Reversibly inhibits dihyroorotate dehydrogenase

A-771726 – 5 mg

Brand:
Cayman
CAS:
163451-81-8
Storage:
-20
UN-No:
Non-Hazardous - /

A-771726 is the active metabolite of leflunomide, a prodrug approved by the FDA for treatment of rheumatoid arthritis. A-771726 reversibly inhibits dihydroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines. It prevents activated lymphocytes from accumulating sufficient pyrimidines to support DNA synthesis (IC50s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively).{22723} At higher doses, A-771726 inhibits tyrosine kinases responsible for early T cell and B cell signaling in the G0/G1 phase of the cell cycle.{22723} A-771726 has also been shown to inhibit the production of prostaglandin E2 in synoviocytes activated by TNF-α and IL-1α (IC50s = 7 and 3 μM, respectively) as well as inhibit MMP-1 and IL-6 production at concentrations >10 μM.{22722}  

 

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Description

Reversibly inhibits dihyroorotate dehydrogenase, the rate-limiting step in the de novo synthesis of pyrimidines, preventing DNA synthesis of activated lymphocytes (IC50s = 0.09, 3.5, and 12.5 μM for rat, mouse, and human, respectively); also inhibits tyrosine kinases responsible for early T cell and B cell cycling and the production of PGE2, MMP-1, and IL-6 in immune-activated synoviocytes

Formal name: 2-cyano-3-hydroxy-N-[4-(trifluoromethyl)phenyl]-2Z-butenamide

Synonyms:  Flucyamide|HMR 1726|SU 20|Teriflunomide

Molecular weight: 270.2

CAS: 163451-81-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cell Biology|Cell Cycle||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases||Research Area|Epigenetics, Transcription, & Translation|RNA, DNA, & Protein Synthesis||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Autoimmunity|Rheumatoid Arthritis||Research Area|Immunology & Inflammation|Inflammatory Lipid Mediators|Prostaglandins||Research Area|Immunology & Inflammation|Innate Immunity

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