NE 52-QQ57

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NE 52-QQ57 是一种选择性口服 GPR4 拮抗剂 (IC50 : 70 nM)，具有抗炎活性。

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%).

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Others

Other Targets

GPR4

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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

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(-20℃)

With Ice Pack

≥ 2 years