Leflunomide (Synonyms: HW 486, SU 101) |
| Catalog No.GC17904 |
Leflunomide (HWA486) is a pyrimidine biosynthesis inhibitor that acts by inhibiting dihydroorotate dehydrogenase (DHODH) and has anti-rheumatic effects.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 75706-12-6
Sample solution is provided at 25 µL, 10mM.
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Leflunomide (HWA486) is a pyrimidine biosynthesis inhibitor that acts by inhibiting dihydroorotate dehydrogenase (DHODH) and has anti-rheumatic effects[1]. Leflunomide is a low molecular weight synthetic oral drug specifically developed for immunosuppression[2]. Leflunomide is rapidly converted to its pharmacologically active metabolite A-771726 in vivo[3].
In vitro, treatment of neuroblastoma cell lines (BE(2)-C, SK-N-DZ, and SK-N-F1 cells) with leflunomide (12.5-100µM) for 6 days reduced cell growth in a dose- and time-dependent manner. Treatment with 100µM leflunomide for 72h reduced cell number by more than 60% and induced S phase cell cycle arrest and apoptosis[4]. Leflunomide (10µM) treatment of Jurkat cells for 2h blocked tumor necrosis factor (TNF)-induced I-κBα (NF-κB inhibitory subunit) phosphorylation and IκB kinase β (IKK-β) activation[5].
In vivo, oral treatment of experimental autoimmune uveitis (EAU) rats with leflunomide (3, 6, 12mg/kg) for 2 weeks significantly prevented and treated EAU, reduced clinical and pathological scores, reduced serum IL17 and IFN-γ levels, and reduced the number of Th17 cells[6]. Leflunomide (4, 20mg/kg) was orally treated in experimental autoimmune neuritis (EAN) rats, significantly preventing and treating EAN, protecting nerves from more extensive demyelination and axonal degeneration, and reducing the number of T cells and activated macrophages in the endoneurium[7].
References:
[1] Kaur H, Sarma P, Bhattacharyya A, et al. Efficacy and safety of dihydroorotate dehydrogenase (DHODH) inhibitors “leflunomide” and “teriflunomide” in Covid-19: A narrative review[J]. European journal of pharmacology, 2021, 906: 174233.
[2] Cannon G W, Kremer J M. Leflunomide[J]. Rheumatic Disease Clinics, 2004, 30(2): 295-309.
[3] Herrmann M L, Schleyerbach R, Kirschbaum B J. Leflunomide: an immunomodulatory drug for the treatment of rheumatoid arthritis and other autoimmune diseases[J]. Immunopharmacology, 2000, 47(2-3): 273-289.
[4] Zhu S, Yan X, Xiang Z, et al. Leflunomide reduces proliferation and induces apoptosis in neuroblastoma cells in vitro and in vivo[J]. PloS one, 2013, 8(8): e71555.
[5] Manna S K, Mukhopadhyay A, Aggarwal B B. Leflunomide suppresses TNF-induced cellular responses: effects on NF-κB, activator protein-1, c-Jun N-terminal protein kinase, and apoptosis[J]. The Journal of Immunology, 2000, 165(10): 5962-5969.
[6] Fang C, Zhou D, Zhan S, et al. Amelioration of experimental autoimmune uveitis by leflunomide in Lewis rats[J]. PloS one, 2013, 8(4): e62071.
[7] Korn T, Toyka K, Hartung H P, et al. Suppression of experimental autoimmune neuritis by leflunomide[J]. Brain, 2001, 124(9): 1791-1802.
| Cell experiment [1]: | |
Cell lines | BE(2)-C、SK-N-F1、SK-N-DZ cells |
Preparation Method | All three cell lines, BE(2)-C, SK-N-DZ, and SK-N-F1, were treated with 12.5, 25, 50, 100, and 200µM leflunomide for 6 days, and DMSO was used as a control. Cell growth was tested every 2 days by CCK-8 assay. |
Reaction Conditions | 12.5, 25, 50, 100, 200µM; 2h |
Applications | Leflunomide reduced the growth of all three cell lines in a dose- and time-dependent manner. Treatment with 100µM Leflunomide for 72h reduced the number of cells by more than 60%. |
| Animal experiment [2]: | |
Animal models | Lewis rats |
Preparation Method | Lewis rats were immunized with interphotoreceptor retinoid-binding peptide (IRBP) in order to generate experimental autoimmune uveitis (EAU). Rats received three dose of leflunomide through intragastric administration (prevention or treatment protocols) after immunization at three separate doses (3mg/kg/d; 6mg/kg/d; 12mg/kg/d). Cyclosporin A was administered as a positive) control. Rats were euthanized during peak disease activity (day 14 or 15). |
Dosage form | 3、6、12mg/kg/day; p.o. |
Applications | Leflunomide treatment significantly prevented and treated EAU-induced ocular inflammation and reduced clinical and pathological scores. Leflunomide significantly reduced serum IL17 and IFN-γ levels. The number of Th17 cells was decreased in rats in the leflunomide prevention group. |
References: [1]Zhu S, Yan X, Xiang Z, et al. Leflunomide reduces proliferation and induces apoptosis in neuroblastoma cells in vitro and in vivo[J]. PloS one, 2013, 8(8): e71555. [2]Fang C, Zhou D, Zhan S, et al. Amelioration of experimental autoimmune uveitis by leflunomide in Lewis rats[J]. PloS one, 2013, 8(4): e62071. | |
| Cas No. | 75706-12-6 | SDF | |
| Synonyms | HW 486, SU 101 | ||
| Chemical Name | 5-methyl-N-[4-(trifluoromethyl)phenyl]-1,2-oxazole-4-carboxamide | ||
| Canonical SMILES | CC1=C(C=NO1)C(=O)NC2=CC=C(C=C2)C(F)(F)F | ||
| Formula | C12H9F3N2O2 | M.Wt | 270.21 |
| Solubility | ≥ 83.3mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7008 mL | 18.5041 mL | 37.0083 mL |
| 5 mM | 0.7402 mL | 3.7008 mL | 7.4017 mL |
| 10 mM | 0.3701 mL | 1.8504 mL | 3.7008 mL |
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- Purity: >99.50%
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