyte signal transduction and the transcription and release of IL-2. It exerts potent immunosuppressive effects and can be used to induce immunosuppression models.

Cremophor EL is a nonionic surfactant. cremophor EL inhibits cellular metabolism and suppresses UGT1A1-mediated rhodopsin glucuronidation.

Pyrimidine (Metadiazine)s are heterocyclic, six-membered, nitrogen-containing carbon ring structures, with uracil, cytosine and thymine being the basal structures of ribose-containing nucleosides (uridine, cytidine, and thymidine respectively), or deoxyribose-containing deoxynucleosides, and their corresponding ribonucleotides or deoxyribonucleotides. Pyrimidines serve essential functions in human metabolism as ribonucleotide bases in RNA (uracil and cytosine), and as deoxyribonucleotide bases in DNA (cytosine and thymine), and are linked by phosphodiester bridges to purine nucleotides in double-stranded DNA, in both the nucleus and the mitochondria. Pyrimidine activated sugars are also involved in polysaccharide and phospholipid synthesis, glucuronidation in detoxification processes, glycosylation of proteins and lipids and in the recently identified novel endothelium-derived vasoactive dinucleotides.

Nebicapone is a reversible catechol-O-methyltransferase (COMT) inhibitor and is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of CO

Fenretinide glucuronide is a metabolite formed through the glucuronidation of Fenretinide. This process enhances the water solubility of Fenretinide and facilitates its excretion. Fenretinide glucuronide shows potential for research in the field of cancer.

1-Piperonylpiperazine (MDBP) undergoes demethylenation followed by methylation to form N-(4-hydroxy-3-methoxybenzyl)piperazine, with partial glucuronidation or sulfation occurring afterwards. It can alter the distribution and metabolism of 3,4-methylenedioxymethamphetamine (MDMA) in the brain and peripheral organs. Furthermore, 1-Piperonylpiperazine has the potential to inhibit the neurotoxic effects induced by MDMA.

Epmedin C (Baohuoside-VI) was metabolized via desugarization, dehydrogenation, hydrogenation, dehydroxylation, hydroxylation, demethylation and glucuronidation pathways in vivo. It has potential activity against osteoporosis by stimulating osteoblasts.

(-)-Sitagliptin carbamoyl glucuronide is a minor phase II metabolite of the dipeptidyl peptidase 4 (DPP-4) inhibitor (-)-sitagliptin . (-)-Sitagliptin carbamoyl glucuronide is formed by N-carbamoyl glucuronidation and has been found in rat and dog plasma following administration of (-)-sitagliptin.

Febuxostat Acyl Glucuronide is the primary metabolite of the potent xanthine oxidase (XO) inhibitor Febuxostat. It is formed through the glucuronidation of the carboxylic acid group of Febuxostat, a process mediated by UDP-glucuronosyltransferase (UGT) enzymes. The production of this acyl glucuronide is a major elimination pathway for the parent drug. Researching this metabolite is essential for characterizing metabolic clearance, understanding drug-drug interactions, and evaluating the pharmacokinetic variability of Febuxostat across different patient populations, including those with UGT enzymatic polymorphisms.

4'-hydroxy Atomoxetine glucuronide is a metabolite of the norepinephrine transporter (NET) inhibitor atomoxetine .1It is formed from atomoxetine by glucuronidation of the intermediate metabolite 4-hydroxy atomoxetine.2 1.Todor, I., Popa, A., Neag, M., et al.Evaluation of a potential metabolism-mediated drug-drug interaction between atomoxetine and bupropion in healthy volunteersJ. Pharm. Pharm. Sci.19(2)198-207(2016) 2.Sauer, J.-M., Ring, B.J., and Witcher, J.W.Clinical pharmacokinetics of atomoxetineClin. Pharmacokinet.44(6)571-590(2005)

(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.

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-Salicylate Glucuronide (Salicylic Acid b-D-O-Glucuronide) is a metabolite of salicylic acid after glucuronidation, promoting excretion.

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.

1. Biotransformation of glucoAurantio-obtusin towards Aurantio-obtusin increased the toxicity of irinotecan through increased inhibition of SN-38 glucuronidation. 2. Aurantio-obtusin, stimulated chemotactic migration of MC3T3-E1 osteoblast cells in a conc

CN128, an orally bioavailable iron chelator, features a side chain hydroxy group serving as an alternate sacrificial glucuronidation site to mitigate metabolic inactivation at the 3-hydroxy group. When administered at doses of 150 and 450 µmol/kg, CN128 enhances iron mobilization by 24.8% in a 59Fe-ferritin-loaded rat model of iron overload.

UGT1A1-IN-1 (Compound 2) is a non-competitive inhibitor of UGT1A1 (UDP-glucuronosyltransferase 1A1). It inhibits the 1-O-glucuronidation process mediated by UGT1A1 with an IC50 of 1.33 μM and a Ki value of 5.02 μM. UGT1A1-IN-1 binds to UGT1A1 at the same ligand-binding site as Bilirubin. Additionally, it displays favorable reactivity in human liver microsomes (HLM) and serves as a practical, high-affinity fluorescent probe substrate for UGT1A1, facilitating the study of bilirubin metabolism disorders and enzyme activity.

Epmedin C (Standard) is a reference standard for research and analysis in studies involving Epmedin C. Epmedin C (Baohuoside-VI) was metabolized via desugarization, dehydrogenation, hydrogenation, dehydroxylation, hydroxylation, demethylation and glucuronidation pathways in vivo. It has potential activity against osteoporosis by stimulating osteoblasts.

p-Cresol (Standard) is the standard substance of p-Cresol, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. P-Cresol is a small molecular phenolic compound, which belongs to endogenous metabolites and has a certain lipophilicity, and can be highly combined with plasma protein in vivo. Its metabolism is mainly carried out through sulfation and glucuronidation, and the unbound part can be excreted in urine.

Molidustatglucuronide (BAY-348) is the N-glucuronide metabolite of Molidustat. Primarily formed through glucuronidation, it is the sole metabolite of Molidustat present in human and animal plasma. Molidustat glucuronide is utilized in the study of Molidustat's metabolic pathways and pharmacokinetic properties.

Solifenacin N-glucuronide is a metabolite of the muscarinic receptor antagonist Solifenacin, formed through direct glucuronidation. [Solifenacin N-glucuronide] levels are associated with diseases such as liver impairment.