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Vabicaserin hydrochloride

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产品编号 T13275Cas号 887258-94-8
别名 SCA 136

Vabicaserin hydrochloride (SCA 136) 是一种选择性的 5-羟色胺2C 受体激动剂,EC50为 8 nM。

Vabicaserin hydrochloride
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Vabicaserin hydrochloride

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纯度: 98.42%
产品编号 T13275 别名 SCA 136Cas号 887258-94-8

Vabicaserin hydrochloride (SCA 136) 是一种选择性的 5-羟色胺2C 受体激动剂,EC50为 8 nM。

规格价格库存数量
1 mg
¥ 592
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5 mg
¥ 1,550
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10 mg
¥ 2,270
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25 mg
¥ 3,550
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50 mg
¥ 4,970
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100 mg
¥ 6,530
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200 mg
¥ 8,790
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1 mL x 10 mM (in DMSO)
¥ 1,720
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"Vabicaserin hydrochloride"的相关化合物库

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纯度:98.42%
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产品介绍

生物活性
产品描述
Vabicaserin hydrochloride (SCA 136) is a selective agonist of 5-hydroxytryptamine 2C (5-HT2C) receptor (EC50: 8 nM).
靶点活性
5-HT2C:8 nM (EC50)
体外活性
In Chinese hamster ovary cell membranes, Vabicaserin displaces 125I-(2,5-dimethoxy)phenylisopropylamine binding from human 5-HT2C receptor sites (Ki: 3 nM) and is >50-fold selective over a number of serotonergic, noradrenergic, and dopaminergic receptors. The binding affinity determined for the human 5-HT2B receptor subtype using [3H]5HT is 14 nM. Vabicaserin is a potent and full agonist (EC50, 8 nM; Emax, 100%) in stimulating 5-HT2C receptor-coupled calcium mobilization and exhibits 5-HT2A receptor antagonism and 5-HT2B antagonist or partial agonist activity in transfected cells, depending on the level of receptor expression. Vabicaserin showed a lower affinity at the binding site (22 nM) of 5-HT2C antagonist labeled with [3H]methsulamide. Other binding studies have shown that Vabicaserin has an affinity for 5-HT2B and 5-HT1A receptors with Ki values of 14 and 112 nM, respectively [1].
体内活性
The unchanged drug represents less than 19, 20, and 35% of total plasma radioactivity at all the time points examined in mice, rats, and dogs, respectively, after a single oral dose of [14C]Vabicaserin at 50, 5, and 15 mg/kg. The carbamoyl glucuronide (CG) represents approximately 7 to 36% of plasma radioactivity in mice and 2 to 28% of plasma radioactivity in dogs but is not detected in rat plasma after the single [14C]Vabicaserin dose. However, the CG is observed in rat plasma after multiple-dose administration of Vabicaserin at higher doses, and the CG is approximately 20 times less than Vabicaserin based on steady-state AUC0-24 values. The estimated plasma AUC0-24 ratios of CG to the parent drug are 1.5 and 1.7 in mice and dogs after the single [14C]Vabicaserin dose, respectively. The plasma AUC0-24 ratios for the CG to Vabicaserin at steady-state with doses used for safety assessment are less for mice (0.2-0.6) and slightly higher for dogs (1.8-4.0) compared with the single-dose values. The CG is detected in dog urine in similar amounts to the parent drug, although it is not detected in mouse or rat urine after the single [14C]Vabicaserin dose. Radioactivity in a 0- to 24-h bile collection from rats receiving a 5 mg/kg [14C]Vabicaserin dose accounts for 19 and 24% of the administered dose in males and females, respectively. Although the CG is not detected in the urine or feces of rats after a single oral administration, In male rats and 15% in female rats, it represents an average of up to 30% of biliary radioactivity. In monkeys after a single oral 25-mg/kg dose of Vabicaserin, the plasma concentrations of the CG exceeded those of Vabicaserin at all the time points (2-24 h) postdose, although the amount of CG relative to Vabicaserin decreased by 24 h postdose, with ratios of 17.5 at 2 h and 1.7 at 24 h.In monkeys, The CG to Vabicaserin AUC0-24 ratio of 12:1 indicates that the CG is a major metabolite [2].
别名SCA 136
化学信息
分子量264.79
分子式C15H21ClN2
CAS No.887258-94-8
SmilesCl.[H][C@@]12CCC[C@]1([H])c1cccc3CNCCN(C2)c13
密度no data available
储存&溶解度
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: 55 mg/mL (207.71 mM), Sonication is recommended.
H2O: 4 mg/mL (15.11 mM), Sonication is recommended.
溶液配制表
H2O/DMSO
1mg5mg10mg50mg
1 mM3.7766 mL18.8829 mL37.7658 mL188.8289 mL
5 mM0.7553 mL3.7766 mL7.5532 mL37.7658 mL
10 mM0.3777 mL1.8883 mL3.7766 mL18.8829 mL
DMSO
1mg5mg10mg50mg
20 mM0.1888 mL0.9441 mL1.8883 mL9.4414 mL
50 mM0.0755 mL0.3777 mL0.7553 mL3.7766 mL
100 mM0.0378 mL0.1888 mL0.3777 mL1.8883 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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