Powder: -20°C for 3 years | In solvent: -80°C for 1 year
TGR5 is a potent TGR5(GPCR19) agonist.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 34.00 | |
5 mg | In stock | $ 79.00 | |
10 mg | In stock | $ 133.00 | |
25 mg | In stock | $ 263.00 | |
50 mg | In stock | $ 483.00 | |
100 mg | In stock | $ 693.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 88.00 |
Description | TGR5 is a potent TGR5(GPCR19) agonist. |
Targets&IC50 | TGR5/GPCR19 (U2-OS cells):6.8(pEC50), TGR5/GPCR19 (melanophore cells):7.5(pEC50) |
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]. |
Molecular Weight | 361.22 |
Formula | C18H14Cl2N2O2 |
CAS No. | 1197300-24-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mM
Ethanol: 100 mM
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
TGR5 Receptor Agonist 1197300-24-5 GPCR/G Protein GPCR19 Calcium Channel anti-obesity Inhibitor bladder hypersensitivity TGR5 G-protein coupled receptor 19 GPBAR1 U2-OS cells C57BL/6J mice G protein-coupled Bile Acid Receptor 1 melanophore cells Ca2+ channels inhibit TGR-5 Receptor Agonist diabetes TGR5 Receptor Agonist CCDC Ca channels inhibitor