AP5 |
| カタログ番号GC35364 |
AP5 は、内因性リガンド (AgoPAM) の正のアロステリック変調を伴う、強力で、活性が高く、選択的な GPR40 受容体アゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1623194-37-5
Sample solution is provided at 25 µL, 10mM.
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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.
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)
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