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Leflunomide (CAS 75706-12-6)

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Alternate Names:
5-Methylisoxazole-4-(4-trifluoromethylcarboxanilide); HWA486; N-(4-Trifluoromethylphenyl)-5-methylisoxazol-4-carboxamide
Application:
Leflunomide is an inhibitor of Cox-2 and tyrosine kinase
CAS Number:
75706-12-6
Purity:
≥99%
Molecular Weight:
270.20
Molecular Formula:
C12H9F3N2O2
Supplemental Information:
This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.

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Leflunomide is an immunosuppressive drug that inhibits T and B cell responses. Leflunomide is an inhibitor of Cox-2, of tyrosine phosphorylation (tyrosine kinase), of DHODH (dihydroorotate dehydrogenase), an enzyme for de novo pyrimidine synthesis, and of TNF-dependent NF-kappaB activation. The physiological activity of leflunomide is attributed mainly to its metabolite A77 1726. By targeting the enzyme dihydroorotate dehydrogenase (DHODH), responsible for pyrimidine nucleotide synthesis, it effectively obstructs DNA and RNA production.


Leflunomide (CAS 75706-12-6) References

  1. Leflunomide (HWA 486), a novel immunomodulating compound for the treatment of autoimmune disorders and reactions leading to transplantation rejection.  |  Bartlett, RR., et al. 1991. Agents Actions. 32: 10-21. PMID: 2058454
  2. Leflunomide-induced liver injury in mice: Involvement of TLR4 mediated activation of PI3K/mTOR/NFκB pathway.  |  Elshaer, RE., et al. 2019. Life Sci. 235: 116824. PMID: 31476305
  3. Efficacy of leflunomide in the treatment of vasculitis.  |  Mustapha, N., et al. 2021. Clin Exp Rheumatol. 39 Suppl 129: 114-118. PMID: 33200732
  4. Leflunomide Suppresses the Growth of LKB1-Inactivated Tumors in the Immune-Competent Host and Attenuates Distant Cancer Metastasis.  |  Jin, R., et al. 2021. Mol Cancer Ther. 20: 274-283. PMID: 33293343
  5. Leflunomide ameliorates experimental autoimmune myasthenia gravis by regulating humoral and cellular immune responses.  |  Huang, H., et al. 2021. Int Immunopharmacol. 93: 107434. PMID: 33556668
  6. Leflunomide therapy for adult patients with steroid-dependent minimal change disease or primary focal segmental glomerulosclerosis.  |  Zhao, C., et al. 2022. Chin Med J (Engl). 135: 866-868. PMID: 34935693
  7. Immunopharmacological profile of a novel isoxazol derivative, HWA 486, with potential antirheumatic activity--I. Disease modifying action on adjuvant arthritis of the rat.  |  Bartlett, RR. and Schleyerbach, R. 1985. Int J Immunopharmacol. 7: 7-18. PMID: 3873420
  8. Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide.  |  Xu, X., et al. 1995. J Biol Chem. 270: 12398-403. PMID: 7759480
  9. Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide.  |  Mattar, T., et al. 1993. FEBS Lett. 334: 161-4. PMID: 8224241
  10. The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase.  |  Davis, JP., et al. 1996. Biochemistry. 35: 1270-3. PMID: 8573583
  11. Regulation of B cell function by the immunosuppressive agent leflunomide.  |  Siemasko, KF., et al. 1996. Transplantation. 61: 635-42. PMID: 8610393
  12. Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation.  |  Xu, X., et al. 1996. Biochem Pharmacol. 52: 527-34. PMID: 8759024
  13. In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice.  |  Xu, X., et al. 1997. J Immunol. 159: 167-74. PMID: 9200452
  14. Potencies of leflunomide and HR325 as inhibitors of prostaglandin endoperoxide H synthase-1 and -2: comparison with nonsteroidal anti-inflammatory drugs.  |  Curnock, AP., et al. 1997. J Pharmacol Exp Ther. 282: 339-47. PMID: 9223572

Ordering Information

Product NameCatalog #UNITPriceQtyFAVORITES

Leflunomide, 10 mg

sc-202209
10 mg
$20.00

Leflunomide, 50 mg

sc-202209A
50 mg
$81.00

What is the appearance of the compound?

Asked by: two2igm05
Thank you for your question. The compound, sc-202209, is provided as a white to off-white crystalline powder. If you have any further questions or concerns, please feel free to contact our Technical Service department by calling 800-457-3801 option 2, emailing scbt@scbt.com, or using the Live Chat function on our website.
Answered by: Tech Service 8
Date published: 2017-01-16
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Rated 5 out of 5 by from Patel A; et alPatel A; et al. (PubMed ID: 26417045) determined that Leflunomide increases pulmonary and hepatic CYP1A enzymes through the aryl hydrocarbon receptor. -SCBT Publication Review
Date published: 2015-01-09
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Leflunomide is rated 5.0 out of 5 by 1.
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