CAS NO: | 1623194-37-5 |
Cas No. | 1623194-37-5 |
Canonical SMILES | FC1=CC(C2=CC(OC)=NC=C2)=CC=C1[C@@H]3CCC(C=CC([C@H](C4CC4)[C@H](C)C(O)=O)=C5)=C5O3 |
分子式 | C28H28FNO4 |
分子量 | 461.52 |
溶解度 | Soluble in DMSO |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | AP5 exhibits potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM). AP5 demonstrates a rat hIP1 EC50 of 0.49±0.28 nM against the GPR40 receptor[1]. EC50: 0.49±0.28 nM (GPR40 Receptor)[1] 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 AP5 1 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[1]. [1]. Chen HY, et al. Structure-Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs. ACS Med Chem Lett. 2018 Jun 14;9(7):685-690. |
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