2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. TC-I 2014

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。

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TC-I 2014 Chemical Structure

TC-I 2014 Chemical Structure

CAS No. : 1221349-53-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2468
In-stock
5 mg ￥2400
In-stock
10 mg ￥3850
In-stock
25 mg 现货 询价
50 mg 现货 询价
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

TC-I 2014 相关抗体

Top Publications Citing Use of Products

查看 TRP Channel 亚型特异性产品:

查看所有亚型
TRPC TRPM TRPV TRPA TRPML

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

TRPM8[1].
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
0.413 nM
Compound: 5
Inhibition of human TRPM8 expressed in HEK293 cells assessed as inhibition of cold-induced channel current by whole cell electrophysiology
Inhibition of human TRPM8 expressed in HEK293 cells assessed as inhibition of cold-induced channel current by whole cell electrophysiology
[PMID: 21128593]
HEK293 IC50
0.8 nM
Compound: 5
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay
[PMID: 21128593]
HEK293 IC50
3 nM
Compound: 5
Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay
Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay
[PMID: 21128593]
HEK293 IC50
4 nM
Compound: 5
Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay
Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay
[PMID: 21128593]
体外研究
(In Vitro)

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[1].

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

TC-I 2014 相关抗体:
体内研究
(In Vivo)

TC-I 2014 (10 mg/kg, Orally once) completely prevents icilin-induced WDS[1].

MCE 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[1].
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.
分子量

467.41

Formula

C23H19F6N3O
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 : 250 mg/mL (534.86 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 2.1394 mL 10.6972 mL 21.3945 mL
5 mM 0.4279 mL 2.1394 mL 4.2789 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

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: ≥99.0%

COA (265 KB) 元素分析报告 (212 KB)

产品使用指南 (1538 KB)
参考文献

TC-I 2014 相关分类

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 2.1394 mL 10.6972 mL 21.3945 mL 53.4862 mL
5 mM 0.4279 mL 2.1394 mL 4.2789 mL 10.6972 mL
10 mM 0.2139 mL 1.0697 mL 2.1394 mL 5.3486 mL
15 mM 0.1426 mL 0.7131 mL 1.4263 mL 3.5657 mL
20 mM 0.1070 mL 0.5349 mL 1.0697 mL 2.6743 mL
25 mM 0.0856 mL 0.4279 mL 0.8558 mL 2.1394 mL
30 mM 0.0713 mL 0.3566 mL 0.7131 mL 1.7829 mL
40 mM 0.0535 mL 0.2674 mL 0.5349 mL 1.3372 mL
50 mM 0.0428 mL 0.2139 mL 0.4279 mL 1.0697 mL
60 mM 0.0357 mL 0.1783 mL 0.3566 mL 0.8914 mL
80 mM 0.0267 mL 0.1337 mL 0.2674 mL 0.6686 mL
100 mM 0.0214 mL 0.1070 mL 0.2139 mL 0.5349 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-I 20141221349-53-6TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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