TC-I 2014|cas:1221349-53-6|西域试剂

TC-I 2014,99.0%

产品编号：Bellancom-110199| CAS NO：1221349-53-6| 分子式：C₂₃H₁₉F₆N₃O| 分子量：467.41

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-110199		￥3500.00	杭州北京（现货）

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TC-I 2014

产品介绍

TC-I 2014 hydrochloride 是一种口服有效的、强效的、苯并咪唑类的、 TRPM8 的拮抗剂，其对犬类、人和大鼠通道的IC₅₀ 值分别为 0.8 nM, 3.0 nM 和 4.4 nM。在疼痛动物模型中具有抗痛觉超敏作用。

生物活性

TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC₅₀ values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models.

体外研究

TC-I 2014 (compound 5) potently inhibits cold-induced TRPM8 currents in HEK293 cells stably expressing canine or human TRPM8, with IC₅₀ values of 0.413 and 1 nM, respectively.

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

体内研究

TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS.

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

Animal Model:	TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS.
Dosage:	3, 5.6, 10 mg/kg.
Administration:	Orally once.
Result:	Produced greater than 90% inhibition at 3, 5.6, and 10 mg/kg administered 2 h prior to icilin challenge.

体内研究

TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS.

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

Animal Model:	TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS.
Dosage:	3, 5.6, 10 mg/kg.
Administration:	Orally once.
Result:	Produced greater than 90% inhibition at 3, 5.6, and 10 mg/kg administered 2 h prior to icilin challenge.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (534.86 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1394 mL	10.6972 mL	21.3945 mL
5 mM	0.4279 mL	2.1394 mL	4.2789 mL
10 mM	0.2139 mL	1.0697 mL	2.1394 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