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Leflunomide

ALX-430-095

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Immunosuppressant

Immunosuppressive drug that inhibits T and B cell responses in vivo. Inhibitor of tyrosine phosphorylation (tyrosine kinase inhibitor), of dihydroorotate dehydrogenase, an enzyme for de novo pyrimidine synthesis, of TNF-dependent NF-κB activation, and of COX-2. The physiological activity of leflunomide is attributed mainly to its metabolite A77 1726 (Prod. No. ALX-430-096).

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Product Details

Alternative Name	HWA486, 5-Methylisoxazole-4-(4-trifluoromethylcarboxanilide), N-(4-Trifluoromethylphenyl)-5-methylisoxazol-4-carboxamide
Appearance	White to off-white crystalline powder.
CAS	75706-12-6
Couple Target	COX, NF-kappaB
Couple Type	Inhibitor
Formula	C₁₂H₉F₃N₂O₂
Identity	Determined by IR.
MI	14: 5432
MW	270.2
Purity	≥98.5% (HPLC)
RTECS	NY2354200
Solubility	Soluble in DMSO or methanol.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Handling	Protect from light. Keep under inert gas.
Long Term Storage	+4°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

Mitochondrial dysfunction induced by leflunomide and its active metabolite: J. Xuan, et al.; Toxicology 396, 33 (2018), Abstract — Full Text
Ginsenoside Rb1 enhances atherosclerotic plaque stability by skewing macrophages to the M2 phenotype: X. Zhang, et al.; J. Cell. Mol. Med. 22, 409 (2018), Abstract — Full Text
Endoplasmic reticulum stress and MAPK signaling pathway activation underlie leflunomide-induced toxicity in HepG2 Cells: Ren, Z., Chen, S., et al.; Toxicology 392, 11 (2017), Abstract
Human Cytomegalovirus Can Procure Deoxyribonucleotides for Viral DNA Replication in the Absence of Retinoblastoma Protein Phosphorylation: Kuny, C. V., Kalejta, R. F., et al.; J. Virol. 90, 8634 (2016), Abstract
The anti-inflammatory drug leflunomide is an agonist of the aryl hydrocarbon receptor: O’Donnell, E. F., Saili, K. S., et al.; PLoS One 5, (2010), Abstract
Leflunomide: mode of action in the treatment of rheumatoid arthritis: F.C. Breedveld & J.M. Dayer; Ann. Rheum. Dis. 59, 841 (2000), Abstract
Immunosuppressive leflunomide metabolite (A77 1726) blocks TNF- dependent nuclear factor-kappa B activation and gene expression: S.K. Manna and B.B. Aggarwal; J. Immunol. 162, 2095 (1999), Abstract
In vivo activity of leflunomide: pharmacokinetic analyses and mechanism of immunosuppression: A.S. Chong, et al.; Transplantation 68, 100 (1999), Abstract
A771726, the active metabolite of leflunomide, directly inhibits the activity of cyclo-oxygenase-2 in vitro and in vivo in a substrate- sensitive manner: L.C. Hamilton, et al.; Br. J. Pharmacol. 127, 1589 (1999), Abstract
Inhibition of JAK3 and STAT6 tyrosine phosphorylation by the immunosuppressive drug leflunomide leads to a block in IgG1 production: K.F. Siemasko, et al.; J. Immunol. 160, 1581 (1998), Abstract

Related Products

A77 1726

ALX-430-096

Dihydrorotate dehydrogenase inhibitor

10 citations

Alternative Name	N-(4-Trifluoromethylphenyl)-2-cyano-3-hydroxycrotonamide, 2-Cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2-butenamide
CAS	108605-62-5
Couple Type	Inhibitor
Purity	≥98% (HPLC)

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Leflunomide

ALX-430-095

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Handling & Storage

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