GNE-131
GNE-131 is a Potent and Selective hNaV1.7 Inhibitor (Na V1.7 IC50 = 3 nM) for the Treatment of Pain. GNE-131 showed excellent potency, good in vitro metabolic stability, and low in vivo clearance in mouse, rat and, dog. GNE-131 also displayed excellent efficacy in a transgenic mouse model of induced pain.
仅供研究使用。 我们不向患者出售。
化学信息
| 名称 | GNE-131 |
|---|---|
| Iupac 化学名称 | N-(7-(Adamantan-1-ylmethoxy)-6-cyclopropyl-[1,2,4]-triazolo[4,3-a]-pyridin-3-yl)cyclo-propanesulfonamide |
| 同义词 | GNE-131; GNE 131; GNE131; |
| 英文同义词 | GNE-131; GNE 131; GNE131 |
| 分子式 | C23H30N4O3S |
| 分子量 | 442.58 |
| Smile | O=S(C1CC1)(NC2=NN=C3C=C(OCC45CC6CC(C5)CC(C6)C4)C(C7CC7)=CN32)=O |
| InChiKey | FPERPEQIXLOVIK-UHFFFAOYSA-N |
| InChi | InChI=1S/C23H30N4O3S/c28-31(29,18-3-4-18)26-22-25-24-21-8-20(19(12-27(21)22)17-1-2-17)30-13-23-9-14-5-15(10-23)7-16(6-14)11-23/h8,12,14-18H,1-7,9-11,13H2,(H,25,26) |
| Cas号 | 1629063-81-5 |
| 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 | 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 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Focken T, Chowdhury S, Zenova A, Grimwood ME, Chabot C, Sheng T, Hemeon I, Decker SM, Wilson M, Bichler P, Jia Q, Sun S, Young C, Lin S, Goodchild SJ, Shuart NG, Chang E, Xie Z, Li B, Khakh K, Bankar G, Waldbrook M, Kwan R, Nelkenbrecher K, Karimi Tari P, Chahal N, Sojo L, Robinette CL, White AD, Chen CA, Zhang Y, Pang J, Chang JH, Hackos DH, Johnson JP, Cohen CJ, Ortwine DF, Sutherlin DP, Dehnhardt CM, Safina BS. Design of Conformationally Constrained Acyl Sulfonamide Isosteres: Identification of N-([1,2,4]Triazolo[4,3-a]pyridin-3-yl)methane-sulfonamides as Potent and Selective hNaV1.7 Inhibitors for the Treatment of Pain. J Med Chem. 2018 May 8. doi: 10.1021/acs.jmedchem.7b01826. [Epub ahead of print] PubMed PMID: 29737846.
