Home Immunology & Inflammation Immunology & Inflammation related modulator Laquinimod

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Laquinimod Immunology & Inflammation related modulator

Cat.No.S2787

Laquinimod (ABR-215062, LAQ) is a potent immunomodulator. Phase 3.
Laquinimod Immunology & Inflammation related modulator Chemical Structure

Chemical Structure

Molecular Weight: 356.8

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 61 mg/mL (170.96 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 356.8 Formula

C19H17ClN2O3

 Storage (From the date of receipt)
CAS No. 248281-84-7 Download SDF Storage of Stock Solutions

Synonyms ABR-215062, LAQ Smiles CCN(C1=CC=CC=C1)C(=O)C2=C(C3=C(C=CC=C3Cl)N(C2=O)C)O

Mechanism of Action

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, this compound is shown to induce suppression of genes related to antigen presentation and corresponding inflammatory pathways. It induces activation of Th2 response in CD14+ and CD4+ cells and suppression of proliferation in CD8+ cells. This chemical 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.
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 this compound may mediate its effects by regulation of Th1/Th2 cytokine balance. It significantly inhibits the development of murine acute experimental autoimmune encephalomyelitis (EAE), being approximately 20 times more potent than the immunomodulator roquinimex. This compound 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). It potently inhibits the development of chronic experimental autoimmune encephalomyelitis (chEAE) in IFN-beta k.o. mice and wild type mice. This chemical 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. The study of this compound in the mice model of EAE using a conditional BDNF knockout strain lacking BDNF expression in myeloid cells and T cells (LLF mice) indicates it also modulates autoimmune demyelination via induction of brain-derived neurotrophic factor (BDNF).
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16472873/
  • [5] https://pubmed.ncbi.nlm.nih.gov/20347159/
  • [6] https://pubmed.ncbi.nlm.nih.gov/20684995/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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