8 Results for "

UGT1A1-IN-1

" in MedChemExpress (MCE) Product Catalog:
Products (8)

8 Results for "UGT1A1-IN-1" in MCE Product Catalog:

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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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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Cat. No.: HY-N4267
CAS No.: 13060-14-5
Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca 2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases .
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Cat. No.: HY-N1902R
CAS No.: 156-38-7
4-Hydroxyphenylacetic acid (Standard) is the analytical standard of 4-Hydroxyphenylacetic acid. This product is intended for research and analytical applications. 4-hydroxyphenylacetic acid, a major microbiota-derived metabolite of polyphenols, is involved in the antioxidative action. 4-hydroxyphenylacetic acid induces expression of Nrf2 . IC50 & Target:Nrf2 In Vivo: 4-Hydroxyphenylacetic acid (6, 12, or 25 mg/kg) increases Nrf2 translocation to the nucleus and enhances the activity of phase II and antioxidant enzymes. The protein levels of nuclear Nrf2 are increased by 170% and 230% in pre-treated 12 and 25 mg/kg 4-Hydroxyphenylacetic acid groups, respectively, compared with the control group.The 4-Hydroxyphenylacetic acid pretreatment at a final dose of 25 mg/kg markedly and selectively up-regulated the target genes of phase II enzymes and resulted in higher up-regulation than that of the control group by 270%, 400%, and 500% or UGT1A1, UGT1A9, and SULT2A1, respectively. 4-Hydroxyphenylacetic acid also suppresses the expression of CYP2E1 .
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Cat. No.: HY-124364
CAS No.: 1578153-27-1
Target:  

HBV Cytochrome P450

Research Areas:  

Infection Metabolic Disease

RO6889678 is a highly potent HBV capsid formation inhibitor with a complex absorption, distribution, metabolism, and excretion (ADME) profile. RO6889678 is a potent inducer of CYP3A4 and coregulated proteins in human hepatocytes. RO6889678 is metabolized by a combination of CYP3A4-mediated oxidation and UDP-glucuronosyltransferase UGT1A3- and UGT1A1-mediated direct glucuronidation .
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Cat. No.: HY-W718401
CAS No.: 1486471-13-9
Synonyms: BelINostat G
Target:  

Drug Metabolite

Research Areas:  

Others

Belinostat glucuronide (Belinostat G) is the major metabolite formed via UGT1A1-catalyzed O-glucuronidation of Belinostat (HY-10225), and exhibits no activity against cancer cells .
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Cat. No.: HY-W739842
CAS No.: 17834-04-7
Synonyms: 8-OH WarfarIN
Target:  

Cytochrome P450

Research Areas:  

Cardiovascular Disease

8-Hydroxywarfarin (8-OH Warfarin) is a CYP2C9 inhibitor. 8-Hydroxywarfarin inactivates the anticoagulant activity of Warfarin (HY-B0687) via 8-hydroxylation. 8-Hydroxywarfarin serves as a glucuronidation substrate for UGT1A1, UGT1A8, UGT1A9, as well as wild-type/mutant UGT1A10. This reaction enhances its polarity, solubility and excretion efficiency, and the process is independent of phenylalanine 90 of UGT1A10. 8-Hydroxywarfarin can be used in studies related to thromboembolic diseases .
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