TC-N 1752

目录号: HY-107405 纯度: 99.18%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

TC-N 1752 是一种有效和具有口服活性的 Nav1.7 抑制剂，抑制 hNav1.7，hNav1.3，hNav1.4，hNaV1.5 和 rNav1.8 的 IC₅₀ 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。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

TC-N 1752 Chemical Structure

CAS No. : 1211866-85-1

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1650	In-stock
1 mg	￥681	In-stock
5 mg	￥1500	In-stock
10 mg	￥2500	In-stock
25 mg	￥5500	In-stock
50 mg	现货	询价
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of TC-N 1752:

TC-N 1752-d₅ 询价

TC-N 1752 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Sodium Channel 亚型特异性产品:

查看所有亚型

Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8

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]

hNa_v1.7

0.17 μM (IC₅₀)

hNa_v1.3

0.3 μM (IC₅₀)

hNa_v1.4

0.4 μM (IC₅₀)

hNa_v1.5

1.1 μM (IC₅₀)

hNa_v1.8

0.1 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	> 10 μM Compound: 52	Inhibition of human Erg expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of human Erg expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	> 10 μM Compound: 52	Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	> 10 μM Compound: 52	Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	> 10 μM Compound: 52	Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of fully inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	0.3 μM Compound: 52	Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.3 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	0.4 μM Compound: 52	Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.4 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	0.5 μM Compound: 52	Inhibition of human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	1.1 μM Compound: 52	Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of 20% inactivated TTX-resistant human sodium channel Nav1.5 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	170 nM Compound: 52	Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	2.2 μM Compound: 52	Inhibition of 20% inactivated TTX-resistant rat sodium channel Nav1.8 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay Inhibition of 20% inactivated TTX-resistant rat sodium channel Nav1.8 expressed in human HEK293 cells at 1 uM by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	3.3 μM Compound: 52	Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay in presence of 5% human serum albumin Inhibition of 20% inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay in presence of 5% human serum albumin	[PMID: 21634377]
HEK293	IC₅₀	3.6 μM Compound: 52	Inhibition of fully inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of fully inactivated human sodium channel Nav1.7 expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]
HEK293	IC₅₀	5.2 μM Compound: 52	Inhibition of human cardiac sodium channel Nav1.5 expressed in human HEK293 cells by patch-clamp electrophysiological assay Inhibition of human cardiac sodium channel Nav1.5 expressed in human HEK293 cells by patch-clamp electrophysiological assay	[PMID: 21634377]

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

1211866-85-1

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
10 mM	0.1936 mL	0.9680 mL	1.9360 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)

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)

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

每只动物的给药体积

μL

动物数量

只

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

纯度: 99.18%

选择批次：

Data Sheet (592 KB) SDS (251 KB)

COA (260 KB) HNMR (290 KB) LCMS (269 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Bregman H, et, al. Identification of a potent, state-dependent inhibitor of Nav1.7 with oral efficacy in the formalin model of persistent pain. J Med Chem. 2011 Jul 14;54(13):4427-45. [Content Brief]

[2]. Lin Z, et, al. Biophysical and Pharmacological Characterization of Nav1.9 Voltage Dependent Sodium Channels Stably Expressed in HEK-293 Cells. PLoS One. 2016 Aug 24;11(8):e0161450. [Content Brief]

[3]. Matson DJ, et, al. Inhibition of Inactive States of Tetrodotoxin-Sensitive Sodium Channels Reduces Spontaneous Firing of C-Fiber Nociceptors and Produces Analgesia in Formalin and Complete Freund's Adjuvant Models of Pain. PLoS One. 2015 Sep 17;10(9):e013 [Content Brief]

TC-N 1752 相关分类

Neurological Disease

完整储备液配制表

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.

Keywords:

TC-N 17521211866-85-1Sodium ChannelNa channelsNa+ channelsFormalinpainanalgesicInhibitorinhibitorinhibit

您最近查看的产品:

产品名称：

* 需求量：

* 客户姓名：

* Email：

* 电话：

* 公司或机构名称：

留言给我们：

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。	站点地图隐私声明
沪ICP备15051369号-4 上海工商沪公网安备31011502019417 沪(浦)应急管危经许[2021]201709(QFYS) 营业执照（三证合一）
Copyright © 2013-2024 MedChemExpress. All Rights Reserved.

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

TC-N 1752

Customer Review

Other Forms of TC-N 1752: