Laquinimod
Based on 2 publication(s) in Google Scholar
Laquinimod (ABR-215062), an orally available carboxamide derivative, is a potent immunomodulator which prevents neurodegeneration and inflammation in the central nervous system. Laquinimod reduces astrocytic NF-κB activation to protect from Cuprizone-induced demyelination. Laquinimod has the potential for relapsing remitting (RR) and chronic progressive (CP) forms of multiple sclerosis (MS; RRMS or CPMS) as well as neurodegenerative diseases research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.46%
- No. CAS: 248281-84-7
- Fòrmula: C19H17ClN2O3
- Peso molecular:356.80
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-10528
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Paquinimod -
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Andrographolide -
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Laquinimod (Standard) -
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HY-N0191R
Andrographolide (Standard) -
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JSH-23 -
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Maslinic acid -
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BAY 11-7085
Publications Citing Use of MedChemExpress (MCE) Laquinimod
More
Actividad biológica
Descripciòn
IC50 & Target
[3]|
NF-κB |
In Vitro
Laquinimod reverses EAE and inhibits pathogenic T cell immune responses. Laquinimod reverses RR-EAE and inhibits inflammatory T cell responses via a direct effect on myeloid APC. Laquinimod alters myeloid APC subsets and inhibits Th1 and Th17 polarization of myelin-specific T cells. Laquinimod-induced type II (M2) monocytes reverse established EAE[1]. Laquinimod modulates the phenotype of B cells of healthy donors. Laquinimod modulates expression of markers related to regulatory capacity in B cells of RRMS patients. Laquinimod reduces IFNγ cytokine expression in CD4+ T cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 248281-84-7
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Appearance Solid
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Peso molecular 356.80
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Fòrmula C19H17ClN2O3
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Color White to off-white
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SMILES
O=C(C1=C(O)C2=C(N(C)C1=O)C=CC=C2Cl)N(CC)C3=CC=CC=C3
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Synonyms
ABR-215062
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Int Immunopharmacol
Laquinimod attenuates oxidative stress-induced mitochondrial injury and alleviates intervertebral disc degeneration by inhibiting the NF-κB signaling pathway. [Abstract]2024 Apr 20:131:111804. PMID: 38457986 -
J Neuroimmunol
Laquinimod and 3,3'-diindolylemethane alleviate neuropathological events and neurological deficits in a mouse model of intracerebral hemorrhage. [Abstract]2020 Feb 20:342:577195. PMID: 32120083
Solvente y solubilidad
In Vitro:
DMSO : 25 mg/mL (70.07 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
Cell Assay[1]
Purified CD11b+ cells from laquinimod- or vehicle-treated mice are cultured with naive CD4+ cells isolated from laquinimod- or vehicle-treated 2D2 mice and antigen (MOG p35-55, 20 µg/mL). Cells are cultured in 96-well microtitre plates at a concentration of 0.25×106 cells/mL. Culture medium consisted of RPMI 1640 supplemented with L-glutamine (2 mM), sodium pyruvate (1 mM), penicillin (100 U/mL), streptomycin (0.1 mg/mL), 2-mercaptoethanol (5×10-5 M) and 10% (v/v) fetal bovine serum. Cells are incubated for 48 h and pulsed for 18 h with 1 µCi per well of [3H]-thymidine before harvesting.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[1]
Seven to 10-week-old female C57BL/6, DBA/1 or SJL/J mice are injected subcutaneously with 50 µg MOG p35-55, 50 µg rMOG or 100 µg PLP p139-151, respectively, in complete Freund's adjuvant. After immunization and 2 days later, mice receive 200 ng (C57BL/6) or 100 ng (SJL/J) pertussis toxin intraperitoneally (i.p.). For adoptive transfer, donor SJL/J mice are immunized as described above and treated daily with laquinimod or vehicle. 10 days later, cells from draining lymph nodes and spleen are isolated, re-stimulated for 48 h (20 µg/mL PLP p139-151), and injected i.p. into naive SJL/J recipients (107 cells per mouse). Animals are observed daily and clinical scores are assessed as follows: 0, no signs; 1, decreased tail tone; 2, mild monoparesis or paraparesis; 3, severe paraparesis; 4, paraplegia and/or quadraparesis; and 5, moribund or death.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (280 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Schulze-Topphoff, Ulf., et al. Laquinimod, a quinoline-3-carboxamide, induces type II myeloid cells that modulate central nervous system autoimmunity. PLoS One (2012), 7(3), e33797. [Content Brief]
[2]. Toubi E, et al. Laquinimod modulates B cells and their regulatory effects on T cells in Multiple Sclerosis. J Neuroimmunol. 2012 Oct 15;251(1-2):45-54. [Content Brief]
[3]. Brück W, et al. Reduced astrocytic NF-κB activation by laquinimod protects from cuprizone-induced demyelination. Acta Neuropathol. 2012 Sep;124(3):411-24. [Content Brief]
[4]. Jan Thöne, et al. Laquinimod in the treatment of multiple sclerosis: a review of the data so far. Drug Des Devel Ther. 2016 Mar 14;10:1111-8. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.8027 mL | 14.0135 mL | 28.0269 mL | 70.0673 mL |
| 5 mM | 0.5605 mL | 2.8027 mL | 5.6054 mL | 14.0135 mL | |
| 10 mM | 0.2803 mL | 1.4013 mL | 2.8027 mL | 7.0067 mL | |
| 15 mM | 0.1868 mL | 0.9342 mL | 1.8685 mL | 4.6712 mL | |
| 20 mM | 0.1401 mL | 0.7007 mL | 1.4013 mL | 3.5034 mL | |
| 25 mM | 0.1121 mL | 0.5605 mL | 1.1211 mL | 2.8027 mL | |
| 30 mM | 0.0934 mL | 0.4671 mL | 0.9342 mL | 2.3356 mL | |
| 40 mM | 0.0701 mL | 0.3503 mL | 0.7007 mL | 1.7517 mL | |
| 50 mM | 0.0561 mL | 0.2803 mL | 0.5605 mL | 1.4013 mL | |
| 60 mM | 0.0467 mL | 0.2336 mL | 0.4671 mL | 1.1678 mL |
Laquinimod Related Classifications
HY-13010 Related Classifications
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