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Niflumic acid (Nifluril) is a Ca2+-activated Cl- channel blocker and an analgesic and anti-inflammatory agent used in the therapy of rheumatoid arthritis.

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.

UGT1A1-IN-1 (compound 2) acts as a non-competitive inhibitor of UGT1A1, effectively inhibiting the 1-O-glucuronidation process mediated by UGT1A1 with a Ki value of 5.02 μM. This compound binds to the same ligand-binding site on UGT1A1 as bilirubin and additionally functions as a 'turn-on' fluorescent probe substrate for UGT1A1 [1].

Deferiprone (Deferidone) is an Iron Chelator. The mechanism of action of deferiprone is as an Iron Chelating Activity.

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

Mycophenolic acid (Mycophenolate) is an inosine monophosphate dehydrogenase(IMPDH) inhibitor with anti-proliferative activity.

Demethylzeylasteral (T-96), isolated from Tripterygium wilfordii, has anti-inflammatory, immunosuppressive and anti-tumor activities. It inhibits the invasion of triple-negative breast cancer by blocking the TGF-β signaling pathway, and it can significantly reduce atherosclerosis.

Licochalcone A is a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch with obvious anti-cancer effects.

1. Corylifol A (Corylinin) displays cytotoxic activity against HepG2 and Hep3B hepatocellular carcinoma cell lines, with IC50 values of 4.6 and 13.5 ug ml, respectively. 2. Corylifol A and Biochanin A can be the potential uncouplers of neuronal nitric oxide synthase-postsynaptic density protein-95. 3. Corylifol A and bavachin are strong inhibitors of UDP-glucuronosyltransferase 1A1 (UGT1A1) with the inhibition kinetic parameters (Ki) values lower than 1 uM.4. Corylifol A and bakuchiol are naturally occurring potent inhibitors of hCE2, with low Ki values ranging from 0.62uM to 3.89 uM. 5. Corylifol A shows an inhibitory effect on IL-6-induced STAT3 promoter activity in Hep3B cells with IC50 values of 0.81 ± 0.15 uμ, it also inhibits STAT3 phosphorylation induced by IL-6 in Hep3B cells, suggests that corylifol A has antiinflammatory activity.

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

UK-157147 is a substrate for UGT1A1 (Km: 105 μM).

1. Gitogenin, tigogenin, and solasodine are novel selective inhibitors of UGT1A4, and do not inhibit the activities of major human CYP isoforms. 2. Gitogenin and (25S)-5α-furastan-3β, 22, 26-triol are the inhibitors of enzyme α-glucosidase with IC50 value

Ophiopogonin D' can activate SIRT1 in a dose-dependent manner. Ophiopogonin D' also noncompetitively inhibits UGT1A6 and UGT1A10.

1,2,3,6-Tetragalloylglucose (TeGG) has antioxidative activity, it also shows the most potent anticomplement activity (IC50 = 34 microM). 1,2,3,6-Tetragalloylglucose is also a potent inhibitor of UDP glucuronosyltransferase 1 A1 (UGT1A1, Ki = 1.68 μM).

Hesperetin belongs to the flavanone class of flavonoids. Hesperetin, in the form of its glycoside hesperidin, is the predominant flavonoid in lemons and oranges.

(Rac)-Hesperetin, the racemate form of Hesperetin, is a natural flavanone compound exhibiting potent inhibitory effects against human UGT activity, making it a broad-spectrum inhibitor. Additionally, Hesperetin induces apoptosis through the activation of p38 MAPK.

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]

(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.

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.

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.

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.

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)

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).

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)