| Bioactivity | Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist. | ||||||||||||
| Target | GPR119 | ||||||||||||
| Invitro | Firuglipel (DS-8500a) increases intracellular cAMP in a concentration-dependent manner in human, rat, and mouse GPR119-expressing Chinese hamster ovary (CHO)-K1 cells, with EC50 values of 51.5, 98.4, and 108.1 nM, respectively. DS-8500a has no effect on intracellular cAMP in pcDNA3.1/CHO-K1 cells[1]. | ||||||||||||
| In Vivo | Firuglipel (DS-8500a) (1-30 mg/kg) upregulates glucagon-like peptide-1 and enhances glucose-dependent insulin secretion and improves glucose homeostasis in type 2 diabetic rats[1]. | ||||||||||||
| Name | Firuglipel | ||||||||||||
| CAS | 1371591-51-3 | ||||||||||||
| Formula | C25H26FN3O5 | ||||||||||||
| Molar Mass | 467.49 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Matsumoto K, et al. DS-8500a, an Orally Available G Protein-Coupled Receptor 119 Agonist, Upregulates Glucagon-Like Peptide-1 and Enhances Glucose-Dependent Insulin Secretion and Improves Glucose Homeostasis in Type 2 Diabetic Rats. J Pharmacol Exp Ther. |