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Laquinimod/拉喹莫德 {[allProObj[0].p_purity_real_show]}

货号:A216404 同义名: ABR-215062; LAQ

Laquinimod is an orally administered neuroimmunomodulator initially developed for the treatment of multiple sclerosis.

Laquinimod/拉喹莫德 化学结构 CAS号:248281-84-7
Laquinimod/拉喹莫德 化学结构
CAS号:248281-84-7
Laquinimod/拉喹莫德 3D分子结构
CAS号:248281-84-7
Laquinimod/拉喹莫德 化学结构 CAS号:248281-84-7
Laquinimod/拉喹莫德 3D分子结构 CAS号:248281-84-7
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Laquinimod/拉喹莫德 纯度/质量文件 产品仅供科研

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Laquinimod/拉喹莫德 生物活性

描述 Laquinimod is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. In vivo laquinimod treatment inhibited donor myelin-specific T cells from transferring EAE (experimental autoimmune encephalomyelitis) to naive recipient mice. In vivo laquinimod treatment altered subpopulations of myeloid antigen presenting cells (APC) that included a decrease in CD11c(+)CD11b(+)CD4(+) dendritic cells (DC) and an elevation of CD11b(hi)Gr1(hi) monocytes[3]. Topical administration of laquinimod to the injured corneas dramatically inhibited alkali-induced corneal neovascularization and decreased inflammatory cell (such as macrophage) infiltration in a corneal injury mouse model. Laquinimod significantly downregulated the expression of chemokines (monocyte chemotactic protein-1 and macrophage inflammatory protein-1), pro-inflammatory cytokines (interleukin-1β and tumor necrosis factor-alpha), vascular endothelial growth factor, nucleotide-binding oligomerization domain-like receptor family pyrin domain-containing 3 and apoptosis-associated speck-like protein containing C-terminal caspase-recruitment domain adaptor protein in both injured corneas and RAW cells. In vitro, laquinimod also dramatically inhibited the proliferation, migration and tube formation of human umbilical vein endothelial cells[4]. Laquinimod had a significant protective impact against MPP+-induced neurotoxicity. Laquinimod prevented MPP+-induced reduction of cell proliferation, the release of lactate dehydrogenase (LDH), and apoptosis[5]. Laquinimod protects against glutamate excitotoxicity of the cerebellum of EAE mice by bursting the expression of glial glutamate transporters, independently of its anti-inflammatory effects[6].

Laquinimod/拉喹莫德 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01404117 Relapsing Multiple Sclerosis Phase 2 Withdrawn(Study is being redes... 展开 >>igned) 收起 << January 2014 -
NCT00605215 Multiple Sclerosis Phase 3 Completed - -
NCT01707992 Multiple Sclerosis Phase 3 Completed - -

Laquinimod/拉喹莫德 参考文献

[1]Yang JS, Xu LY, et al. Laquinimod (ABR-215062) suppresses the development of experimental autoimmune encephalomyelitis, modulates the Th1/Th2 balance and induces the Th3 cytokine TGF-beta in Lewis rats. J Neuroimmunol. 2004 Nov;156(1-2):3-9.

[2]Zou LP, Abbas N, et al. Suppression of experimental autoimmune neuritis by ABR-215062 is associated with altered Th1/Th2 balance and inhibited migration of inflammatory cells into the peripheral nerve tissue. Neuropharmacology. 2002 Apr;42(5):731-9.

[3]Schulze-Topphoff U, Shetty A, Varrin-Doyer M, Molnarfi N, Sagan SA, Sobel RA, Nelson PA, Zamvil SS. Laquinimod, a quinoline-3-carboxamide, induces type II myeloid cells that modulate central nervous system autoimmunity. PLoS One. 2012;7(3):e33797

[4]Li Z, Chen J, Lei L, Jiang N, Zhu Y, Jia Y, Zhuo Y, Su W. Laquinimod Inhibits Inflammation-Induced Angiogenesis in the Cornea. Front Med (Lausanne). 2020 Nov 10;7:598056

[5]Zhang X, Jin J, Xie A. Laquinimod inhibits MMP+ induced NLRP3 inflammasome activation in human neuronal cells. Immunopharmacol Immunotoxicol. 2020 Jun;42(3):264-271

[6]Gentile A, Musella A, De Vito F, Fresegna D, Bullitta S, Rizzo FR, Centonze D, Mandolesi G. Laquinimod ameliorates excitotoxic damage by regulating glutamate re-uptake. J Neuroinflammation. 2018 Jan 5;15(1):5

Laquinimod/拉喹莫德 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.80mL

0.56mL

0.28mL

14.01mL

2.80mL

1.40mL

28.03mL

5.61mL

2.80mL

Laquinimod/拉喹莫德 技术信息

CAS号248281-84-7
分子式C19H17ClN2O3
分子量 356.8
SMILES Code C1=CC=C(Cl)C2=C1N(C(=C(C2=O)C(=O)N(CC)C3=CC=CC=C3)O)C
MDL No. MFCD08689859
别名 ABR-215062; LAQ; TV-5600; SAIK-MS
运输蓝冰
InChI Key GKWPCEFFIHSJOE-UHFFFAOYSA-N
Pubchem ID 54677946
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, room temperature

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的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
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