产品
编 号:F194833
分子式:C28H28FNO4
分子量:461.52
产品类型
结构图
CAS No: 1623194-37-5
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产品详情
生物活性:
AP5 is a potent, orlly active, and selective GPR40 receptor agonist with a positive allosteric modulation of endogenous ligand (AgoPAM). AP5 demonstrates rat and human inositol monophosphate (IP1) EC50 values of 0.49 nM and 0.8 nM against the GPR40 receptor, respectively. AP5 has the potential for type II diabetes research.
体外研究:
AP5 is a potent and selective GPR40 AgoPAM that demonstrates excellent in vivo efficacy. In the GK rat oral glucose tolerance test (oGTT), oral administration of AP51 h before an oral dextrose challenge shows that AP5 significantly reduces blood glucose levels compared to the vehicle. AP5 is determined to be more efficacious in this model, demonstrating maximally efficacious glucose lowering at a plasma concentration of 4.9 μM at 10 mg/kg.