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TC-N 1752
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TC-N 1752图片
CAS NO:1211866-85-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议

产品介绍
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。
生物活性

TC-N 1752 is a potent and orally active inhibitor ofNav1.7, withIC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM athNav1.7,hNav1.3,hNav1.4,hNaV1.5andrNav1.8, 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 IC50of 170 nM on channels that are 20% inactivated and IC50of 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].

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].

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

性状

Solid

Formula

C25H27F3N6O3

CAS 号

1211866-85-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 125 mg/mL(242.00 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.9360 mL9.6802 mL19.3603 mL
5 mM0.3872 mL1.9360 mL3.8721 mL
10 mM0.1936 mL0.9680 mL1.9360 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。