1142214-62-7

1142214-62-7 structure

Name: AM-1638
Chemical Name: (3S)-3-Cyclopropyl-3-(3-{[2-(5,5-dimethyl-1-cyclopenten-1-yl)-2'-fluoro-5'-methoxy-4-biphenylyl]methoxy}phenyl)propanoic acid
CAS Number: 1142214-62-7
Molecular Formula: C₃₃H₃₅FO₄
Molecular Weight: 514.62700
Catalog: Signaling Pathways GPCR/G Protein GPR40
Create Date: 2018-12-05 07:23:11
Modify Date: 2024-01-06 21:21:05
AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.

Name	(3S)-3-Cyclopropyl-3-(3-{[2-(5,5-dimethyl-1-cyclopenten-1-yl)-2'-fluoro-5'-methoxy-4-biphenylyl]methoxy}phenyl)propanoic acid
Synonyms	AM 1638 [3H]-AM 1638 (S)-3-cyclopropyl-3-(3-((2-(5,5-dimethylcyclopent-1-en-1-yl)-2'-fluoro-5'-methoxy-[1,1'-biphenyl]-4-yl)methoxy)phenyl)propanoic acid

Description	AM-1638 is a potent and orally bioavailable GPR40/FFA1 full agonist with an EC50 of 0.16 μM.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> GPR40 Research Areas >> Metabolic Disease
Target	IC50: 0.16 μM (GPR40/FFA1)[1]
In Vivo	AM-1638 exhibits moderate cross-species plasma clearance and volume of distribution, resulting in plasma half-lives suitable for evaluation of its antidiabetic properties in mouse, rat, and cynomologus monkey. Moreover, oral administration of full agonist AM-1638 demonstrates excellent oral bioavailability (mouse, >100%; rat, 72%; and cyno, 71%). AM-1638exhibits antidiabetic activity in BDF/DIO mice[1].
Animal Admin	Mice[1] On the morning of the experiment, Male B6D2F1/J mice are fasted for four hours and body weight and blood glucose levels are measured. Animals are randomized into treatment groups based on these two parameters. Treatments are administered by oral gavage and sixty minutes later, the mice received a 2 g/kg glucose challenge dose by oral gavage (defined as t=0 min). Blood samples are collected at -60, 0, 15, 30, 60, 90 and 120 minutes via tail vein relative to the glucose challenge. Glucose levels are monitored with a glucometer. Plasma insulin is measured using a mouse insulin ELISA[1].
References	[1]. Brown SP, et al. Discovery of AM-1638: A Potent and Orally Bioavailable GPR40/FFA1 Full Agonist. ACS Med Chem Lett. 2012 Aug 15;3(9):726-30.