192755-52-5

192755-52-5 structure

Name: Pralnacasan
Chemical Name: (4S,7S)-N-[(2R,3S)-2-ethoxy-5-oxooxolan-3-yl]-7-(isoquinoline-1-carbonylamino)-6,10-dioxo-2,3,4,7,8,9-hexahydro-1H-pyridazino[1,2-a]diazepine-4-carboxamide
CAS Number: 192755-52-5
Molecular Formula: C₂₆H₂₉N₅O₇
Molecular Weight: 523.53800
Catalog: Signaling Pathways Apoptosis Caspase
Create Date: 2017-12-05 11:41:03
Modify Date: 2024-01-12 11:05:38
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].

Name	(4S,7S)-N-[(2R,3S)-2-ethoxy-5-oxooxolan-3-yl]-7-(isoquinoline-1-carbonylamino)-6,10-dioxo-2,3,4,7,8,9-hexahydro-1H-pyridazino[1,2-a]diazepine-4-carboxamide
Synonyms	Pralnaan [INN] HMR 3480 Pralnaan Pralnaan (USAN/INN) UNII-N986NI319S

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.