NE 52-QQ57
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货号：A1165850
NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity.
NE 52-QQ57 化学结构
NE 52-QQ57 3D分子结构
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NE 52-QQ57 纯度/质量文件 产品仅供科研
货号：A1165850
标准纯度：
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NE 52-QQ57 质控信息
NE 52-QQ57 生物活性
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] 50 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]
NE 52-QQ57 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.
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NE 52-QQ57 实验方案
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1mg
5mg
10mg
1 mM
5 mM
10 mM
2.40mL
0.48mL
0.24mL
12.00mL
2.40mL
1.20mL
24.01mL
4.80mL
2.40mL
NE 52-QQ57 技术信息
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