NE52-QQ57 is an orally available GPR4 antagonist with an IC50 of 70 nM. NE 52-QQ57 significantly inhibited the AGE-induced increased expression of several key inflammatory cytokines and signaling molecules, including tumor necrosis factor-α (TNF-α), interleukin (IL)-1β, IL-6, inducible nitric oxide synthase (iNOS), nitric oxide (NO), cyclooxygenase 2 (COX2), and prostaglandin E2 (PGE2).
仅供研究使用。 我们不向患者出售。
名称 | NE 52-QQ57 |
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Iupac 化学名称 | 2-(4-((2-ethyl-5,7-dimethylpyrazolo[1,5-a]pyrimidin-3-yl)methyl)phenyl)-5-(piperidin-4-yl)-1,3,4-oxadiazole |
同义词 | NE52-QQ57; NE-52-QQ57; NE 52-QQ57; NE52QQ57; NE-52QQ57; NE 52QQ57; |
英文同义词 | NE52-QQ57; NE-52-QQ57; NE 52-QQ57; NE52QQ57; NE-52QQ57; NE 52QQ57; |
分子式 | C24H28N6O |
分子量 | 416.529 |
Smile | CCC1=NN(C(C)=CC(C)=N2)C2=C1CC3=CC=C(C4=NN=C(C5CCNCC5)O4)C=C3 |
InChiKey | HXPQWNPLNIEJOW-UHFFFAOYSA-N |
InChi | InChI=1S/C24H28N6O/c1-4-21-20(22-26-15(2)13-16(3)30(22)29-21)14-17-5-7-18(8-6-17)23-27-28-24(31-23)19-9-11-25-12-10-19/h5-8,13,19,25H,4,9-12,14H2,1-3H3 |
Cas号 | 1401728-56-0 |
相关CAS号 |
包装 | 价格 | 库存 | 纯度 | 备货期 |
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大货 | 询价 | 询价 | 询价 |
外观性状 | 固体粉末 |
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纯度 | 98% Min. |
存储 | 短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度 |
可溶性 | 可溶于DMSO |
处理方式 | |
运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周 |
海关编码 |
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Mechanism | |
Cell study | |
Animal study | |
Clinical study |
1: Liu H, Liu Y, Chen B. Antagonism of GPR4 with NE 52-QQ57 and the Suppression of AGE-Induced Degradation of Type II Collagen in Human Chondrocytes. Chem Res Toxicol. 2020 May 18. doi: 10.1021/acs.chemrestox.0c00111. Epub ahead of print. PMID: 32370492.
2: 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. doi: 10.1016/j.neuropharm.2018.06.007. Epub 2018 Jun 9. PMID: 29894771; PMCID: PMC6063991.