JNJ-54175446
JNJ-54175446 is a potent and selective P2X7 Receptor Antagonist. JNJ-54175446 is potent, stable in liver microsomes and has an acceptable protein binding profile. JNJ-54175446 is highly permeable and has no evidence of efflux as measured by a Caco-2 cell line. JNJ-54175446 efficiently binds to recombinant rat and human P2X7 and to native tissues in both human and rat. JNJ-54175446 also inhibited P2X7 activity in human, rat, dog, mouse, and macaque Ca2+ flux assays and inhibited IL1-β release in human peripheral blood monocytes (pIC50 of 7.7 ± 0.1) and in human whole blood (pIC50 of 8.1 ± 0.1).
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化学信息
| 名称 | JNJ-54175446 |
|---|---|
| Iupac 化学名称 | (R)-(2-chloro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyrimidin-2-yl)-4-methyl-1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridin-5-yl)methanone |
| 分子式 | C18H13ClF4N6O |
| 分子量 | 440.78 |
| Smile | ClC1=C(C(F)(F)F)C=CC=C1C(N(CC2)[C@H](C)C(N=N3)=C2N3C4=NC=C(C=N4)F)=O |
| InChiKey | CWFVVQFVGMFTBD-SECBINFHSA-N |
| InChi | InChI=1S/C18H13ClF4N6O/c1-9-15-13(29(27-26-15)17-24-7-10(20)8-25-17)5-6-28(9)16(30)11-3-2-4-12(14(11)19)18(21,22)23/h2-4,7-9H,5-6H2,1H3/t9-/m1/s1 |
| Cas号 | 1627902-21-9 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 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 | 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 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Letavic MA, Savall BM, Allison BD, Aliusio L, Andrés JI, De Angelis M, Ao H, Beauchamp DA, Bonaventure P, Bryant S, Carruthers NI, Ceusters M, Coe KJ, Dvorak CA, Fraser I, Gelin CF, Koudriakova T, Liang J, Lord B, Lovenberg TW, Otieno M, Schoetens F, Swanson DM, Wang Q, Wickenden AD, Bhattacharya A. 4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate. J Med Chem. 2017 May 11. doi: 10.1021/acs.jmedchem.7b00408. [Epub ahead of print] PubMed PMID: 28493698.
