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(2R,3S)-3-(formyl-hydroxy-amino)-4-methyl-2-(2-methylpropyl)-N-[(1S,2S)-2-methyl-1-(pyridin-2-ylcarbamoyl)butyl]pentanamide

Names

[ CAS No. ]:
212609-68-2

[ Name ]:
(2R,3S)-3-(formyl-hydroxy-amino)-4-methyl-2-(2-methylpropyl)-N-[(1S,2S)-2-methyl-1-(pyridin-2-ylcarbamoyl)butyl]pentanamide

[Synonym ]:
Pentanamide, 3-(formylhydroxyamino)-4-methyl-2-(2-methylpropyl)-N-[(1S,2S)-2-methyl-1-[(2-pyridinylamino)carbonyl]butyl]-, (2R,3S)-
N2-{(2R,3S)-3-[Formyl(hydroxy)amino]-2-isobutyl-4-methylpentanoyl}-N-2-pyridinyl-L-isoleucinamide

Biological Activity

[Description]:

GW-3333 is a potent and orally active TNF-alpha-converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitor. GW-3333 inhibits tumor necrosis factor-alpha (TNF-alpha) production. GW-3333 can be used in research of arthritis[1][2].

[Related Catalog]:

Research Areas >> Inflammation/Immunology
Signaling Pathways >> Metabolic Enzyme/Protease >> MMP

[In Vivo]

GW-3333 在关节炎大鼠模型中抑制踝关节肿胀和关节破坏[1]。 GW-3333 (p.o.) 在关节炎大鼠模型中阻断 LPS 后血浆 TNF 的增加长达 12 小时[1]。

[References]

[1]. Conway JG, et, al. Inhibition of tumor necrosis factor-alpha (TNF-alpha) production and arthritis in the rat by GW3333, a dual inhibitor of TNF-alpha-converting enzyme and matrix metalloproteinases. J Pharmacol Exp Ther. 2001 Sep;298(3):900-8.  

[2]. Doggrell SA. TACE inhibition: a new approach to treating inflammation. Expert Opin Investig Drugs. 2002 Jul;11(7):1003-6.  

Chemical & Physical Properties

[ Density]:
1.1±0.1 g/cm3

[ Molecular Formula ]:
C22H36N4O4

[ Molecular Weight ]:
420.55

[ Exact Mass ]:
420.273651

[ LogP ]:
3.40

[ Index of Refraction ]:
1.538


Related Compounds

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