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TCN238 是一种可口服的代谢型谷氨酸受体 4 正变构调节剂,EC50值为 1 μM。
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TCN238 是一种可口服的代谢型谷氨酸受体 4 正变构调节剂,EC50值为 1 μM。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 115 | 现货 | |
5 mg | ¥ 296 | 现货 | |
10 mg | ¥ 523 | 现货 | |
25 mg | ¥ 1,120 | 现货 | |
50 mg | ¥ 1,930 | 现货 | |
100 mg | ¥ 2,860 | 现货 | |
200 mg | ¥ 3,970 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 328 | 现货 |
产品描述 | TCN238 is an orally bioavailable positive allosteric modulator of the metabotropic glutamate receptor 4 (mGluR4with an EC50 of 1 μM). |
靶点活性 | mGlu4 receptor:1 μM (EC50) |
体外活性 | TCN238 has a greater than 30-fold selectivity for mGluR4 over mGluR5 using human recombinant receptors in CHO-K1 cells[1]. |
体内活性 | TCN238 has no activity at the adenosine A2A, serotonin 5-HT1A, or α2A-adrenergic receptors at concentrations up to 10 μM.?In a haloperidol-induced catalepsy rat model of Parkinson's disease, it dose-dependently reduces catalepsy with an ED50 of approximately 1 mg/kg.?TCN 238 administration in rats leads to downregulation of the mGluR4 gene, GRM4, in the hippocampus and the gene for the GABAA receptor α subunit, GABRA1, in the frontal cortex without affecting hippocampal-dependent memory[1]. |
别名 | TCN 238 |
分子量 | 197.24 |
分子式 | C12H11N3 |
CAS No. | 125404-04-8 |
Smiles | Nc1nccc(\C=C\c2ccccc2)n1 |
密度 | no data available |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 150 mg/mL (760.49 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
DMSO
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