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Vabicaserin HCl {[allProObj[0].p_purity_real_show]}

货号:A1005250 同义名: SCA 136;Vabicaserin hydrochloride

Vabicaserin HCl是一种选择性的 5-HT2C 受体激动剂,EC50 为 8 nM。

Vabicaserin HCl 化学结构 CAS号:887258-94-8
Vabicaserin HCl 化学结构
CAS号:887258-94-8
Vabicaserin HCl 3D分子结构
CAS号:887258-94-8
Vabicaserin HCl 化学结构 CAS号:887258-94-8
Vabicaserin HCl 3D分子结构 CAS号:887258-94-8
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Vabicaserin HCl 纯度/质量文件 产品仅供科研

货号:A1005250 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 5-HT 5-HT1 5-HT2 5-HT3 5-HT5 5-HT6 5-HT7 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

98%
Venlafaxine 98%
Fluvoxamine maleate 99%
Iloperidone 98%
Ziprasidone HCl 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

98%
Dapoxetine HCl 97%
Trazodone 98+%
Clomipramine HCl 98%
Mirtazapine 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

97%
Duloxetine 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
Latrepirdine 2HCl GluR 98%
Fluoxetine HCl 99.5%
Paroxetine hydrochloride AChR 97%
BMY 7378 ++

5-HT1D, pIC50: 5.9

5-HT1A, pIC50: 6.4

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

98%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

98% HPLC
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

99+%
Olanzapine 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Rat), Ki: 50 nM

5-HT2C (Human), Ki: 2.5 nM

99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

99%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

99%+
Sarpogrelate HCl ++++

5-HT2C, Kd: 1.1 nM

5-HT2A, Kd: 2.1 nM

98%
Tropisetron 99%
Palonosetron 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

98%
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron hydrochloride dihydrate 98%
VUF10166 ++++

5-HT3AB, Ki: 22 nM

5-HT3A, Ki: 0.04 nM

99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

98%
Asenapine maleate +++

5-HT1A, pKi: 8.6

5-HT1B, pKi: 8.4

++++

5-HT2C, pKi: 10.46

5-HT2A, pKi: 9.75

+++

5-HT5A, pKi: 8.84

++++

5-HT6, pKi: 9.6

++++

5-HT7, pKi: 9.94

97%
Risperidone ++

5-HT1D, Ki: 84.6 nM

5-HT1B, Ki: 14.9 nM

++++

5-HT2A, Ki: 61.9 nM

5-HT2C, Ki: 12 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

99%+
Intepirdine ++++

5-HT6, pKi: 9.63

99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

98+%
BRL 15572 ++

5-HT1B, pKi: 6.1

5-HT1D, pKi: 6

++

5-HT2B, pKi: 6.2

5-HT2A, pKi: 6.6

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Vabicaserin HCl 生物活性

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] .

Vabicaserin HCl 参考文献

[1]Dunlop J, et al. Characterization of Vabicaserin (SCA-136), a selective 5-hydroxytryptamine 2C receptor agonist. J Pharmacol Exp Ther. 2011 Jun;337(3):673-80.

Vabicaserin HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.78mL

0.76mL

0.38mL

18.88mL

3.78mL

1.89mL

37.77mL

7.55mL

3.78mL

Vabicaserin HCl 技术信息

CAS号887258-94-8
分子式C15H21ClN2
分子量 264.794
别名 SCA 136;Vabicaserin hydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

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

动物实验配方
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