AR 231453 is a potent, specific and orally available GPR119 agonist. AR 231453 can stimulate β-cell replication and improve islet graft function s.
体外研究
AR 231453 is inactive at all other GPCRs tested (more than 230, including all known pancreatic islet receptors), indicating that it is highly selective for GPR119.
AR 231453 potently stimulats cAMP accumulation (EC50 = 4.7 nM) with a maximal efficacy similar to that seen with forskolin. AR 231453 significantly enhancesinsulin release in HIT-T15 cells, with an EC50 of 3.5 nM.
AR 231453 also stimulates insulin release in isolated mouse islets at glucose concentrations ranging from 8-17 mM.
体内研究
AR231453 (20 mg/kg, orally) markedly improves oral glucose tolerance in a dose-dependent fashion, with efficacy similar to maximally effective doses of the sulfonylurea glyburide.
Animal Model:
Mice.
Dosage:
20 mg/kg.
Administration:
Orally, once.
Result:
Improved glucose tolerance in mice.
分子式
C21H24N7O5FS
分子量
505.52
CAS号
733750-99-7
运输条件
Room temperature in continental US; may vary elsewhere.