GNE-616

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GNE-616

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2349371-81-7

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

GNE-616 是一种高效的，代谢稳定的，具有口服活性的，亚型选择性的Nav1.7抑制剂 (对 hNav1.7 的K_i值为 0.79 nM，K_d值为 0.38 nM)，用于慢性疼痛的相关研究。与 hNav1.1，hNav1.3, hNav1.4，hNav1.5 相比，GNE-616 显示大于 1000 nM 的 K_d值和大于 2500 倍的选择性。对 hNav1.2 和 hNav1.6 的选择性分别是 31 倍和 73 倍。

生物活性

GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selectiveNav1.7inhibitor (K_iof 0.79 nM andK_dof 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM K_dand >2500-fold selectivity over hNav1.1, hNav1.3, hNav1.4, and hNav1.5. Selectivity over hNav1.2 and hNav1.6 is more modest at 31- and 73-fold, respectively^[1].

IC₅₀& Target^[1]

hNa_v1.7

0.79 nM (Ki)

hNa_v1.7

0.38 nM (Kd)

体外研究
(In Vitro)

Site-directed mutagenesis is critical for the isoform selectivity profile of GNE-616 (hNav1.7, K_d: Y1537s/W1538=170±67 nM, V1541=3.9±1.1 nM, Y1537s/W1538/V1541=790±350 nM)^[1].

体内研究
(In Vivo)

GNE-616 shows robust activity in a Nav1.7-dependent inherited erythromelalgia (IEM) PK/PD model with an EC₅₀of 740 nM and EC₅₀,u of 9.6 nM^[1].

分子量

537.53

Formula

C₂₄H₂₃F₄N₅O₃S

CAS 号

2349371-81-7

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.