产品说明书
Vabicaserin HCl
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同义名 : | SCA 136;Vabicaserin hydrochloride |
| CAS号 : | 887258-94-8 | |
| 货号 : | A1005250 | |
| 分子式 : | C15H21ClN2 | |
| 纯度 : | 98+% | |
| 分子量 : | 264.794 | |
| MDL号 : | MFCD31706226 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 60 mg/mL(226.59 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 4 mg/mL(15.11 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
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| 描述 | Vabicaserin HCl can replace the binding of 125I-(2,5-dimethoxy)phenylisopropylamine at the human 5-HT2C receptor site on the CHO cell membrane, with a Ki value of 3 nM, and its selectivity exceeds some serotonergic, noradrenergic and 50 times more dopaminergic receptors. The binding affinity to the human 5-HT2B receptor subtype was determined to be 14 nM using [3H]5HT. Vabicaserin HCl is a potent full agonist (EC50, 8 nM; Emax, 100%) in stimulating 5-HT2C receptor-coupled calcium mobilization. Depending on the receptor expression level in transfected cells, it exhibits 5-HT2A receptor antagonism and 5-HT2B antagonism or partial agonistic activity. Vabicaserin exhibits lower affinity at the 5-HT2C antagonist binding site labeled with [3H]mesulergine (22 nM). Additional binding studies have shown that Vabicaserin has affinity for the 5-HT2B and 5-HT1A receptors with Ki values of 14 nM and 112 nM, respectively [1] . | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
3.78mL 0.76mL 0.38mL |
18.88mL 3.78mL 1.89mL |
37.77mL 7.55mL 3.78mL |
| 参考文献 |
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