Firuglipel(DS-8500a)是高效，选择性，有口服活性的GPR119激动剂。
Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
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].
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].
[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. 2018 Dec;367(3):509-517.
Animal experiment: | Rats[1]Male SD rats (8 weeks) are fasted overnight and orally given vehicle (0.5% MC), DS-8500a (0.1, 1, 3 and 10 mg/kg), or glimepiride (10 mg/kg). Thirty minutes later, all animals received a 50% glucose solution intravenously (glucose load: 0.5 g/kg). Blood collection is performed from the tail vein 35 minutes before, 5 minutes before, and 5 minutes after the glucose load. The plasma insulin concentration is measured using ELISA kits. |
参考文献: [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. 2018 Dec;367(3):509-517. | |
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