Baclofen

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Baclofen

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

1134-47-0

包装与价格：

包装	价格(元)
500mg	电议
1 g	电议
5 g	电议
10 g	电议
50 g	电议

产品名称

巴氯芬

产品介绍

Baclofen 是 γ-氨基丁酸 (GABA) 的亲脂性衍生物，是一种口服有效，选择性的代谢型 GABA_B受体 (GABA_BR) 激动剂。Baclofen 可以模拟 GABA 的作用并通过 GABA_B受体产生缓慢的突触前抑制。Baclofen 具有高的血脑屏障透过率。Baclofen 有用于肌肉痉挛研究的潜力。

生物活性

Baclofen, a lipophilic derivative of γ-aminobutyric acid (GABA), is an orally active, selective metabotropicGABA_Breceptor (GABA_BR)agonist. Baclofen mimics the action of GABA and produces slow presynaptic inhibition through the GABA_Breceptor. Baclofen has high blood brain barrier penetrance. Baclofen has the potential for muscle spasticity research^[1]^[2]^[3].

体外研究
(In Vitro)

Baclofen (1, 10 μM; 24 h) causes markedly decreased lactate dehydrogenase (LDH) activity, indicating increased cell viability in wild-type or mutant huntingtin-expressing striatal cells (HD19 or HD43). Baclofen significantly increases chymotrypsin-like proteasome activity and cell viability were in the HD43 cells^[3].

体内研究
(In Vivo)

Baclofen (i.p.; 10 μg/g; twice daily for 3 consecutive days) ameliorates motor deficits in YAC128 HD transgenic mice^[3].

Animal Model:	Wild type (WT) and mutant (MT) male YAC128 mice at 13-18 months of age^[3]
Dosage:	10 μg/g
Administration:	IP; twice daily at 9:00 a.m. and 5:00 p.m., for 3 consecutive days; then single dose on the fourth day at 9:00 a.m
Result:	Ameliorated motor deficits in YAC128 HD transgenic mice. Increased proteasome activity and reduces neuronal intranuclear inclusions (NIIs) in YAC128 HD transgenic mice.

Clinical Trial

分子量

213.66

性状

Solid

Formula

C₁₀H₁₂ClNO₂

CAS 号

1134-47-0

中文名称

巴氯芬；氯苯氨丁酸

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

H₂O : 2 mg/mL(9.36 mM;Need ultrasonic)

DMSO :< 1 mg/mL(insoluble or slightly soluble)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	4.6803 mL	23.4017 mL	46.8033 mL
5 mM	0.9361 mL	4.6803 mL	9.3607 mL
10 mM	---	---	---

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

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

1.
请依序添加每种溶剂： PBS
Solubility: 2.5 mg/mL (11.70 mM); Clear solution; Need ultrasonic and warming and heat to 60℃

*以上所有助溶剂都可在本网站选购。