NE 52-QQ57
目录号: PL01282 纯度: ≥99%
CAS No. :1401728-56-0
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PL01282-5mg 5mg ¥4574.55 请登录
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PL01282-200mg 200mg 询价 询价
PL01282-10mM*1mLinDMSO 10mM*1mLinDMSO ¥5032.00 请登录
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中文名称
NE 52-QQ57
英文名称
NE 52-QQ57
英文别名
GPR4 antagonist 13;GTPL10206;BDBM123510;example 35 [WO2012131633A1];J3.652.496K;US8748435, 35;2-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidine-3-yl)methyl]phenyl]-5-(piperidine-4-yl)-1,3,4-oxadiazole;2-(4-((2-Ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole;2-[4-[(2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl]phenyl]-5-piperidin-4-yl-1,3,4-oxadiazole;CID 68379135;NE 52-QQ57;NE52QQ57;AMY24092;s6850;2-[4-[(2-Ethyl-5,7-dimethylpyrazolo[1,5-a]p
Cas No.
1401728-56-0
分子式
C24H28N6O
分子量
416.52
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
NE 52-QQ57 是选择性,有口服活性的 GPR4 拮抗剂,IC50为70 nM。NE 52-QQ57 具有抗炎活性。
生物活性
NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC 50 of 70 nM. NE 52-QQ57 has anti-inflammatory activity.
性状
Solid
IC50 & Target[1][2]
IC50: 70 nM (GPR4).
体外研究(In Vitro)
NE 52-QQ57 effectively blocks GPR4-mediated cAMP accumulation (IC50 26.8?nM in HEK293?cells). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
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.
溶解度数据
In Vitro: DMSO : 20 mg/mL (48.02 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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