• 产品描述： NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity

• 靶点： IC50: 70 nM (GPR4);GPR

• 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.

• 参考文献：
  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. 2. Hosford PS, et al. CNS distribution, signalling properties and central effects of G-protein coupled receptor 4. Neuropharmacology. 2018 Aug;138:381-392.

• 溶解性： Soluble  in  DMSO

• 保存条件： -20°C

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	2.401 ml	12.004 ml	24.008 ml
  5 mM	0.48 ml	2.401 ml	4.802 ml
  10 mM	0.24 ml	1.2 ml	2.401 ml
  50 mM	0.048 ml	0.24 ml	0.48 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

输入产品批号：

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *