1. Membrane Transporter/Ion Channel
  2. Sodium Channel
  3. TC-N 1752

TC-N 1752 是一种有效和具有口服活性的 Nav1.7 抑制剂,抑制 hNav1.7hNav1.3hNav1.4hNaV1.5rNav1.8IC50 值分别为 0.17 μM,0.3 μM,0.4 μM,1.1 μM 和 2.2 μM。TC-N 1752 还抑制河豚毒素敏感的钠通道。TC-N 1752 在福尔马林疼痛模型中显示出镇痛效果。

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TC-N 1752 Chemical Structure

TC-N 1752 Chemical Structure

CAS No. : 1211866-85-1

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1650
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1 mg ¥681
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5 mg ¥1500
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10 mg ¥2500
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25 mg ¥5500
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50 mg ¥9500
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Customer Review

Other Forms of TC-N 1752:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain[1][2][3].

IC50 & Target[1][2]

hNav1.7

0.17 μM (IC50)

hNav1.3

0.3 μM (IC50)

hNav1.4

0.4 μM (IC50)

hNav1.5

1.1 μM (IC50)

hNav1.8

0.1 μM (IC50)

体外研究
(In Vitro)

TC-N 1752 (compound 52) state-dependently inhibits Nav1.7, with IC50 of 170 nM on channels that are 20% inactivated and IC50 of 3.6 μM on fully noninactivated channels[1].
TC-N 1752 inhibits hNav1.7, hNav1.8, hNav1.9, rNav1.9, and mNav1.9 with IC50s of 0.2, 0.1, 1.6, 0.5 and 1.4 μM, respectively[2].

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

体内研究
(In Vivo)

TC-N 1752 (compound 52) (3-30 mg/kg; p.o.) dose-dependently shows analgesic effect in the Formalin model[1].
TC-N 1752 (3-30 mg/kg; p.o.) decreases thermal hyperalgesia produced by inflammation[3].
TC-N 1752 (5 mg/mL; 500 μL; i.v.) attenuates complete Freund’s adjuvant (CFA)-induced sensitization of C-fiber nociceptors[3].

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

Animal Model: Rats were injected intraplantar with Formalin[1]
Dosage: 3, 10, 20, 30 mg/kg
Administration: Administered p.o. 120 min prior to Formalin
Result: Showed analgesic efficacy starting at the dose of 3 mg/kg, with full efficacy at 20 mg/kg dose.
分子量

516.52

Formula

C25H27F3N6O3

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (242.00 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9360 mL 9.6802 mL 19.3603 mL
5 mM 0.3872 mL 1.9360 mL 3.8721 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9360 mL 9.6802 mL 19.3603 mL 48.4008 mL
5 mM 0.3872 mL 1.9360 mL 3.8721 mL 9.6802 mL
10 mM 0.1936 mL 0.9680 mL 1.9360 mL 4.8401 mL
15 mM 0.1291 mL 0.6453 mL 1.2907 mL 3.2267 mL
20 mM 0.0968 mL 0.4840 mL 0.9680 mL 2.4200 mL
25 mM 0.0774 mL 0.3872 mL 0.7744 mL 1.9360 mL
30 mM 0.0645 mL 0.3227 mL 0.6453 mL 1.6134 mL
40 mM 0.0484 mL 0.2420 mL 0.4840 mL 1.2100 mL
50 mM 0.0387 mL 0.1936 mL 0.3872 mL 0.9680 mL
60 mM 0.0323 mL 0.1613 mL 0.3227 mL 0.8067 mL
80 mM 0.0242 mL 0.1210 mL 0.2420 mL 0.6050 mL
100 mM 0.0194 mL 0.0968 mL 0.1936 mL 0.4840 mL
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:
TC-N 1752
目录号:
HY-107405
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