TGR5 Receptor Agonist
Référence M2588-5mg
Conditionnement : 5mg
Marque : AbMole Bioscience
All AbMole products are for research use only, cannot be used for human consumption.
Quality Control & Documentation
Biological Activity
TGR5 Receptor Agonist is a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).TGR5 Receptor Agonist has good physicochemical properties.But it has no measurable activity against three of the common cytochrome P450 (CYP450) isoforms (1A2, 2C9, and 2D6) or hERG dofetilide binding (pIC50 <4.3).GR5 receptor agonists are potentially useful therapeutics for metabolic disorders like type II diabetes and its associated complications.
Customer Product Validations & Biological Datas
Source | Sci Rep (2018). Figure 5. TGR5 | |
Method | TGR5KO cells | |
Cell Lines | NRVMs | |
Concentrations | 10–100 μM | |
Incubation Time | 10–15 mins | |
Results | NMVMs in culture show spontaneous contraction. Incubation with INT-777, in the range of 10–100 μM, does not change the contraction rate of NMVMs in both wild type and TGR5KO cells |
Chemical Information
Molecular Weight | 361.22 |
Formula | C18H14Cl2N2O2 |
CAS Number | 1197300-24-5 |
Solubility (25°C) | DMSO ≥ 30 mg/mL |
Storage | Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
References
[1] Evans KA,et al. J Med Chem. Discovery of 3-aryl-4-isoxazolecarboxamides as TGR5 receptor agonists.