Leflunomide

SKU: orb1309564

Description

Leflunomide (HWA486) is a disease-modifying antirheumatic drug (DMARD) used to treat rheumatoid and psoriatic arthritis. Its active metabolite, teriflunomide, inhibits dihydroorotate dehydrogenase (DHODH), suppressing pyrimidine synthesis in proliferating lymphocytes. This mechanism is validated in both in vitro cellular assays and in vivo animal models of autoimmune disease.

Research Area

Immunology & Inflammation

Key Properties

• CAS Number: 75706-12-6
• MW: 270.21
• Purity: >98%
• Formula: C₁₂H₉F₃N₂O₂
• SMILES: CC1=C(C=NO1)C(=O)NC1=CC=C(C=C1)C(F)(F)F
• Target: Dehydrogenase (GAPDH, GPDH, IMPDH, PHGDH, LDH, DHODH, ALDH, GDH, IDH, UGDH, DPD, DHPDH, KGDH, PDH, and MDH)
• Solubility: Soluble in DMSO (up to 30 mg/ml) or in Ethanol (up to 25 mg/ml).

Bioactivity

• In Vivo:
  Leflunomide is an immunomodulatory drug that acts by inhibiting the mitochondrial enzyme dihydrolactate dehydrogenase.Leflunomide inhibits anti-CD3- and interleukin-2 (IL-2)-stimulated T-cell proliferation.Leflunomide also inhibits the response stimulated by the anti-CD3 monoclonal antibody to the production of IL-2 and the expression of the IL-2 receptor in human T lymphocytes. Leflunomide also inhibits IL-2-stimulated tyrosine phosphorylation in CTLL-4 cells.Leflunomide prevents activation and expansion of autoimmune lymphocytes by interfering with cell cycle progression due to insufficient production of rUMP and the use of mechanisms involved in p53.Leflunomide inhibits p53-stimulated T-cell proliferation in an in vitro tyrosine kinase assay. assay, was able to inhibit p59fyn and p56lck activity.
• In Vitro:
  Leflunomide is an immunomodulatory drug that acts by inhibiting the mitochondrial enzyme dihydrolactate dehydrogenase.Leflunomide inhibits anti-CD3- and interleukin-2 (IL-2)-stimulated T-cell proliferation.Leflunomide also inhibits the response stimulated by the anti-CD3 monoclonal antibody to the production of IL-2 and the expression of the IL-2 receptor in human T lymphocytes. Leflunomide also inhibits IL-2-stimulated tyrosine phosphorylation in CTLL-4 cells.Leflunomide prevents activation and expansion of autoimmune lymphocytes by interfering with cell cycle progression due to insufficient production of rUMP and the use of mechanisms involved in p53.Leflunomide inhibits p53-stimulated T-cell proliferation in an in vitro tyrosine kinase assay. assay, was able to inhibit p59fyn and p56lck activity.

Storage & Handling

• Storage: RT
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RS-34821

Compound Identifiers

PubChem CID

3899