33 Results for "

UGT1A1

" in MedChemExpress (MCE) Product Catalog:
Products (33)

33 Results for "UGT1A1" in MCE Product Catalog:

  • Targets Recommended:
19
19 Publications Verification
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) .
loading...
    loading...
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 .
loading...
    loading...
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 .
loading...
    loading...
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 .
loading...
    loading...
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 .
loading...
    loading...
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 .
loading...
    loading...
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 .
loading...
    loading...
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 .
loading...
    loading...
Cat. No.: HY-111539
CAS No.: 1613264-40-6
Purity:  99.73%
BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC50 of 15.3 nM for human EP4-R. BAY-1316957 has excellent agent metabolism and pharmacokinetics properties, and can be used for endometriosis research .
loading...
    loading...
Cat. No.: HY-RS15426
Research Areas:  

Others

UGT1A1 Human Pre-designed siRNA Set A contains three designed siRNAs for UGT1A1 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

loading...
    loading...
Cat. No.: HY-RS16797
Research Areas:  

Others

Ugt1a1 Mouse Pre-designed siRNA Set A contains three designed siRNAs for Ugt1a1 gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.

loading...
    loading...
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 .
loading...
    loading...
Cat. No.: HY-100319
CAS No.: 162704-20-3
Target:  

UGT

Research Areas:  

Metabolic Disease

UK-157147 is a substrate for UDP-glucuronosyltransferases (UGT1A1) with a Km value of 105 μM.
loading...
    loading...
Cat. No.: HY-E72105
Target:  

UGT

Research Areas:  

Others

Human UGT1A1 is a uridine diphosphate glucuronosyltransferase (UGT). Human UGT1A1 mediates the metabolism of active compounds by conjugating glucuronic acid to toxic or lipophilic compounds, converting them into water-soluble waste products that can be safely eliminated from the human body via bile or urine .
loading...
    loading...
Cat. No.: HY-130046
CAS No.: 547-81-9
Purity:  99.04%
Synonyms: 16-epi-Estriol; 16β,17β-Estriol
Target:  

UGT Bacterial

Research Areas:  

Infection Inflammation/Immunology

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 .
loading...
    loading...
Cat. No.: HY-RS23238
Research Areas:  

Others

Ugt1a1 Rat Pre-designed siRNA Set A contains three designed siRNAs for Ugt1a1 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.

loading...
    loading...
Cat. No.: HY-N0372R
CAS No.: 58749-22-7
Licochalcone A (Standard) is the analytical standard of Licochalcone A (HY-N0372). This product is intended for research and analytical applications. 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) .
loading...
    loading...
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 .
loading...
    loading...
Cat. No.: HY-135581
CAS No.: 174264-50-7
Target:  

Estrogen Receptor/ERR

Research Areas:  

Endocrinology

Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression .
loading...
    loading...
Cat. No.: HY-15592R
CAS No.: 1051375-10-0
Synonyms: GSK-1265744 (Standard); S/GSK1265744 (Standard)
Research Areas:  

Infection

Cabotegravir (Standard) is the analytical standard of Cabotegravir. This product is intended for research and analytical applications. 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 .
loading...
    loading...