化合物TGR5 T1824

Product Introduction
Bioactivity


英文名: TGR5 Receptor Agonist

描述: TGR5 Receptor Agonist 是一种TGR5(GPCR19)激动剂。

激酶实验: Inhibition assays are carried out in 384-well white ProxiPlates in 10 μL of reaction volume. Standard reaction mixtures consisted of the compound (in 2% DMSO final concentration), enzyme mix (0.001 μM of PHD2, 10 μM of Fe(II), 100 μM of ascorbate) and peptide mix (0.06 μM of biotinylated C-terminal oxygen dependent degradation domain (CODD) peptide, 2 μM of 2OG) in 50 mM HEPES pH 7.5, 0.01% Tween-20 and 0.1% BSA buffer. Compounds (e.g., IOX2) are preincubated with the enzyme mix for 15 min before being incubated with peptide mix for 10 min at 22°C. Each reaction is quenched with 5 μL of 30 mM EDTA. The bead mix containing AlphaScreen beads is preincubated for 1h with a rabbit monoclonal antibody selective for hydroxy-HIF1α (Pro564) and are added to the wells for a further 1 h at 22°C. The plates are then analyzed with an Envision plate reader. The IC50 values are calculated using nonlinear regression with normalized dose-response fit using Prism GraphPad (n≥3)[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (138.42 mM)
Ethanol : 100 mM


关键字: Calcium Channel | anti-obesity | Inhibitor | bladder hypersensitivity | GPCR19 | TGR5 | G-protein coupled receptor 19 | GPBAR1 | U2-OS cells | C57BL/6J mice | G protein-coupled Bile Acid Receptor 1 | TGR5 Receptor Agonist | melanophore cells | Ca2+ channels | inhibit | TGR-5 Receptor Agonist | diabetes | TGR5 Receptor Agonist | CCDC | Ca channels

相关产品: INT-777 | Hyodeoxycholic acid | BAR502 | Ursodeoxycholic acid sodium | BAR 501 impurity | L-692429 | SBI-115 | SB756050 | Deoxycholic acid sodium salt | TC-G 1005

相关库: Anti-Cancer Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | GPCR Compound Library | Anti-Obesity Compound Library | Target-Focused Phenotypic Screening Library | NO PAINS Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途