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Vabicaserin hydrochloride

产品编号 T13275 CAS 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。

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Vabicaserin hydrochloride Chemical Structure

Vabicaserin hydrochloride, CAS 887258-94-8

规格	价格/CNY	货期
1 mg	￥ 1,260	现货
5 mg	￥ 3,110	现货
10 mg	￥ 4,570	现货
25 mg	￥ 7,260	现货
50 mg	￥ 9,790	现货
100 mg	￥ 13,200	现货
500 mg	￥ 26,300	现货
1 mL * 10 mM (in DMSO)	￥ 3,230	现货

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选择批次

纯度: 98.42%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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
分子量	264.79
分子式	C15H21ClN2
CAS No.	887258-94-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 75 mg/mL (283.24 mM), Sonication is recommended.

H2O: 4 mg/mL (15.11 mM), Sonication is recommended.

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO / H2O	1 mM	3.7766 mL	18.8829 mL	37.7658 mL	94.4144 mL
	5 mM	0.7553 mL	3.7766 mL	7.5532 mL	18.8829 mL
	10 mM	0.3777 mL	1.8883 mL	3.7766 mL	9.4414 mL
DMSO	20 mM	0.1888 mL	0.9441 mL	1.8883 mL	4.7207 mL
	50 mM	0.0755 mL	0.3777 mL	0.7553 mL	1.8883 mL
	100 mM	0.0378 mL	0.1888 mL	0.3777 mL	0.9441 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

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. 2. Tong Z, et al. Species differences in the formation of Vabicaserin carbamoyl glucuronide. Drug Metab Dispos. 2010 Apr;38(4):581-90.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：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

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Vabicaserin hydrochloride 887258-94-8 GPCR/G Protein Neuroscience 5-HT Receptor SCA136 inhibit 5-hydroxytryptamine Receptor Vabicaserin Inhibitor SCA 136 Vabicaserin Hydrochloride Serotonin Receptor SCA-136 inhibitor

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Vabicaserin hydrochloride

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords