产品
编 号：F151335
分子式：C24H28N6O
分子量：416.52
分子式：C24H28N6O
分子量：416.52
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 1401728-56-0
产品详情
生物活性：
NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity.
体内研究：
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%).
体外研究：
NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation (IC50 26.8?nM in HEK293?cells).
NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity.
体内研究：
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%).
体外研究：
NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation (IC50 26.8?nM in HEK293?cells).
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