同义名 :	ABR-215062; LAQ; TV-5600; SAIK-MS
	CAS号 :	248281-84-7
	货号 :	A216404
	分子式 :	C19H17ClN2O3
	纯度 :	98%
	分子量 :	356.8
	MDL号 :	MFCD08689859
	存储条件：	Pure form Sealed in dry, room temperature In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

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].

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NCT01404117	Relapsing Multiple Sclerosis	Phase 2	Withdrawn(Study is being redes...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	-	-

实验方案
	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

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