UGT

UDP-glucuronosyltransferase; Uridine diphosphate glucuronosyltransferase

UGT is a type of catabolic enzyme that belongs to the family of detoxification enzymes. UGT consists of two subfamilies, UGT1 and UGT2. UGT1 consists of 5 exons and has a unique gene structure. There are thirteen exon 1s from UGT1A1 to UGT1A13P, and exon 2 to exon 5 are used in common for all mRNAs expressed from the gene. Each isoform of UGT1 results from differential splicing of exon1s to common exon 2-5, and has an unique spectrum of substrate specificity. In contrast, the genes of the UGT2 family consist of 6 exons, and all the enzymes have an individual set of exon 1 to exon 6. UGT involves in the detoxification and excretion of many xenobiotic and endogeneous substances in intrahepatic and extrahepatic tissues. The mutations of UGT1A1 cause hereditary unconjugated hyperbilirubinemias: Crigler-Najjar syndrome type I, type II and Gilbert syndrome.

References:

[1]. Maruo Y, et al. Polymorphism of UDP-glucuronosyltransferase and drug metabolism. Curr Drug Metab. 2005 Apr;6(2):91-9. [Content Brief]

[2]. Tephly TR, et al. UDP-glucuronosyltransferases: a family of detoxifying enzymes. Trends Pharmacol Sci. 1990 Jul;11(7):276-9. [Content Brief]

UGT Related Products (30):

By Effects:	Inhibitors (18) Substrates (3) Activators (4)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-W011910

Potassium 1H-indol-3-yl sulfate	Activator	99.95%
Potassium 1H-indol-3-yl sulfate is a metabolite of tryptophan, produced by intestinal microorganisms and combined with sulfate in the liver before entering the circulatory system. Potassium 1H-indol-3-yl sulfate is a potent endogenous agonist of the aryl hydrocarbon receptor (AhR) and a urinary toxin. Potassium 1H-indol-3-yl sulfate can be used for research on kidney diseases.

HY-N0235

Bakuchiol	Inhibitor	99.25%
Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC₅₀s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory, antibacterial, antitumor therapies, as well as drug metabolism regulation.

HY-111832

1,2,3,6-Tetragalloylglucose	Inhibitor	99.08%
1,2,3,6-Tetragalloylglucose (TEgG) is a competitive inhibitor of UDP-glucuronyltransferase UGT1A1, targeting the competitive substrate binding site of UGT1A1. 1,2,3,6-Tetragalloylglucose inhibits UGT1A1-mediated β-estradiol 3-glucuronidation and SN-38 glucuronidation with IC₅₀ of 6.01 μM and 4.31 μM, respectively, and binds to UGT1A1 with K_i of 3.55 μM. 1,2,3,6-Tetragalloylglucose also induces tumor cell apoptosis, inhibit cell proliferation, activates caspase-3 and induces DNA fragmentation in HL-60 cells. 1,2,3,6-Tetragalloylglucose also inhibits HIV integrase and reverse transcriptase, and inhibits HCV protease.

HY-131703

UGT8-IN-1	Inhibitor	99.94%
UGT8-IN-1 is a brain penetrable and orally active inhibitor of ceramide galactosyltransferase enzyme (UGT8). UGT8-IN-1 can be used in the study for lysosomal storage disorders.

HY-N0762

Isobavachin	Inhibitor	99.88%
Isobavachin is an orally active, blood-brain barrier-penetrating prenylated flavonoid present in Psoralea corylifolia. Isobavachin inhibits human CYP2B6, CYP2C9, CYP2C19, UGT1A1, UGT1A9, and UGT2B7. Isobavachin suppresses MAPK activation, NF-κB nuclear translocation, overexpression of iNOS/COX-2, FcεRI-mediated signaling pathways, and RANKL-induced osteoclastogenesis. Isobavachin induces autophagy, cytotoxicity, neuronal differentiation, and NRF2 activation; it alleviates oxidative damage, inflammatory responses, apoptosis, iron accumulation, mitochondrial biogenesis, and mast cell degranulation. Isobavachin is applicable to research related to liver injury, inflammatory diseases, osteoporosis, liver cancer, prostate cancer, glioma, periodontitis-induced bone loss, and Alzheimer's disease.

HY-107081

Berupipam hemifumarate
Berupipam hemifumarate is a selective antagonist of the dopamine D1 receptor (dopamine D1 receptor). Berupipam hemifumarate is a substrate of UDP-glucuronosyltransferase (UGT) and has a high affinity for UGT enzymes but a relatively low conversion rate. The glucuronidation rate of Berupipam hemifumarate varies among different species and genders. Berupipam hemifumarate can be used for the study of psychotic disorders.

HY-122163

MK-3901	Inhibitor
MK-3901 is a selective P2X3 receptor antagonist with an IC₅₀ of 24 nM. MK-3901 inhibits UGT1A1 (with an IC₅₀ of 1 μM) and CYP2C9 (with an IC₅₀ of 5.7 μM). MK-3901 activates PXR. MK-3901 induces hyperbilirubinemia. MK-3901 can be used for the research of inflammatory pain.

HY-B0811

Salicylamide	Inhibitor	99.92%
Salicylamide is an inhibitor of microsomal UDP-glucuronosyltransferase. Salicylamide is an analgesic and anti-pyretic agent.

HY-107850

Pregnanediol	Inhibitor	99.97%
Pregnanediol (NSC 1612) is a Progesterone (HY-N0437) metabolite. Pregnanediol does not affect the transcriptional activity of UGT1A1 enhancer-promoter complex of WT and variant type. pregnanediol inhibits glucuronidation activity of G71R-UGT1A1. Pregnanediol is a cause of breast milk jaundice in carriers of G71R.

HY-N0897

Corylifol A		99.90%
Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC₅₀ of 0.81 μM.

HY-137083

Trifluoperazine N-Glucuronide	Inhibitor
Trifluoperazine N-Glucuronide (UGT1A4), as one of the human UGT1A isoforms, is expressed in the liver. Trifluoperazine N-Glucuronide catalyzes the imipramine and trifluoperazine Nglucuronide formation.

HY-160250

UGT1A1-IN-1	Inhibitor	99.27%
UGT1A1-IN-1 is a UGT1A1 inhibitor and fluorescent probe (Ex=370 nm, Em=520 nm), with an IC₅₀ of 1.33 μM and a K_i of 5.02 μM. UGT1A1-IN-1 is selectively glucuronidated by UGT1A1 at the bilirubin homologous binding site, and its PET effect is blocked along with this reaction, triggering fluorescence changes. UGT1A1-IN-1 can serve as a substitute for bilirubin to detect UGT1A1 activity and perform high-throughput screening of UGT1A1 modulators.

HY-N0859

Schisanhenol	Inhibitor	99.99%
Schisanhenol (Schizanhenol), a lignan, is an orally active antioxidant. Schisanhenol reduces AChE activity, increases SIRT1 and PGC-1α expression, and decreases phosphorylated Tau (Ser 396) levels. Schisanhenol increases SOD and glutathione peroxidase activity, decreases malondialdehyde (MDA) content, and inhibits UGT2B7 activitY. Schisanhenol attenuates ox-LDL-induced apoptosis, intracellular reactive oxygen species generation, and cytotoxicity in endothelial cells. Schisanhenol inhibits LDL oxidation, brain mitochondrial and membrane peroxidative damage, and brain mitochondrial swelling and disintegration. Schisanhenol can be used for the research of Alzheimer’s disease, atherosclerosis, brain ischemia, and age-related brain deterioration.

HY-N2413

Gomisin D	Inhibitor	99.56%
Gomisin D is an orally active lignan that binds to PDGFRβ with a K_d of 10 μM. By targeting PDGFRβ to regulate signaling pathways, Gomisin D inhibits the activation and proliferation of hepatic stellate cells and promotes their apoptosis, thereby ameliorating hepatic fibrosis. Gomisin D exhibits multiple activities such as photoprotection, antimelanogenesis, antioxidant effects, and hypoglycemic activity. Gomisin D can be used in studies related to diabetes, Alzheimer's disease, and hepatic fibrosis.

HY-125904

4-Hydroxyretinoic acid	Substrate
4-Hydroxyretinoic acid (4-HRA) is a derivative of Retinoic acid (HY-14649). 4-Hydroxyretinoic acid is formed via the catalysis of retinol by cytochrome P-450 isoenzymes. 4-Hydroxyretinoic acid also serves as a substrate for UDP-glucuronosyltransferase (s) and recombinant UGT2B7. 4-Hydroxyretinoic acid binds to the nuclear receptor RAR (Retinoic Acid Receptor), activates RAR and RXR-alpha, subsequently regulates gene expression and cell differentiation, and induces cancer cell apoptosis (Apoptosis). 4-Hydroxyretinoic acid also participates in multiple physiological processes such as immunoregulation, neuroprotection and antioxidation.

HY-W011910S

Potassium 1H-indol-3-yl sulfate-d₄	Activator	99.9%
Potassium 1H-indol-3-yl sulfate-d₄ potassium is the deuterium labeled Potassium 1H-indol-3-yl sulfate. Potassium 1H-indol-3-yl sulfate is a metabolite of tryptophan, produced by intestinal microorganisms and combined with sulfate in the liver before entering the circulatory system. Potassium 1H-indol-3-yl sulfate is a potent endogenous agonist of the aryl hydrocarbon receptor (AhR) and a urinary toxin. Potassium 1H-indol-3-yl sulfate can be used for research on kidney diseases.

HY-145668

Cyclopentenyl uracil	Inhibitor	99.84%
Cyclopentenyl uracil, a non-cytotoxic inhibitor of uridine kinase, effectively blocks the salvage of circulating uridine by host and tumor tissues in the intact mouse.

HY-130046

16-Epiestriol	Inhibitor	99.04%
16-Epiestriol (16-epi-Estriol; 16β,17β-Estriol) is a natural stereoisomer of estriol and an anti-inflammatory agent that targets UGT. The Ki values of 16-Epiestriol against human UGT1A10 and UGT2B7 are 98.1 μM and 162 μM, respectively. As a glucuronidation substrate, 16-Epiestriol can be modified at the 3-OH, 16-OH and 17-OH sites by various UGT enzymes; in liver microsomes, the modification mainly occurs at the 16-OH and 17-OH sites, while reactions take place at all three sites in intestinal microsomes. 16-Epiestriol acts on the phase II inflammatory process by blocking edema mediated by prostaglandins and leukocyte infiltration. It lacks glycogenic activity or any effect on blood glucose levels, and serves as an important candidate molecule in the research of inflammatory diseases.

HY-N12360A

2,3-Dehydrosilybin B		98.11%
2,3-Dehydrosilybin B is an enantiomer formed by the oxidation of the natural flavonolignans silybin A.

HY-W006081

3-Methyl-2-nitrophenol	Substrate	99.55%
3-Methyl-2-nitrophenol is a UDP-glucuronyltransferase (EC 2.4.1.17) acceptor substrate that can be confirmed to undergo glucuronidation catalyzed by the enzyme to form a glucuronide conjugate. 3-Methyl-2-nitrophenol functions as a substrate for conjugation, with glucuronidation forming a glucuronide conjugate that eliminates the parent compound’s characteristic yellow color. 3-Methyl-2-nitrophenol has higher lipid solubility that contributes to high glucuronidation conversion rate, and exhibits lower absorbance at 340 nm to act as a less interfering substrate for the NADH-NAD⁺-linked UDP-glucuronyltransferase assay.

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