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CAS No.: 1401728-56-0

NE 52-QQ57 Catalog No. CSN27549

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

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靶点选择性

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描述GPR4, a proton sensing G protein-coupled receptor (GPCR), has been shown to respond to acidic pH by eliciting cAMP via gas signaling and plays a key role in tissue acidosis. NE 52-QQ57 is a selective and orally available GPR4 antagonist with an IC₅₀ value of 70 nM^[3]. In HEK293 cells, NE 52-QQ57 effectively blocked GPR4-mediated cAMP accumulation with an IC₅₀ value of 26.8 nM. In HUVEC cells which natively express GPR4, physiological acidification (pH 7.4-7.0) resulted in a cAMP increase by ∼55% which was completely prevented by 1 μM NE 52-QQ57. In unanaesthetised mice and rats, NE 52-QQ57 (20 mg/kg) reduced ventilatory response to 5 and 10% CO₂^[4].
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.
[3] Velcicky J, Miltz W, Oberhauser B, Orain D, Vaupel A, Weigand K, Dawson King J, Littlewood-Evans A, Nash M, Feifel R, Loetscher P. 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.
[4] Hosford PS, Mosienko V, Kishi K, Jurisic G, Seuwen K, Kinzel B, Ludwig MG, Wells JA, Christie IN, Koolen L, Abdala AP, Liu BH, Gourine AV, Teschemacher AG, Kasparov S. CNS distribution, signalling properties and central effects of G-protein coupled receptor 4. Neuropharmacology. 2018 Aug;138:381-392.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4009 mL
- 12.0043 mL
- 24.0085 mL
- 5 mM
- 0.4802 mL
- 2.4009 mL
- 4.8017 mL
- 10 mM
- 0.2401 mL
- 1.2004 mL
- 2.4009 mL

技术信息

CAS号

1401728-56-0

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H28N6O

运输

蓝冰

分子量

416.52

别名

溶解度

DMSO	12.0 mg/mL (28.8 mM)
Water	Insoluble
Ethanol	50.0 mg/mL (120.0 mM)

动物实验配方

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总药量计算器 ✕

动物实验：给药剂量mg/kg 动物体重g 动物数量只每天给药次给药天

需要的总药量：mg

工作液计算器 ✕

动物实验：给药剂量mg/kg 动物体重g 给药体积μL

您需要配制的工作液浓度为：mg/mL

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