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SSD114 HCl

产品编号 T4522 CAS 2319790-02-6

SSD114 is a novel GABAB receptor positive allosteric modulator.

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SSD114 HCl, CAS 2319790-02-6

规格	价格/CNY	货期
1 mg	￥ 673	现货
2 mg	￥ 987	现货
5 mg	￥ 1,660	现货
10 mg	￥ 2,490	现货
25 mg	￥ 4,160	现货
50 mg	￥ 5,890	现货
100 mg	￥ 8,290	现货
1 mL * 10 mM (in DMSO)	￥ 1,390	现货

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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	SSD114 is a novel GABAB receptor positive allosteric modulator.
体外活性	In the presence of 10 μM GABA, SSD114 hydrochloride at 25 μM significantly increases (to approximately 170% above basal levels) the [35S]GTPγS stimulation induced by GABA alone. SSD114 hydrochloride (15 or 30 μM) induces a leftward shift of the GABA concentration-response curve with a slight concomitant increase of maximal GABA stimulation at the highest concentration. In the presence of both 15 and 30 μM SSD114 hydrochloride, the EC50 for GABA decreases by 2 and 2.5 fold, respectively, while the maximal stimulation (Emax) is potentiated only at the concentration of 30 μM, reaching 161±5.09% over the basal value [1].
体内活性	The onset of loss of righting reflex (LORR) is reduced by pretreatment with SSD114 hydrochloride [F(5,30)=4.55, P<0.005]. Post hoc analysis indicates that the onset of LORR is significantly lower in mouse groups pretreated with doses of SSD114 hydrochloride equal to or higher than 10 mg/kg than in vehicle-treated mice. The duration of LORR is increased by pretreatment with SSD114 hydrochloride [F(5,30)=4.81, P<0.005]. Post hoc analysis indicates that the duration of LORR is significantly longer in mouse groups pretreated with 10 and 100 mg/kg SSD114 hydrochloride than in vehicle-treated mice [1].
细胞实验	Cells are transfected and seeded into 96-well microplates. 24 h after transfection, cells are washed twice with PBS and incubated in the presence or absence of SSD114 hydrochloride (different concentrations) for 15 min before substrate addition in a 96-well microplate. The Bioluminescence resonance energy transfer (BRET) ratio is calculated as the emission of YFP (530 to 570 nm) over the emission of RLuc (370 to 470 nm). The curves are fitted using Graph Pad Prism 5.0. The amplitude-weighted mean time constant is obtained by fitting the BRET recovery phase to a double exponential function [1].
动物实验	Male Sprague-Dawley rats and DBA mice, weighing 200 to 250 and 20 to 25 g, respectively, are used. On the test day, mice are divided into six groups (n=6 each) matched by body weight. Mice are treated acutely and intraperitoneally with 0, 1, 3, 10, 30, and 100 mg/kg SSD114 hydrochloride and sedation/hypnosis are measured. Specifically, after baclofen injection, each mouse is placed on its back once every 60 s until it is unable to right itself within 60 s. The time between baclofen injection and the start of the 60-s interval during which the mouse is unable to right itself is measured at the onset of loss of righting reflex (LORR). Each mouse is then left undisturbed on its back until it spontaneously regained its righting reflex (determined as having at least three paws under its body). Complete recovery of the righting reflex is defined as the mouse being able to turn itself upright twice more within 60 s. If this criterion is not fulfilled, the mouse is left undisturbed until it spontaneously regained its righting reflex. The time between loss and recovery of the righting reflex is monitored in each mouse and defined as the duration of LORR. Observations are conducted by an operator unaware of the drug treatment [1].

分子量	387.83
分子式	C18H21ClF3N3O
CAS No.	2319790-02-6

存储

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

溶解度

DMSO: 45 mg/mL (116.03 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5784 mL	12.8922 mL	25.7845 mL	64.4612 mL
	5 mM	0.5157 mL	2.5784 mL	5.1569 mL	12.8922 mL
	10 mM	0.2578 mL	1.2892 mL	2.5784 mL	6.4461 mL
	20 mM	0.1289 mL	0.6446 mL	1.2892 mL	3.2231 mL
	50 mM	0.0516 mL	0.2578 mL	0.5157 mL	1.2892 mL
	100 mM	0.0258 mL	0.1289 mL	0.2578 mL	0.6446 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)

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质量

配液浓度

参考文献

1. Porcu A, et al. In vitro and in vivo pharmacological characterization of SSD114, a novel GABAB positive allosteric modulator. Eur J Pharmacol. 2016 Nov 15;791:115-123.

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

SSD114 HCl 2319790-02-6 Membrane transporter/Ion channel Neuroscience GABA Receptor SSD-114 hydrochloride SSD114 Hydrochloride SSD-114 Hydrochloride SSD 114 Hydrochloride Inhibitor inhibitor inhibit

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SSD114 HCl

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