92 Results for "

UGT

" in MedChemExpress (MCE) Product Catalog:
Products (92)

92 Results for "UGT" in MCE Product Catalog:

  • Targets Recommended:
30
30 Publications Verification
Cat. No.: HY-N0168
CAS No.: 520-33-2
Hesperetin is a natural flavanone that can be found in citrus, and acts as a potent and orally active broad-spectrum inhibitor against human UGT activity. Hesperetin induces apoptosis via p38 MAPK activation. Hesperetin displays a range of bioactivities including antioxidant, anti-inflammatory, and anti-cancer. Hesperetin is found to induce cell-cycle arrest at G2/M phase. Hesperetin can reduce Bcl-2 and enhance BaxM. Hesperetin induces apoptosis through inhibiting NF-κB receptor .
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19
19 Cited Publications
Cat. No.: HY-N0372
CAS No.: 58749-22-7
Licochalcone A (LCA), a chalconoid, presents obvious anti-cancer effects, displays broad-spectrum inhibition against UDP-glucuronosyltransferases (UGTs) . Licochalcone A (LCA) exhibits strong inhibitory effects against UGT1A1, 1A3, 1A4, 1A6, 1A7, 1A9, and 2B7 (both IC50 and Ki values lower than 5 μM) .
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14
14 Cited Publications
Cat. No.: HY-15592
CAS No.: 1051375-10-0
Purity:  99.91%
Synonyms: GSK-1265744; S/GSK1265744
Target:  

OAT HIV HIV Integrase

Research Areas:  

Infection

Cabotegravir (GSK-1265744) is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively. Cabotegravir is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir can be used to research AIDS .
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14
14 Cited Publications
Cat. No.: HY-15592A
CAS No.: 1051375-13-3
Purity:  99.87%
Synonyms: GSK-1265744 sodium; S/GSK1265744 sodium
Target:  

OAT HIV HIV Integrase

Research Areas:  

Infection

Cabotegravir (GSK-1265744) sodium is a orally active and long-acting HIV integrase strand transfer inhibitor and organic anion transporter 1/3 (OAT1/OAT3) inhibitor with IC50 values of 2.5 nM, 0.41 μM and 0.81 μM for HIVADA, OAT3 and OAT1, respectively. Cabotegravir sodium is primarily metabolized by uridine diphosphate glucuronosyltransferase (UGT) 1A1, with low potential to interact with other antiretroviral agents (ARVs). Cabotegravir sodium can be used to research AIDS .
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6
6 Cited Publications
Cat. No.: HY-N0762
CAS No.: 31524-62-6
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 .
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2
2 Cited Publications
Cat. No.: HY-111832
CAS No.: 79886-50-3
Purity:  99.08%
Synonyms: TeGG
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 Ki 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 .
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2
2 Cited Publications
Cat. No.: HY-N0548
CAS No.: 591-12-8
α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes .
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2
2 Cited Publications
Cat. No.: HY-N2574
CAS No.: 511-96-6
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms .
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2
2 Cited Publications
Cat. No.: HY-N0235
CAS No.: 10309-37-2
Synonyms: (S)-(+)-Bakuchiol
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.
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2
2 Cited Publications
Cat. No.: HY-119323
CAS No.: 95633-27-5
Purity:  99.11%
Target:  

Fluorescent Dye

Research Areas:  

Others

7-Azido-4-methylcoumarin is a selective coumarin-based fluorescent probe for hydrogen sulfide (H2S). In the presence of H2S, the aromatic azido group of 7-Azido-4-methylcoumarin is selectively reduced to produce the fluorescently active 7-amino-4-methylcoumarin (AMC). 7-Azido-4-methylcoumarin binds to the coumarin/phenol-binding site of BSA, the aglycone-binding site of UGT1A6, and the substrate-binding site of SULT1A1, respectively. 7-Azido-4-methylcoumarin retains its fluorescent properties after covalent binding, acts as a fluorescent H2S probe, and does not react with cysteine, homocysteine or glutathione (Ex/Em = 340/445 nm) .
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1
1 Cited Publications
Cat. No.: HY-131703
CAS No.: 2414349-93-0
Purity:  99.94%
Target:  

UGT

Research Areas:  

Metabolic Disease

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 .
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1
1 Cited Publications
Cat. No.: HY-125904
CAS No.: 66592-72-1
Purity:  95.11%
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 .
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1
1 Cited Publications
Cat. No.: HY-N4194
CAS No.: 60008-02-8
Glabrone is an isoflavone found in Glycyrrhiza glabra roots. Glabrone exhibits significant PPAR-γ ligand binding activity. Glabrone is a specific UGT1A9 probe substrate, and its metabolites can block influenza virus release by inhibiting neuraminidase (NA). Glabrone can be used to screen for herb-drug interactions and for anti-influenza virus activity .
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Cat. No.: HY-Y1683
CAS No.: 89-78-1
Synonyms: Racementhol
DL-Menthol (Racementhol) is an orally active, GABAaR positive allosteric modulator and UDP-glucuronosyltransferase (UGT) inhibitor that can cross the blood-brain barrier. DL-Menthol binds to GABAAR and exhibits an allosteric activation effect, enhancing GABA-mediated chloride influx and inhibiting neuronal excitability. DL-Menthol can induce surgical anesthesia in fish and inhibit the metabolic detoxification of tobacco carcinogens by human liver and intestinal UGT enzymes, resulting in reduced NNAL-N-Gluc production .
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Cat. No.: HY-107850
CAS No.: 80-92-2
Purity:  99.71%
Synonyms: NSC 1612; NSC 47462
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 .
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Cat. No.: HY-137083
CAS No.: 165602-90-4
Purity:  95.80%
Synonyms: UGT1A4
Target:  

UGT

Research Areas:  

Metabolic Disease

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 .
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Cat. No.: HY-137522
CAS No.: 133525-01-6
Purity:  99.05%
Synonyms: 3'-Azido-3'-deoxythymidine β-D-glucuronide sodium
Target:  

Drug Metabolite

Research Areas:  

Others

Zidovudine O-β-D-glucuronide (3'-Azido-3'-deoxythymidine β-D-glucuronide) sodium is the glucuronide conjugate and metabolite of Zidovudine (HY-17413), which can be used to detect UGT2B7 activity. As a substrate, Zidovudine O-β-D-glucuronide sodium undergoes deconjugation via hydrolysis by immobilized β-glucuronidase to produce Zidovudine .
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Cat. No.: HY-N0859
CAS No.: 69363-14-0
Synonyms: Schizanhenol; Gomisin-K3
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 .
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Cat. No.: HY-160250
CAS No.: 2097024-37-6
Target:  

Fluorescent Dye UGT

Research Areas:  

Metabolic Disease

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 Ki 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 .
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Cat. No.: HY-135582
CAS No.: 182507-22-8
Target:  

Estrogen Receptor/ERR

Research Areas:  

Endocrinology

Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. . Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
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