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首页-小分子抑制剂&激动剂-GPCR-Proton-sensing GPCRs-NE 52-QQ57
NE 52-QQ57

Chemical Structure : NE 52-QQ57

CAS No.: 1401728-56-0

NE 52-QQ57 (NE52-QQ57, GPR4 antagonist 13)

货号: PC-20835Not For Human Use, Lab Use Only.

NE 52-QQ57 (GPR4 antagonist 13) is a potent, elective, and efficacious GPR4 antagonist with IC50 of 70 nM (hGPR4).

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25 mg ¥2980 In stock
50 mg ¥4880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

NE 52-QQ57 (GPR4 antagonist 13) is a potent, elective, and efficacious GPR4 antagonist with IC50 of 70 nM (hGPR4).
GPR4 antagonist 13 displays no significant inhibition against a panel of enzymes, receptors, and ion channels.
GPR4 antagonist 13 is also selective over the related proton sensing receptors OGR1 and TDAG8.
GPR4 antagonist 13 weakly inhibits rat GPR4 with IC50 of 1.84 uM.
GPR4 antagonist 13 shows significant efficacy in the rat antigen induced arthritis as well as in the hyperalgesia and angiogenesis model at a well-tolerated dose of 30 mg/kg.

物理化学性质&存储条件

分子量 416.53
分子式 C24H28N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole

参考文献

1. Juraj Velcicky, et al. J Med Chem. 2017 May 11;60(9):3672-3683.

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