1. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  2. Sodium Channel Cytochrome P450
  3. Nav1.7-IN-8

Nav1.7-IN-8 是一种有效的 NaV1.7 的阻断物,对 NaV1.7 在 hNaV1.1 和 hNaV1.5 亚型上的抑制具有高选择性。Nav1.7-IN-8 对 CYP2C9CYP3A4 的抑制 IC50 分别为 0.17 μM 和 0.077 μM。Nav1.7-IN-8 可用于急性和炎症性疼痛模型中缓解疼痛的研究。

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Nav1.7-IN-8 Chemical Structure

Nav1.7-IN-8 Chemical Structure

CAS No. : 1432913-44-4

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain[1].

IC50 & Target

CYP2C9

0.17 μM (IC50)

CYP3A4

0.077 μM (IC50)

体外研究
(In Vitro)

Nav1.7-IN-8 plasma protein binding is very high in rat with a free fraction of ∼1.1 %[1].

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

体内研究
(In Vivo)

Nav1.7-IN-8 (0~100 mpk, i.p.; 1 hour) shows a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produces a substantial inhibition of the pain response[1].
. Nav1.7-IN-8 (10~100 mpk, i.p.; 2 days) displays a dose-dependent reduction of the pain response[1].

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

Animal Model: Rats[1]
Dosage: 0~100 mpk
Administration: I.p.; 1 hour
Result: Showed a reduction of the pain response in phase 2a of the formalin assay in a dose dependent manner and produced a substantial inhibition of the pain response.
Animal Model: Mice[1]
Dosage: 10~100 mpk
Administration: I.p.; 2 days
Result: Displayed a dose-dependent reduction of the pain response.
分子量

535.93

Formula

C21H12ClF2N5O4S2

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
  • 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.

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产品名称:
Nav1.7-IN-8
目录号:
HY-141547
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