TC-N 1752|cas:1211866-85-1|西域试剂

TC-N 1752,99.18%

产品编号：Bellancom-107405| CAS NO：1211866-85-1| 分子式：C₂₅H₂₇F₃N₆O₃| 分子量：516.52

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货号	价格	库存与货期
Bellancom-107405	￥1500.00	杭州北京（现货）
Bellancom-107405	￥2500.00	杭州北京（现货）
Bellancom-107405	￥5500.00	杭州北京（现货）
Bellancom-107405	￥9500.00	杭州北京（现货）

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TC-N 1752

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 hNav1.7，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。

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.

体外研究

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.
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.

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

体内研究

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

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

Animal Model:	Rats were injected intraplantar with Formalin
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.

体内研究

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

Animal Model:	Rats were injected intraplantar with Formalin
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.

性状

Solid

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 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

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。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式