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Laquinimod
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。
Laquinimod图片
CAS NO:248281-84-7

拉喹莫德
ABR-215062
Laquinimod (ABR-215062) 是一种可口服的羧酰胺衍生物,是一种有效的免疫调节剂,可防止中枢神经系统的神经变性和炎症。Laquinimod 减少星形胶质细胞NF-κB的活化以防止铜酮 (Cuprizone) 诱导的脱髓鞘。Laquinimod 具有用于多发性硬化症 (MS;RRMS 或 CPMS) 的复发缓解 (RR) 和慢性进行性 (CP) 形式以及神经退行性疾病研究的潜力。
生物活性

Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocyticNF-κBactivation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research[1][2][3][4].

IC50& Target[3]

NF-κB

 

体外研究
(In Vitro)

Laquinimod reverses EAE and inhibits pathogenic T cell immune responses. Laquinimod reverses RR-EAE and inhibits inflammatory T cell responses via a direct effect on myeloid APC. Laquinimod alters myeloid APC subsets and inhibits Th1 and Th17 polarization of myelin-specific T cells. Laquinimod-induced type II (M2) monocytes reverse established EAE[1]. Laquinimod modulates the phenotype of B cells of healthy donors. Laquinimod modulates expression of markers related to regulatory capacity in B cells of RRMS patients. Laquinimod reduces IFNγ cytokine expression in CD4+T cells[2].

体内研究
(In Vivo)

Laquinimod treatment inhibits donor myelin-specific T cells from transferring EAE to naive recipient mice. In vivo laquinimod treatment alters subpopulations of myeloid antigen presenting cells (APC) that include a decrease in CD11c+CD11b+CD4+ dendritic cells (DC) and an elevation of CD11bhiGr1himonocytes[1].

Clinical Trial
分子量

356.80

性状

Solid

Formula

C19H17ClN2O3

CAS 号

248281-84-7

中文名称

拉喹莫德

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL(70.07 mM;ultrasonic and warming and heat to 60℃)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.8027 mL14.0135 mL28.0269 mL
5 mM0.5605 mL2.8027 mL5.6054 mL
10 mM0.2803 mL1.4013 mL2.8027 mL
*

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: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (7.01 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.01 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。
 
 
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