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1623194-37-5

1623194-37-5 structure
1623194-37-5 structure
  • Name: GPR40 AgoPAM AP5
  • Chemical Name: AP5
  • CAS Number: 1623194-37-5
  • Molecular Formula: C28H28FNO4
  • Molecular Weight: 461.52
  • Catalog: Signaling Pathways GPCR/G Protein GPR40
  • Create Date: 2019-03-03 22:22:20
  • Modify Date: 2024-01-16 16:35:19
  • 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].

Name AP5
Description 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].
Related Catalog
Target

EC50: 0.49±0.28 nM (GPR40 Receptor)[1]

In Vitro 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].
References

[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.

Molecular Formula C28H28FNO4
Molecular Weight 461.52