1371591-51-3

1371591-51-3 structure

Name: Firuglipel
Chemical Name: firuglipel
CAS Number: 1371591-51-3
Molecular Formula: C₂₅H₂₆FN₃O₅
Molecular Weight: 467.489
Catalog: Signaling Pathways GPCR/G Protein GPR119
Create Date: 2019-01-20 08:33:03
Modify Date: 2024-01-12 17:50:34
Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.

Name	firuglipel
Synonyms	4-(5-{(1R)-1-[4-(Cyclopropylcarbonyl)phenoxy]propyl}-1,2,4-oxadiazol-3-yl)-2-fluoro-N-[(2R)-1-hydroxy-2-propanyl]benzamide

Description	Firuglipel (DS-8500a) is an orally available, potent and selective GPR119 agonist.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> GPR119 Research Areas >> Metabolic Disease
Target	GPR119[1]
In Vitro	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].
Animal Admin	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.
References	[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.