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Purity: ≥98%
Leflunomide (formerly also known as HWA486; Leflunomidum, trade/brand name Arava) is a potent pyrimidine synthesis inhibitor belonging to the DMARD (disease-modifying antirheumatic drug), it is used as an immunosuppressant agent for treating inflammatory conditions such as RA-rheumatoid arthritis.
| ln Vitro |
It has been demonstrated that leflunomide, a prodrug, inhibits the growth of T- and mononuclear cells. Leflunomide exhibits IC50 values ranging from 30 mM to 100 mM in in vitro cellular and enzymatic studies, indicating its ability to inhibit several protein tyrosine kinases[1]. Leflunomide has the ability to prevent T cell proliferation that is driven by interleukin-2 (IL-2) and anti-CD3. Leflunomide has the ability to block the activity of p59fyn and p56lck in in vitro tyrosine kinase tests. Additionally, leflunomide prevents Ca2+ mobilization in Jurkat cells that are activated by anti-CD3 antibodies, but not in cells that are activated by ionomycin. Leflunomide also prevents the synthesis of IL-2 and the development of IL-2 receptors on human T cells, which are distal outcomes of anti-CD3 monoclonal antibody activation. Leflunomide also prevents CTLL-4 cells activated by IL-2 from phosphorylating tyrosine [2]. The immunomodulatory medication leflunomide may work by preventing the mitochondrial enzyme dihydroorotate dehydrogenase (DHODH) from doing its job. DHODH is essential for the de novo production of pyrimidine ribonucleotide uridine monophosphate (rUMP). Leflunomide inhibits the growth of autoimmune and activated lymphocytes by disrupting the cell cycle through mechanisms involving p53 and insufficient rUMP production[3].
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| ln Vivo |
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| References |
[1]. Davis JP, et al. The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase. Biochemistry. 1996 Jan 30;35(4):1270-3.
[2]. Xu X, et al. Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide. J Biol Chem. 1995 May 26;270(21):12398-403. [3]. Fox RI, et al. Mechanism of action for leflunomide in rheumatoid arthritis. Clin Immunol. 1999 Dec;93(3):198-208 |
| Molecular Formula |
C12H9F3N2O2
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| Molecular Weight |
270.21
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| CAS # |
75706-12-6
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| Related CAS # |
Leflunomide-d4;1189987-23-2
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| SMILES |
O=C(C1=C(C)ON=C1)NC2=CC=C(C(F)(F)F)C=C2
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| InChi Key |
VHOGYURTWQBHIL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H9F3N2O2/c1-7-10(6-16-19-7)11(18)17-9-4-2-8(3-5-9)12(13,14)15/h2-6H,1H3,(H,17,18)
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| Chemical Name |
5-methyl-N-[4-(trifluoromethyl)phenyl]-1,2-oxazole-4-carboxamide
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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