2. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. Sodium Channel Cytochrome P450
  4. 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 CYP2C9 和 CYP3A4 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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Nav1.7-IN-8 相关抗体

Top Publications Citing Use of Products

查看 Sodium Channel 亚型特异性产品:

查看所有亚型
Nav1.1 Nav1.2 Nav1.3 Nav1.4 Nav1.5 Nav1.6 Nav1.7 Nav1.8

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
0.4 nM
Compound: 3
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
[PMID: 26985315]
HEK293 IC50
0.4 nM
Compound: 3
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage clamp analysis
Inhibition of full length human Nav1.7 channel expressed in HEK cells co-expressing human sodium channel subunit beta3 at -150 mV by manual voltage clamp analysis
[PMID: 26985315]
HEK293 IC50
11 nM
Compound: 3
Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.6 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
[PMID: 26985315]
HEK293 IC50
1380 nM
Compound: 3
Inhibition of full length human Nav1.5 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.5 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -60 mV by automated voltage clamp analysis
[PMID: 26985315]
HEK293 IC50
3080 nM
Compound: 3
Inhibition of full length human Nav1.1 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -40 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.1 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -40 mV by automated voltage clamp analysis
[PMID: 26985315]
HEK293 IC50
4.2 nM
Compound: 3
Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
Inhibition of full length human Nav1.2 channel expressed in HEK cells co-expressing human sodium channel subunit beta1 at holding potential -35 mV by automated voltage clamp analysis
[PMID: 26985315]
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.

Nav1.7-IN-8 相关抗体:
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

Nav1.7-IN-8 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:

Nav1.7-IN-81432913-44-4Sodium ChannelCytochrome P450Na channelsNa+ channelsCYPspotentselectivityhNaV1.1hNaV1.5analgesicacuteinflammatorypainInhibitorinhibitorinhibit

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