Laquinimod

Catalog No.S2787 Synonyms: ABR-215062, LAQ

Laquinimod Chemical Structure

Molecular Weight(MW): 356.8

Laquinimod is a potent immunomodulator. Phase 3.

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In DMSO USD 390 In stock
USD 270 In stock
USD 470 In stock
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Biological Activity

Description Laquinimod is a potent immunomodulator. Phase 3.
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]

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]

Protocol

Cell Research:[5]
+ Expand
  • 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.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • 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
  • Formulation: Dissolved in PBS
  • Dosages: 0.16, 1.6 and 16 mg/kg/day
  • Administration: Administered via a daily subcutaneous injection
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 61 mg/mL (170.96 mM)
Ethanol 1 mg/mL (2.8 mM)
Water Insoluble
In vivo Add solvents individually and in order:
30% propylene glycol, 5% Tween 80, 65% D5W
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 356.8
Formula

C19H17ClN2O3

CAS No. 248281-84-7
Storage powder
Synonyms ABR-215062, LAQ

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02284568 Active, not recruiting Primary Progressive Multiple Sclerosis Teva Pharmaceutical Industries January 2015 Phase 2
NCT02215616 Recruiting Huntingtons Disease Teva Branded Pharmaceutical Products, R&D Inc.|Teva Pharmaceutical Industries November 2014 Phase 2
NCT02085863 Completed Pharmacokinetics|Pharmacodynamics Teva Pharmaceutical Industries February 2014 Phase 1
NCT01975298 Withdrawn Relapsing Remitting Multiple Sclerosis Teva Pharmaceutical Industries January 2014 Phase 3
NCT01707992 Active, not recruiting Multiple Sclerosis (MS) Teva Pharmaceutical Industries February 2013 Phase 3
NCT01404117 Withdrawn Relapsing Multiple Sclerosis Teva Pharmaceutical Industries March 2012 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID