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.
Product information
CAS Number: 1623194-37-5
Molecular Weight: 461.52
Formula: C28H28FNO4
Chemical Name: (2R,3S)-3-cyclopropyl-3-[(2R)-2-[2-fluoro-4-(2-methoxypyridin-4-yl)phenyl]-3,4-dihydro-2H-1-benzopyran-7-yl]-2-methylpropanoic acid
Smiles: C[C@H]([C@H](C1CC1)C1=CC=C2CC[C@@H](OC2=C1)C1=CC=C(C=C1F)C1=CC(=NC=C1)OC)C(O)=O
InChiKey: ABSKJGYIWZMOAF-FLFAQTGJSA-N
InChi: InChI=1S/C28H28FNO4/c1-16(28(31)32)27(18-4-5-18)21-6-3-17-8-10-24(34-25(17)14-21)22-9-7-19(13-23(22)29)20-11-12-30-26(15-20)33-2/h3,6-7,9,11-16,18,24,27H,4-5,8,10H2,1-2H3,(H,31,32)/t16-,24-,27-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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