CARTProduct Variations
| Product # | Price | Quantity | |
|---|---|---|---|
| VD-OEIA-0113-0005-5mg | $100 | ||
| VD-OEIA-0113-0050-50mg | $800 |
Leflunomide
$100.00 – $800.00
Product Specification
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Appearance:
White crystalline solid
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CAS Number:
75706-12-6
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Cat.number:
VD-OEIA-0113
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Formula:
C12H9F3N2O2
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MW:
270.21
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Purity:
>=99%
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Solubility:
DMSO or EtOH
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Storage:
+4°C.
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Synonyms:
5-Methyl-N-[4-(trifluoromethyl)phenyl]-4-isoxazolecarboxamide
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Size:
50mg, 5mg
Description
An immunosuppressive agent. Inhibits T and B cell proliferation. Activity is attributed mainly to its metabolite, a malononitrile derivative, which is beleived to inhibit dihydroorotate dehydrogenase as well as several protein tyrosine kinases. Therapeutically as a antirheumatic. In vitro the active metabolite A77 1726 (RS-61980) inhibits dihydroorotate dehydrogenase (Ki = 2.7 μM) and de novo pyrimidine synthesis in T-cells; blocks lymphocyte cell cycle progression and proliferation. A77 1726 also inhibits anti-CD3/CD28-induced cytokine production in PBMC cells (IC50 = 21-27 μg/ml). In vivo reduces inflammation in several animal models of autoimmune disease, arthritis, asthma and graft rejection.
1.Vrenken, T., et al.: J. Hepatol., 49, 799 (2008).
2.Mazzucco, G., et al.: Clin. Nephrol., 70, 163 (2008).
3.Greene et al (1995). Biochem.Pharmacol. 50 861.
4.Cherwinski et al (1995). J.Pharmacol.Exp.Ther. 275 1043.
5.Brazelton and Morris (1996). Curr.Opin.Immunol. 8 710.
6.Magari et al (2004). Inflamm.Res. 53 544.
7.Davies, M., et al.: J. Med. Chem., 52, 2683 (2009).
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