Hazard Information | Back Directory | [Description]
AM-5262 is a Potent GPR40 Full Agonist with improved rat PK profile and general selectivity profile. AM-5262 enhanced glucose stimulated insulin secretion (mouse and human islets) and improved glucose homeostasis in vivo (OGTT in HF/STZ mice) when compared to AM-1638. GPR40 (FFAR1 or FFA1) is a target of high interest being pursued to treat type II diabetes due to its unique mechanism leading to little risk of hypoglycemia. | [Uses]
AM-5262 is a GPR40 full agonist with an EC50 value of 0.081 μM. AM-5262 can be used for the research of type II diabetes[1]. | [in vivo]
AM-5262 (26) (i.v., 0.5 mg/kg; oral, 2 mg/kg) improves rat PK profile and general selectivity profile[1].
AM-5262 (0-100 μM) enhances glucose stimulated insulin secretion (mouse and human islets) and improves glucose homeostasis in vivo (OGTT in HF/STZ mice) [1]. | [References]
[1] Wang Y, et al. Discovery and Optimization of Potent GPR40 Full Agonists Containing Tricyclic Spirocycles. ACS Med Chem Lett. 2013;4(6):551-555. Published 2013 May 7. DOI:10.1021/ml300427u |
|
Company Name: |
SPIRO PHARMA
|
Tel: |
|
Website: |
www.spiropharma.com.cn |
|