GPR4 antagonist 3(NE 52-QQ57 )|CAS 1401728-56-0|DC Chemicals

Cas No.:	1401728-56-0
Synonyms:	NE 52-QQ57
SMILES:	CCC1C(CC2C=CC(C3OC(C4CCNCC4)=NN=3)=CC=2)=C2N=C(C)C=C(C)N2N=1
Formula:	C₂₄H₂₈N₆O
M.Wt:	416.52
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:	GPR4 antagonist 3 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM[1]. Anti-inflammatory activities[1].
Target:	IC50: 70 nM (GPR4)[1].
In Vivo:	GPR4 antagonist 3 shows a significant anti-inflammatory effect in the rat antigen induced arthritis model after oral administration at 30 mg/kg bid[1].GPR4 antagonist 3 also prevents angiogenesis in the mouse chamber model as well as pain as demonstrated in the rat complete Freund’s adjuvant model[1].
References:	[1]. Velcicky J, et al. Development of Selective, Orally Active GPR4 Antagonists with Modulatory Effects on Nociception, Inflammation, and Angiogenesis. J Med Chem. 2017 May 11;60(9):3672-3683.

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