2. Membrane Transporter/Ion Channel
  3. Sodium Channel
  4. AMG8379

AMG8379 是一种有效的、口服的、选择性的、电压门控钠通道 NaV1.7 拮抗剂， 对人和小鼠 NaV1.7 的 IC50 值分别为 8.5 和 18.6 nM。AMG8379 能可逆地阻断背根神经节 (DRG) 神经元内源性河豚毒素 (TTX) 敏感钠通道， IC50为 3.1 nM。

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AMG8379 Chemical Structure

AMG8379 Chemical Structure

CAS No. : 1642112-31-9

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Other Forms of AMG8379:

AMG8379 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM[1].

IC50 & Target

hNav1.7

8.5 nM (IC50)

mNav1.7

18.6 nM (IC50)

体外研究
(In Vitro)

AMG8379 is 100 to 1000-fold selective over other NaV family members, including NaV1.4 expressed in muscle and NaV1.5 expressed in heart, as well as TTX-resistant NaV channels in DRG neurons[1].
The IC50 for AMG8379 inhibition of C-fiber spiking based on the level of firing in NaV1.7 KO mice representing complete pharmacological block of the NaV1.7-component of this assay is calculated. In this manner, the IC50 for AMG8379 block is 47.0 ± 8.1 nM[1].

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

AMG8379 相关抗体:
体内研究
(In Vivo)

AMG8379 (30-100 mg/kg; p.o.) inhibits Capsaicin-induced nociceptive behavior[1].

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

Animal Model: CD-1 male mice[1]
Dosage: 30 or 100 mg/kg body weight
Administration: Oral
Result: Showed a dose-dependent reduction in overall nociceptive behavior.
分子量

543.93

Formula

C25H16ClF2N3O5S
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

AMG8379 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

AMG83791642112-31-9AMG 8379AMG-8379Sodium ChannelNa channelsNa+ channelsselectiveoraldorsalrootgangliasulfonamideC-fibernociceptivepainitchInhibitorinhibitorinhibit

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产品名称：
AMG8379
目录号：
HY-108425
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