NE 52-QQ57

1401728-56-0

C12269-5mg

GPR

GPCR & G Protein

CCC1=NN2C (=CC (=NC2=C1CC3=CC=C (C=C3) C4=NN=C (O4) C5CCNCC5) C) C

C24H28N6O

NE 52-QQ57 is a selective, and orally available antagonist of G-protein coupled receptor 4 (GPR4) with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL) -1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2) .

3 years -20°C powder