A2764 2HCl
产品说明书
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同义名 : | A2764 (hydrochloride); A2764 dihydrochloride |
| CAS号 : | 861038-72-4 | |
| 货号 : | A1219196 | |
| 分子式 : | C15H21Cl3N2O | |
| 纯度 : | 99%+ | |
| 分子量 : | 351.7 | |
| MDL号 : | MFCD32667019 | |
| 存储条件： |
Pure form Sealed in dry,2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 描述 | A2764 2HCl is a highly selective inhibitor of TRESK (TWIK-related spinal cord K+ channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception. The degree of inhibition by 100 µM A2764 (77.8% ± 3.5%, n = 6) was larger in the activated state of TRESK (i.e., after calcineurin-dependent stimulation) than in the resting state of the channel (42.8% ± 11.5% inhibition, n = 7). A2764 (100 µM) shows an improved inhibitory potency for activated channel. The subsequent application of A2764 strongly inhibits the current (77.8±3.5%)[1]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.84mL 0.57mL 0.28mL |
14.22mL 2.84mL 1.42mL |
28.43mL 5.69mL 2.84mL |
| 参考文献 |
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