| Name | TGR5 Receptor Agonist |
| Description | TGR5 is a potent TGR5(GPCR19) agonist. |
| Kinase Assay | 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]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 50 mg/mL (138.42 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 10 mg/mL (27.68 mM), Sonication is recommended.
Ethanol : 100 mM, Sonication is recommended.
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| Keywords | U2-OS cells | TGR5 Receptor Agonist | TGR-5 Receptor Agonist | TGR5 Receptor Agonist | TGR5 | melanophore cells | Inhibitor | inhibit | G-protein coupled receptor 19 | GPCR19 | GPBAR1 | G protein-coupled Bile Acid Receptor 1 | diabetes | CCDC | Calcium Channel | Ca2+ channels | Ca channels | C57BL/6J mice | bladder hypersensitivity | anti-obesity |
| Inhibitors Related | Quadrol | Tricaine methanesulfonate | Nisoldipine | 2,4,6-Tri-tert-butylphenol | Chlorocresol | L-Ascorbic acid | Ursodeoxycholic acid | Deoxycholic acid sodium salt | L-Ascorbic acid sodium salt | 2-Nitrobenzoic acid | Magnesium Chloride Hexahydrate | Magnesium sulfate |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Calcium Channel Compound Library | Anti-Obesity Compound Library | Multi-Target Compound Library | NO PAINS Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library |
United States
