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Pralnacasan

Names

[ CAS No. ]:
192755-52-5

[ Name ]:
Pralnacasan

[Synonym ]:
Pralnaan [INN]
HMR 3480
Pralnaan
Pralnaan (USAN/INN)
UNII-N986NI319S

Biological Activity

[Description]:

Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a Ki of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment[1][2].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Caspase
Research Areas >> Inflammation/Immunology

[Target]

Interleukin-1β converting enzyme:1.4 nM (Ki)


[In Vivo]

Pralnacasan (0 -50 mg/kg; oral gavage; twice a day; for 6 weeks; female Balb/c mice) treatment reduces joint damage. Pralnacasan treatment does not appear to affect the weight of the animals[1]. Animal Model: Female Balb/c mice induced with collagenase[1] Dosage: 0 mg/kg, 12.5 mg/kg, 25 mg/kg and 50 mg/kg Administration: Oral gavage; twice a day; for 6 weeks Result: Significantly ameliorated the histopathological damage of the medial knee joint compartments.

[References]

[1]. Rudolphi K, et al. Pralnacasan, an inhibitor of interleukin-1beta converting enzyme, reduces joint damage in two murine models of osteoarthritis. Osteoarthritis Cartilage. 2003 Oct;11(10):738-46.

[2]. Loher F, et al. The interleukin-1 beta-converting enzyme inhibitor pralnacasan reduces dextran sulfate sodium-induced murine colitis and T helper 1 T-cell activation. J Pharmacol Exp Ther. 2004 Feb;308(2):583-90.

Chemical & Physical Properties

[ Density]:
1.44g/cm3

[ Molecular Formula ]:
C26H29N5O7

[ Molecular Weight ]:
523.53800

[ Exact Mass ]:
523.20700

[ PSA ]:
150.73000

[ LogP ]:
1.76290

[ Index of Refraction ]:
1.657

Related Compounds