Carabersat (Synonyms: 卡拉博沙; SB-204269)

目录号: HY-U00307 纯度: 98.22%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Carabersat 是一种有效的抗惊厥剂。

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Carabersat Chemical Structure

CAS No. : 184653-84-7

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规格	价格	是否有货
5 mg	￥1800	In-stock
10 mg	￥2900	In-stock
25 mg	￥5800	In-stock
50 mg	现货	询价
100 mg		询价
200 mg		询价

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Carabersat is a potent anticonvulsant agent.

体外研究
(In Vitro)

[³H]Carabersat ([³H]SB 204269) binds to rat forebrain membranes with moderate affinity (K_d 40 nM) and pK_i values of 7.3^[1]. Carabersat is able to bind to mouse forebrain membranes, and the binding is saturable and stereospecific, with a K_d of 53 nM. The labelled [³H]Carabersat produces a K_d of 32 nM^[2]. Carabersat (SB-204269, 1-100 μM) has no effect on Na⁺ current in cultured hippocampal neurones. Carabersat also shows no effect on action potential discharges evoked by elevating external K⁺^[3]. Carabersat (SB-204269) is structurally-related to the benzopyran ATP-sensitive potassium channel (KATP) opener, cromakalim, but has opposite stereochemistry, and the mechanism of action of Carabersat is not thought to involve KATP^[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Carabersat (5b) significantly elevates anticonvulsant activity in mice^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

357.38

Formula

C₂₀H₂₀FNO₄

CAS 号

184653-84-7

性状

固体

颜色

White to off-white

中文名称

卡拉博沙

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 200 mg/mL (559.63 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7981 mL	13.9907 mL	27.9814 mL
5 mM	0.5596 mL	2.7981 mL	5.5963 mL
10 mM	0.2798 mL	1.3991 mL	2.7981 mL

查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (13.99 mM); 澄清溶液

此方案可获得 ≥ 5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 98.22%

选择批次：

Data Sheet (617 KB) SDS (251 KB)

COA (197 KB) HNMR (208 KB) RP-HPLC (114 KB) LCMS (117 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Wai N. Chan, et al. Synthesis of Novel trans-4-(Substituted-benzamido)-3,4-dihydro-2H-benzo[b]pyran-3-ol Derivatives as Potential Anticonvulsant Agents with a Distinctive Binding Profile. J. Med. Chem., 1996, 39 (23), pp 4537-4539.

[2]. Herdon H, et al. The novel anticonvulsant SB 204269 binds to a stereospecific site in the mouse brain. Eur J Pharmacol. 1996 Oct 31;314(3):R7-8. [Content Brief]

[3]. Caeser M, et al. Lack of effect of the novel anticonvulsant SB-204269 on voltage-dependent currents in neurones cultured from rat hippocampus. Neurosci Lett. 1999 Aug 13;271(1):57-60. [Content Brief]

[4]. Crespi F, et al. SB-204269 SmithKline Beecham. IDrugs. 1998 Sep;1(5):595-8. [Content Brief]

Animal Administration ^[1]	Mice^[1] In this model, groups of 10-20 naive mice (25-30 g) are assessed for production of a tonic hindlimb extension seizure following a single corneal electroshock using an "up and down" method of shock titration. The effects of drug treatment are expressed as a percentage change from vehicle control values and statistical comparisons between groups are made. Carabersat is administered orally as a fine suspension in 1% methylcellulose one hour before electroshock application^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Wai N. Chan, et al. Synthesis of Novel trans-4-(Substituted-benzamido)-3,4-dihydro-2H-benzo[b]pyran-3-ol Derivatives as Potential Anticonvulsant Agents with a Distinctive Binding Profile. J. Med. Chem., 1996, 39 (23), pp 4537-4539. [2]. Herdon H, et al. The novel anticonvulsant SB 204269 binds to a stereospecific site in the mouse brain. Eur J Pharmacol. 1996 Oct 31;314(3):R7-8. [Content Brief] [3]. Caeser M, et al. Lack of effect of the novel anticonvulsant SB-204269 on voltage-dependent currents in neurones cultured from rat hippocampus. Neurosci Lett. 1999 Aug 13;271(1):57-60. [Content Brief] [4]. Crespi F, et al. SB-204269 SmithKline Beecham. IDrugs. 1998 Sep;1(5):595-8. [Content Brief]

Animal Administration
^[1]

Mice^[1]
In this model, groups of 10-20 naive mice (25-30 g) are assessed for production of a tonic hindlimb extension seizure following a single corneal electroshock using an "up and down" method of shock titration. The effects of drug treatment are expressed as a percentage change from vehicle control values and statistical comparisons between groups are made. Carabersat is administered orally as a fine suspension in 1% methylcellulose one hour before electroshock application^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[1]. Wai N. Chan, et al. Synthesis of Novel trans-4-(Substituted-benzamido)-3,4-dihydro-2H-benzo[b]pyran-3-ol Derivatives as Potential Anticonvulsant Agents with a Distinctive Binding Profile. J. Med. Chem., 1996, 39 (23), pp 4537-4539.

[2]. Herdon H, et al. The novel anticonvulsant SB 204269 binds to a stereospecific site in the mouse brain. Eur J Pharmacol. 1996 Oct 31;314(3):R7-8. [Content Brief]

[3]. Caeser M, et al. Lack of effect of the novel anticonvulsant SB-204269 on voltage-dependent currents in neurones cultured from rat hippocampus. Neurosci Lett. 1999 Aug 13;271(1):57-60. [Content Brief]

[4]. Crespi F, et al. SB-204269 SmithKline Beecham. IDrugs. 1998 Sep;1(5):595-8. [Content Brief]

Carabersat 相关分类

Neurological Disease

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.7981 mL	13.9907 mL	27.9814 mL	69.9535 mL
	5 mM	0.5596 mL	2.7981 mL	5.5963 mL	13.9907 mL
	10 mM	0.2798 mL	1.3991 mL	2.7981 mL	6.9954 mL
	15 mM	0.1865 mL	0.9327 mL	1.8654 mL	4.6636 mL
	20 mM	0.1399 mL	0.6995 mL	1.3991 mL	3.4977 mL
	25 mM	0.1119 mL	0.5596 mL	1.1193 mL	2.7981 mL
	30 mM	0.0933 mL	0.4664 mL	0.9327 mL	2.3318 mL
	40 mM	0.0700 mL	0.3498 mL	0.6995 mL	1.7488 mL
	50 mM	0.0560 mL	0.2798 mL	0.5596 mL	1.3991 mL
	60 mM	0.0466 mL	0.2332 mL	0.4664 mL	1.1659 mL
	80 mM	0.0350 mL	0.1749 mL	0.3498 mL	0.8744 mL
	100 mM	0.0280 mL	0.1399 mL	0.2798 mL	0.6995 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Carabersat184653-84-7SB-204269卡拉博沙SB204269SB 204269OthersInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

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上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

Carabersat (Synonyms: 卡拉博沙; SB-204269)