1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. TC-N 22A

TC-N 22A 是一种强效的、选择性的、口服活性的、可以通透血脑的 mGlu4 正向别构调节剂 (PAM),在表达人 mGlu4 的 BHK 细胞中 EC50 为 9 nM。TC-N 22A 在激动和正向别构模型中,对 mGlu 1、2、3、5 和 7 受体的活性很小 (EC50 >10 μM)。TC-N 22A 可以用于中枢神经系统疾病研究的潜力。

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TC-N 22A Chemical Structure

TC-N 22A Chemical Structure

CAS No. : 1314140-00-5

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
1 mg ¥2627
1 - 2 周
5 mg   询价  
10 mg   询价  

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo[1].

IC50 & Target

EC50: 9 nM (mGlu4 receptor)
EC50: >10 μM (mGlu 1, 2, 3, 5, and 7 receptors)[1]

体外研究
(In Vitro)

TC-N 22A is selected for mGlu4 and has an EC50 of 9 nM in human mGlu4-expressing BHK cells. This compound is less active in agonist and PAM modelinactive (EC50>10 μM), and is inactive in negative allosteric modulator (NAM) model at mGlu 1, 2, 3, 5, and 7 receptors (IC50 >10 μM) and shows low potential for hERG channel inhibition[1].

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

体内研究
(In Vivo)

TC-N 22A (oral administration; 10 mg/kg) displays good plasma (259 ng/mL) and brain exposure levels (200 ng/mL) as well as good brain penetration (brain/plasma ratios of 0.8) after 1 h following a 10 mg/kg oral administration in SpragueDawley rats[1].

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

分子量

283.35

Formula

C14H13N5S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据
  • 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

动物实验:

以下溶解方案源自文献,仅供参考,建议您先取少量样品进行尝试。

  • 方案 一

    TC-N 22A is suspended in 20% aqueous hydroxypropyl β-cyclodextrin[1].

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

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
参考文献
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.

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产品名称:
TC-N 22A
目录号:
HY-18679
需求量: