© 2008 Alexis Corporation
ALX-430-095
Revised 23-Jan-08
Leflunomide
SYNONYMS
HWA486
5-Methylisoxazole-4-(4-trifluoromethylcarboxanilide)
N-(4-Trifluoromethylphenyl)-5-methylisoxazol-4-carboxamide
PRODUCT LINE
Immunology
PRODUCT CATEGORY
Immunomodulators Other Products
Ordering Information
Product Numbers:
Format:
Size:
Unit Price:
Quantity:
Add To Cart
ALX-430-095-M010
10 mg
15.00 USD
ALX-430-095-M050
50 mg
40.00 USD
ALX-430-095-G001
1 g
380.00 USD
Product Specification
FORMULA:
C
12
H
9
F
3
N
2
O
2
MW:
270.2
CAS NUMBER:
75706-12-6
MERCK INDEX:
14:
5432
RTECS:
NY2354200
PURITY:
≥99% (HPLC)
APPEARANCE:
White to off-white solid.
SOLUBILITY:
Soluble in DMSO or methanol.
SHIPPING:
AMBIENT
LONG TERM STORAGE:
+4°C
HANDLING:
Keep under inert gas. Protect from light.
HAZARD:
HARMFUL.
Product Description
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
).
Product Specific Literature References
Immunopharmacological profile of a novel isoxazol derivative, HWA 486, with potential antirheumatic activity-I. Disease modifying action on adjuvant arthritis of the rat:
R.R. Bartlett & R. Schleyerbach; Int. J. Immunopharmacol.
7
, 7 (1985)
Abstract
Leflunomide (HWA 486), a novel immunomodulating compound for the treatment of autoimmune disorders and reactions leading to transplantation rejection:
R.R. Bartlett, et al.; Agents Actions
32
, 10 (1991)
Abstract
Inhibition of the epidermal growth factor receptor tyrosine kinase activity by leflunomide:
T. Mattar, et al.; FEBS Lett.
334
, 161 (1993)
Abstract
Inhibition of protein tyrosine phosphorylation in T cells by a novel immunosuppressive agent, leflunomide:
X. Xu, et al.; J. Biol. Chem.
270
, 12398 (1995)
Abstract
;
Full Text
Molecular mechanisms of action of new xenobiotic immunosuppressive drugs: tacrolimus (FK506), sirolimus (rapamycin), mycophenolate mofetil and leflunomide:
T.R. Brazelton & R.E. Morris; Curr. Opin. Immunol.
8
, 710 (1996)
Abstract
The immunosuppressive metabolite of leflunomide is a potent inhibitor of human dihydroorotate dehydrogenase:
J.P. Davis, et al.; Biochemistry
35
, 1270 (1996)
Abstract
Regulation of B cell function by the immunosuppressive agent leflunomide:
K.F. Siemasko, et al.; Transplantation
61
, 635 (1996)
Abstract
Two activities of the immunosuppressive metabolite of leflunomide, A77 1726. Inhibition of pyrimidine nucleotide synthesis and protein tyrosine phosphorylation:
X. Xu, et al.; Biochem. Pharmacol.
52
, 527 (1996)
Abstract
Potencies of leflunomide and HR325 as inhibitors of prostaglandin endoperoxide H synthase-1 and -2: comparison with nonsteroidal anti- inflammatory drugs:
A.P. Curnock, et al.; J. Pharmacol. Exp. Ther.
282
, 339 (1997)
Abstract
In vivo mechanism by which leflunomide controls lymphoproliferative and autoimmune disease in MRL/MpJ-lpr/lpr mice:
X. Xu, et al.; J. Immunol.
159
, 167 (1997)
Abstract
Leflunomide, a novel immunomodulating agent, prevents the development of allergic sensitization in an animal model of allergic asthma:
E. Eber, et al.; Clin. Exp. Allergy
28
, 376 (1998)
Abstract
Species-related inhibition of human and rat dihydroorotate dehydrogenase by immunosuppressive isoxazol and cinchoninic acid derivatives:
W. Knecht & M. Löffler; Biochem. Pharmacol.
56
, 1259 (1998)
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
In vivo activity of leflunomide: pharmacokinetic analyses and mechanism of immunosuppression:
A.S. Chong, et al.; Transplantation
68
, 100 (1999)
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
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
Leflunomide: mode of action in the treatment of rheumatoid arthritis:
F.C. Breedveld & J.M. Dayer; Ann. Rheum. Dis.
59
, 841 (2000)
Abstract
General Literature References
Leflunomide, a novel immunomodulator for the treatment of active rheumatoid arthritis
:
M.M. Goldenberg; Clin. Ther.
21
, 1837 (1999), (Review)
Abstract
Leflunomide, mycophenolic acid and matrix metalloproteinase inhibitors
:
D.E. Furst; Rheumatology (Oxford)
38 Suppl 2
, 14 (1999), (Review)
Abstract
Leflunomide and methotrexate
:
R.F. Laan, et al.; Curr. Opin. Rheumatol.
13
, 159 (2001), (Review)
Abstract
Experiences with leflunomide in solid organ transplantation
:
J.W. Williams, et al.; Transplantation
73
, 358 (2002), (Review)
Abstract
Further Categories Containing This Product:
COX Inhibitors
•
NF-kB Pathway Inhibitors
•
Tyrosine Kinase Inhibitors
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