1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. TCN238

TCN238 是一种口服有效的 mGlu4 受体的正变构调节物,EC50 值为 1 μM。

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TCN238 Chemical Structure

TCN238 Chemical Structure

CAS No. : 125404-04-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥660
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1 mg ¥240
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5 mg ¥600
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10 mg ¥1050
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25 mg ¥2250
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50 mg ¥3900
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100 mg ¥6800
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500 mg   询价  

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Top Publications Citing Use of Products
  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

TCN238 is an orally bioavailable mGlu4 receptor positive allosteric modulator (PAM) with an EC50 of 1 μM[1].

IC50 & Target[1]

mGlu4 Receptor

1 μM (EC50)

体外研究
(In Vitro)

In the rat mGlu4 PAM in vitro assay the EC50 of TCN238 (Compound 11) is 1 μM which is comparable to the human assay. TCN238 is screened in rat and human mGlu5 assays, the IC50 of 11 is >30 μM on human mGlu5and >10 μM on rat mGlu5. TCN238 is run in a receptor screening panel of 68 targets and no activity is observed at ≥50% at 10 μM for any of the receptors. In CaCo-2 cells, TCN238 is found to have good permeability with no apparent efflux issue[1].

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

体内研究
(In Vivo)

TCN238 is highly CNS penetrant with a concentration of 33.8 μM in the brain. The plasma protein binding in rats is measured as 90% bound. The metabolic stability of TCN238 is assessed in rat and human microsomes and found to be 62% and 83% hepatic blood flow. The limited stability translated into a high in vivo clearance in rats of 75 mL/min/kg and TCN238 has a moderate volume of distribution (2.7 L/kg) with a short mean residence time (0.6 h) when dosed at 2 mg/kg via intravenous injection. TCN238 is orally bioavailable and 30 min following administration of a30 mg/kg dose, the plasma concentration is found to be 11.6 μM[1]. TCN 238 does not affect the performance of the learned task. However, the expression level of GRM4 in the hippocampus is reliable down-regulated five days after treatment with TCN 238. In addition, the expression level of GABRA1, encoding GABAA α-subunit is downregulated five days after the treatment in the frontal cortex[2].

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

分子量

197.24

Formula

C12H11N3

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 150 mg/mL (760.49 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.0700 mL 25.3498 mL 50.6997 mL
5 mM 1.0140 mL 5.0700 mL 10.1399 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

  • 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

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
Animal Administration
[2]

Rats: TCN 238 is administered subcutaneously at a dose of 2 mg/kg (volume of 0.5 mL) four times in two days (morning and evening). Retrieval of the task is tested 30min after the first and third injections of TCN 238, and 5 days after the last injection of the substance. During the retrieval test the animals are placed to the start box, the door is opened, and the latent period of response is registered.[2].

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

参考文献

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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 5.0700 mL 25.3498 mL 50.6997 mL 126.7491 mL
5 mM 1.0140 mL 5.0700 mL 10.1399 mL 25.3498 mL
10 mM 0.5070 mL 2.5350 mL 5.0700 mL 12.6749 mL
15 mM 0.3380 mL 1.6900 mL 3.3800 mL 8.4499 mL
20 mM 0.2535 mL 1.2675 mL 2.5350 mL 6.3375 mL
25 mM 0.2028 mL 1.0140 mL 2.0280 mL 5.0700 mL
30 mM 0.1690 mL 0.8450 mL 1.6900 mL 4.2250 mL
40 mM 0.1267 mL 0.6337 mL 1.2675 mL 3.1687 mL
50 mM 0.1014 mL 0.5070 mL 1.0140 mL 2.5350 mL
60 mM 0.0845 mL 0.4225 mL 0.8450 mL 2.1125 mL
80 mM 0.0634 mL 0.3169 mL 0.6337 mL 1.5844 mL
100 mM 0.0507 mL 0.2535 mL 0.5070 mL 1.2675 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.

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产品名称:
TCN238
目录号:
HY-14419
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