NE 52-QQ57

Research use only, not for human use.

NE 52-QQ57 is a selective, and orally available antagonist of GPR4(IC50 : 70 nM),with anti-inflammatory activity.

NE 52-QQ57 is a selective, and orally available antagonist of GPR4(IC50 : 70 nM),with anti-inflammatory activity.

NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation (IC50 26.8?nM in HEK293?cells).

NE 52-QQ57 (Compound 13) shows a significant anti-inflammatory effect in the rat antigen induced arthritis model after oral administration at 30 mg/kg bid for 20 days.NE 52-QQ57 (30 mg/kg bid po for 4 days) also prevents angiogenesis in the mouse chamber model as well as pain as demonstrated in the rat complete Freund’s adjuvant model. Animal Model:Female FVB mice (8-10 weeks)Dosage:30 mg/kg Administration:Oral, 4 days, bid Result:Treatment at 30 mg/kg p.o. bid starting on day 0, the day of the chamber implantation, showed a statistically significant reduction (46.8±10.6%) of tissue growth by day 4. The blood levels of 13 on day 4 at 2 and 16 h after compound application in this model were 9.03±2.87 and 0.09±0.06 μM.Animal Model:Male Wistar Han rats Dosage:3, 10, and 30 mg/kg Administration:Oral, 20 days, bid Result:Displayed not only higher exposures in the rat AIA but also lower plasma protein binding in rat (95%).

——

Others

Other Targets

GPR4

——

——

1401728-56-0

416.52

C24H28N6O

>98% (HPLC)

DMSO:5mg/ml (12 Mm; Need ultrasonic)

CCC1=NN2C(N=C(C)C=C2C)=C1CC1=CC=C(C=C1)C1=NN=C(O1)C1CCNCC1

——

(-20℃)

With Ice Pack

≥ 2 years