Guvacine hydrochloride (Synonyms: 去甲槟榔次碱)

目录号: HY-100809 纯度: 99.73%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Guvacine hydrochloride 是从槟榔中得到的生物碱，为 GABA transporter 的抑制剂，对几种克隆的 GABA 转运体具有适度的选择性，IC₅₀ 值分别为 14 μM (human GAT-1)，39 μM (rat GAT-1)，58 μM (rat GAT-2)，119 μM (human GAT-3)，378 μM (rat GAT-3) 和 1870 μM (human BGT-3)。

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Guvacine hydrochloride Chemical Structure

CAS No. : 6027-91-4

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规格	价格	是否有货
10 mM * 1 mL in Water	￥660	In-stock
5 mg	￥600	In-stock
10 mg	￥800	In-stock
50 mg		询价
100 mg		询价

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Customer Review

Other Forms of Guvacine hydrochloride:

Guvacine 询价
Guvacine hydrobromide 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

Guvacine hydrochloride is an alkaloid from the nut of Areca catechu, acts as an inhibitor of GABA transporter, and dispalys modest selectivity for cloned GABA transporters with IC₅₀s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3).

IC₅₀ & Target

IC50: 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), 1870 μM (human BGT-3)^[1]

体外研究
(In Vitro)

Guvacine hydrochloride is a potent inhibitor of GABA transporter, dispalys modest selectivity for cloned GABA transporters with IC₅₀s of 14 μM (human GAT-1), 39 μM (rat GAT-1), 58 μM (rat GAT-2), 119 μM (human GAT-3), 378 μM (rat GAT-3), and 1870 μM (human BGT-3). Guvacine has low affinity at hBGT-1 (IC₅₀ >1 mM)^[1]. Guvacine hydrochloride is a potent inhibitor of GABA uptake, but does not inhibit sodium-independent GABA binding, and is weak or inactive as a GABA receptor agonist^[2]. Guvacine inhibits the uptake GABA and β-alanine with IC₅₀s of 23 ± 2 μM, 66 ± 11 μM in the Cat spinal cord, and 8 ± 1 μM, 123 ± 28 μM in the rat cerebral cortex, respectively^[3].

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

分子量

163.60

Formula

C₆H₁₀ClNO₂

CAS 号

6027-91-4

性状

固体

颜色

White to off-white

中文名称

去甲槟榔次碱盐酸盐；四氢烟酸盐酸盐；盐酸去甲槟榔次碱；盐酸四氢烟酸

结构分类

初始来源

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

细胞实验：

H₂O 中的溶解度 : 41.67 mg/mL (254.71 mM; 超声助溶)

DMSO 中的溶解度 : 10 mg/mL (61.12 mM; 超声助溶 (<60°C); 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	6.1125 mL	30.5623 mL	61.1247 mL
5 mM	1.2225 mL	6.1125 mL	12.2249 mL
10 mM	0.6112 mL	3.0562 mL	6.1125 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 (sealed storage, away from moisture)。-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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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：

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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： PBS
Solubility: 25 mg/mL (152.81 mM); 澄清溶液; 超声助溶

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

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

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

纯度 & 产品资料

纯度: 99.73%

选择批次：

Data Sheet (617 KB) SDS (393 KB)

COA (264 KB) HNMR (205 KB) LCMS (115 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Borden LA, et al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994 Oct 14;269(2):219-24. [Content Brief]

[2]. Krogsgaard-Larsen P, et al. Structure-activity studies on the inhibition of GABA binding to rat brain membranes by muscimol and related compounds. J Neurochem. 1978 Jun;30(6):1377-82. [Content Brief]

[3]. Lodge D, et al. Effects of the Areca nut constituents arecaidine and guvacine on the action of GABA in the cat central nervous system. Brain Res. 1977 Nov 18;136(3):513-22. [Content Brief]

Cell Assay ^[1]	Cells grown in 24-well plates are washed 3 × with Hepes-buffered saline (HBS, in mM: NaC1, 150; Hepes, 20; CaCl₂, 1; glucose, 10; KC1, 5; MgCl₂, 1; pH 7.4) and allowed to equilibrate on a 37°C slide warmer. After 10 min the medium is removed and unlabeled drugs (Guvacine , etc.) in HBS are added (450 μL/well). Transport is initiated by adding 50 μL per well of a concentrated solution of [³H]GABA in HBS (final concentration = 50 nM). Non-specific uptake is defined in parallel wells with 1 mM unlabeled GABA, and is subtracted from total uptake to yield specific uptake; all data represent specific uptake. Plates are incubated at 37°C for 10 min, then washed rapidly 3 × with ice-cold HBS, using a 24-position plate washer. Cells are solubilized with 0.05% sodium deoxycholate/0.1 N NaOH (0.25 mL/well), an aliquot neutralized with 1 N HC1, and radioactivity is determined by scintillation counting. Protein is quantified in an aliquot of the solubilized cells using a BIO-RAD protein assay kit^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Borden LA, et al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994 Oct 14;269(2):219-24. [Content Brief] [2]. Krogsgaard-Larsen P, et al. Structure-activity studies on the inhibition of GABA binding to rat brain membranes by muscimol and related compounds. J Neurochem. 1978 Jun;30(6):1377-82. [Content Brief] [3]. Lodge D, et al. Effects of the Areca nut constituents arecaidine and guvacine on the action of GABA in the cat central nervous system. Brain Res. 1977 Nov 18;136(3):513-22. [Content Brief]

Cell Assay
^[1]

Cells grown in 24-well plates are washed 3 × with Hepes-buffered saline (HBS, in mM: NaC1, 150; Hepes, 20; CaCl₂, 1; glucose, 10; KC1, 5; MgCl₂, 1; pH 7.4) and allowed to equilibrate on a 37°C slide warmer. After 10 min the medium is removed and unlabeled drugs (Guvacine , etc.) in HBS are added (450 μL/well). Transport is initiated by adding 50 μL per well of a concentrated solution of [³H]GABA in HBS (final concentration = 50 nM). Non-specific uptake is defined in parallel wells with 1 mM unlabeled GABA, and is subtracted from total uptake to yield specific uptake; all data represent specific uptake. Plates are incubated at 37°C for 10 min, then washed rapidly 3 × with ice-cold HBS, using a 24-position plate washer. Cells are solubilized with 0.05% sodium deoxycholate/0.1 N NaOH (0.25 mL/well), an aliquot neutralized with 1 N HC1, and radioactivity is determined by scintillation counting. Protein is quantified in an aliquot of the solubilized cells using a BIO-RAD protein assay kit^[1].

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

参考文献

[1]. Borden LA, et al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994 Oct 14;269(2):219-24. [Content Brief]

[2]. Krogsgaard-Larsen P, et al. Structure-activity studies on the inhibition of GABA binding to rat brain membranes by muscimol and related compounds. J Neurochem. 1978 Jun;30(6):1377-82. [Content Brief]

[3]. Lodge D, et al. Effects of the Areca nut constituents arecaidine and guvacine on the action of GABA in the cat central nervous system. Brain Res. 1977 Nov 18;136(3):513-22. [Content Brief]

Guvacine hydrochloride 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 / H₂O	1 mM	6.1125 mL	30.5623 mL	61.1247 mL	152.8117 mL
	5 mM	1.2225 mL	6.1125 mL	12.2249 mL	30.5623 mL
	10 mM	0.6112 mL	3.0562 mL	6.1125 mL	15.2812 mL
	15 mM	0.4075 mL	2.0375 mL	4.0750 mL	10.1874 mL
	20 mM	0.3056 mL	1.5281 mL	3.0562 mL	7.6406 mL
	25 mM	0.2445 mL	1.2225 mL	2.4450 mL	6.1125 mL
	30 mM	0.2037 mL	1.0187 mL	2.0375 mL	5.0937 mL
	40 mM	0.1528 mL	0.7641 mL	1.5281 mL	3.8203 mL
	50 mM	0.1222 mL	0.6112 mL	1.2225 mL	3.0562 mL
	60 mM	0.1019 mL	0.5094 mL	1.0187 mL	2.5469 mL
H₂O	80 mM	0.0764 mL	0.3820 mL	0.7641 mL	1.9101 mL
H₂O	100 mM	0.0611 mL	0.3056 mL	0.6112 mL	1.5281 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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:

Guvacine6027-91-4去甲槟榔次碱盐酸盐四氢烟酸盐酸盐盐酸去甲槟榔次碱盐酸四氢烟酸GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorInhibitorinhibitorinhibit

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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。

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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）

Guvacine hydrochloride (Synonyms: 去甲槟榔次碱)

Customer Review

Other Forms of Guvacine hydrochloride: