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CAS No.: 248281-84-7

拉喹莫德 Catalog No. CSN10659

Synonyms: ABR-215062;LAQ;SAIK-MS

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

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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NCT01404117	Relapsing Multiple Sclerosis	Phase 2	Withdrawn(Study is being redes... more >>igned) Collapse <<	January 2014	-
NCT00605215	Multiple Sclerosis	Phase 3	Completed	-	-
NCT01707992	Multiple Sclerosis	Phase 3	Completed	-	-

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8027 mL
- 14.0133 mL
- 28.0267 mL
- 5 mM
- 0.5605 mL
- 2.8027 mL
- 5.6053 mL
- 10 mM
- 0.2803 mL
- 1.4013 mL
- 2.8027 mL

技术信息

CAS号

248281-84-7

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H17ClN2O3

运输

蓝冰

分子量

356.80

别名

ABR-215062;LAQ;SAIK-MS;TV-5600;拉喹莫德

溶解度

DMSO	59.0 mg/mL (165.4 mM)
Water	Insoluble
Ethanol	1.0 mg/mL (2.8 mM)

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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... more >>igned) Collapse <<	January 2014	-
NCT00605215	Multiple Sclerosis	Phase 3	Completed	-	-
NCT01707992	Multiple Sclerosis	Phase 3	Completed	-	-
NCT00349193	Relapsing Remitting Multiple S... more >>clerosis Collapse <<	Phase 2	Completed	-	-
NCT00745615	Relapsing Remitting Multiple S... more >>clerosis Collapse <<	Phase 2	Terminated(Sponsor terminated ... more >>RRMS studies as sufficient long term clinical data was collected for the study drug in the relevant dose.) Collapse <<	-	-
NCT01975298	Relapsing Remitting Multiple S... more >>clerosis Collapse <<	Phase 3	Withdrawn(Business Decision)	-	-
NCT00988052	Relapsing Multiple Sclerosis	Phase 3	Terminated(Sponsor terminated ... more >>RRMS studies as sufficient long term clinical data was collected for the study drug in the relevant dose.) Collapse <<	-	-
NCT01085097	Lupus Nephritis	Phase 2	Completed	-	-
NCT00737932	Crohn's Disease	Phase 2	Completed	-	-
NCT00509145	Multiple Sclerosis	Phase 3	Completed	-	-
NCT01085084	Lupus Arthritis	Phase 2	Completed	-	United States, Alabama ... more >> Teva Investigational Site 1363 Birmingham, Alabama, United States United States, California Teva Investigational Site 1359 Los Angeles, California, United States Teva Investigational Site 1352 San Francisco, California, United States Teva Investigational Site 1365 San Leandro, California, United States Teva Investigational Site 1368 West Hollywood, California, United States United States, Illinois Teva Investigational Site 1367 Chicago, Illinois, United States United States, Maryland Teva Investigational Site 1370 Baltimore, Maryland, United States Teva Investigational Site 1362 Cumberland, Maryland, United States Teva Investigational Site 1360 Hagerstown, Maryland, United States United States, New York Teva Investigational Site 1369 Bronx, New York, United States Teva Investigational Site 1353 Manhasset, New York, United States Teva Investigational Site 1355 New York, New York, United States United States, North Carolina Teva Investigational Site 1356 Charlotte, North Carolina, United States United States, Ohio Teva Investigational Site 1354 Columbus, Ohio, United States United States, South Carolina Teva Investigational Site 1366 Charleston, South Carolina, United States Canada, Alberta Teva Investigational Site 1139 Edmonton, Alberta, Canada Canada, Ontario Teva Investigational Site 1136 London, Ontario, Canada Teva Investigational Site 1137 Toronto, Ontario, Canada Canada, Quebec Teva Investigational Site 1142 Montreal, Quebec, Canada Collapse <<
NCT02215616	Huntington's Disease	Phase 2	Completed	-	-
NCT02284568	Primary Progressive Multiple S... more >>clerosis Collapse <<	Phase 2	Completed	-	-
NCT01047319	Relapsing Multiple Sclerosis	Phase 3	Terminated(Sponsor terminated ... more >>RRMS studies as sufficient long term clinical data was collected for the study drug in the relevant dose) Collapse <<	-	-
NCT02085863	Pharmacokinetics ... more >> Pharmacodynamics Collapse <<	Phase 1	Completed	-	Germany ... more >> Teva Investigational Site 32415 Moenchengladbach, Germany Collapse <<
NCT02284568	-	-	Completed	-	-

拉喹莫德 Catalog No. CSN10659

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