2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. GNE-616

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 Ki 值为 0.79 nM，Kd 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 Kd 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。

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GNE-616 Chemical Structure

GNE-616 Chemical Structure

CAS No. : 2349371-81-7

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GNE-616 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GNE-616 is a highly potent, metabolically stable, orally bioavailable, and subtype selective Nav1.7 inhibitor (Ki of 0.79 nM and Kd of 0.38 nM for hNav1.7) for the treatment of chronic pain. GNE-616 shows >1000 nM Kd and >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]

hNav1.7

0.79 nM (Ki)

hNav1.7

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, Kd: Y1537s/W1538=170±67 nM, V1541=3.9±1.1 nM, Y1537s/W1538/V1541=790±350 nM)[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GNE-616 相关抗体:
体内研究
(In Vivo)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

537.53

Formula

C24H23F4N5O3S
CAS 号
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.
纯度 & 产品资料
参考文献

GNE-616 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNE-6162349371-81-7GNE616GNE 616Sodium ChannelNa channelsNa+ channelsInhibitorinhibitorinhibit

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产品名称：
GNE-616
目录号：
HY-126291
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