Name: Laquinimod
Brand: Selleck Chemicals
SKU: S2787
Rating: 5 (2 reviews)

Laquinimod (ABR-215062, LAQ) is a potent immunomodulator. Phase 3.

Laquinimod Chemical Structure

CAS: 248281-84-7

Selleck's Laquinimod has been cited by 2 publications

Purity & Quality Control

Batch: S278701 DMSO] 61 mg/mL] false] Ethanol] 1 mg/mL] false] Water] Insoluble] false Purity: 99.96%

99.96

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Biological Activity

Description	Laquinimod (ABR-215062, LAQ) is a potent immunomodulator. Phase 3.

In vitro
In vitro	Laquinimod treatment at 0.1-1 μM does not affect the viability of peripheral blood mononuclear cells (PBMC). By performing the large-scale gene expression microarray analysis in PBMC from healthy subjects or relapsing-remitting multiple sclerosis (RRMS) patients, Laquinimod is shown to induce suppression of genes related to antigen presentation and corresponding inflammatory pathways. Laquinimod induces activation of Th2 response in CD14+ and CD4+ cells and suppression of proliferation in CD8+ cells. Laquinimod displays significant effects on immune modulation related to the suppression of antigen presenting mechanism followed by a decrease of chemotaxis and adhesion, and exhibits potent anti-inflammatory potency through the suppression of the NF-κB pathway that concordantly leads to the activation of apoptosis of immuno-competent cells. ^[5]
Cell Research	Cell lines	PBMC
	Concentrations	Dissolved in PBS, final concentrations ~1 μM
	Incubation Time	24 hours
	Method	The peripheral blood mononuclear cells (PBMC) are incubated with Laquinimod for 24 hours. Cell viability is measured on total PBMC by propidium iodide (PI) staining using an automated cell counter. Protein expression level is assessed in PBMC samples by Western blot using anti-HLA-DQA/DQB monoclonal antibodies.

In Vivo
In vivo	Administration of Laquinimod (0.16-16 mg/kg/day) dose-dependently inhibits the incidence of experimental autoimmune neuritis (EAN) in Lewis rats, ameliorates clinical signs and inhibits P0 peptide 180-199-specific T cell responses as well as the inflammation and demyelination in the peripheral nerves, suggesting that Laquinimod may mediate its effects by regulation of Th1/Th2 cytokine balance. ^[1] Laquinimod significantly inhibits the development of murine acute experimental autoimmune encephalomyelitis (EAE), being approximately 20 times more potent than the immunomodulator roquinimex. ^[2] Laquinimod treatment inhibits the development of experimental autoimmune encephalomyelitis (EAE) in the Lewis rat in a dose-dependent manner, and shows better disease inhibitory effects as compared to roquinimex (Linomide). ^[3] Laquinimod potently inhibits the development of chronic experimental autoimmune encephalomyelitis (chEAE) in IFN-beta k.o. mice and wild type mice. ^[4] Laquinimod reduces clinical signs, inflammation, and demyelination in C57BL/6 mice with active EAE induced with MOG(35-55) peptide, and down-regulates VLA-4-mediated adhesiveness and pro-inflammatory cytokines such as IL-17. ^[6] The study of Laquinimod in the mice model of EAE using a conditional BDNF knockout strain lacking BDNF expression in myeloid cells and T cells (LLF mice) indicates Laquinimod also modulates autoimmune demyelination via induction of brain-derived neurotrophic factor (BDNF). ^[7]
Animal Research	Animal Models	Lewis rats with experimental autoimmune neuritis (EAN) induced by inoculation with peripheral nerve myelin P0 protein peptide 180-199 and Freund's complete adjuvant
	Dosages	0.16, 1.6 and 16 mg/kg/day
	Administration	Administered via a daily subcutaneous injection

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT06161415	Not yet recruiting	Uveitis	Quan Dong Nguyen\|Global Ophthalmic Research Center (GORC)\|Stanford University	January 2024	Phase 1
NCT05187403	Completed	Eye Diseases	Active Biotech AB	December 9 2021	Phase 1
NCT02772523	Completed	Alzheimer''s Disease	Barcelonabeta Brain Research Center Pasqual Maragall Foundation	May 2016	Not Applicable
NCT02085863	Completed	Pharmacokinetics\|Pharmacodynamics	Teva Branded Pharmaceutical Products R&D Inc.	February 2014	Phase 1
NCT01975298	Withdrawn	Relapsing Remitting Multiple Sclerosis	Teva Branded Pharmaceutical Products R&D Inc.	January 2014	Phase 3

References

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Chemical Information & Solubility

Molecular Weight	356.8	Formula	C₁₉H₁₇ClN₂O₃
CAS No.	248281-84-7	SDF	Download Laquinimod SDF
Smiles	CCN(C1=CC=CC=C1)C(=O)C2=C(C3=C(C=CC=C3Cl)N(C2=O)C)O
Storage (From the date of receipt)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 61 mg/mL ( (170.96 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

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In vivo
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