Home Immunology & Inflammation Immunology & Inflammation related modulator Laquinimod For research use only.

Laquinimod

Synonyms: ABR-215062, LAQ

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

Laquinimod Chemical Structure

Laquinimod Chemical Structure

CAS No. 248281-84-7

Purity & Quality Control

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

Laquinimod Related Products

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
NCT06161415 Recruiting
Inflammation|Uveitis
Quan Dong Nguyen|Global Ophthalmic Research Center (GORC)|Stanford University
 April 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

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)

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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