| Bioactivity | TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.39. TUG-499 exhibits >100-fold selectivity over the related receptors FFA2, FFA3, and the nuclear receptor PPARγ and other diverse receptors, ion channels, and transporters. TUG-499 can be used for the research of type 2 diabetes[1]. |
| Target | pEC50: 7.39 (FFAR1) |
| Invitro | TUG-499 (compound 7) demonstrates high chemical stability, no inhibition of selected CYP enzymes or P-glycoprotein, and excellent Caco-2 permeability. TUG-499 has potent activity on recombinant human FFA1 receptors and on the rat insulinoma cell line INS-1E[1]. |
| Name | TUG-499 |
| CAS | 1206629-08-4 |
| Formula | C16H11Cl2NO2 |
| Molar Mass | 320.17 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Elisabeth Christiansen, et al. Identification of a potent and selective free fatty acid receptor 1 (FFA1/GPR40) agonist with favorable physicochemical and in vitro ADME properties. J Med Chem. 2011 Oct 13;54(19):6691-703. |
TUG-499
CAS: 1206629-08-4 F: C16H11Cl2NO2 W: 320.17
TUG-499 is a selective free fatty acid receptor 1 (FFAR1 or GPR40) (Free Fatty Acid Receptor) agonist with a pEC50 of 7.
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