货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
T95838-1ml促销	10mM in DMSO	￥720.00 ￥648.00 T95838-1ml ￥648.00 现货	6 6	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

T95838-1ml促销

10mM in DMSO

￥720.00 ￥648.00

产品描述：

TNF-α 选择性抑制剂 | 活化剂 | 拮抗剂;TNF-α Selective Inhibitors | Activators | Antagonists;;InformationNE 52-QQ57 is a selective, and orally available antagonist ofG-protein coupled receptor 4 (GPR4)with IC50 of 0.07 μM. NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation with IC50 of 26.8 nM in HEK293 cells. The antagonism of GPR4 with NE 52-QQ57 significantly inhibits the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, includingtumor necrosis factor-α (TNF-α),interleukin (IL)-1β,IL-6,inducible nitricTargetsTNF-α ; IL-1β ; IL-6 ; iNOS ; NO 33706,;

靶点：

IC50: 70 nM (GPR4).

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.

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.

保存条件：

-80℃（运输条件：冰袋低温运输）

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。

参考文献

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