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Pralnacasan

Cat. No. M10905
Pralnacasan Structure
Synonym:

VX-740

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Biological Activity

Pralnacasan (VX-740) is a potent, selective, non-peptide inhibitor with an oral active interleukin 1β-convertase (ICE, caspase 1) inhibitor,Ki 1.4 nM. Pralnacasan inhibits pro-inflammatory cytokines IL-18, IL-1β, and IFN-γ. Pralnacasan has the potential to be used in the study of osteoarthritis and rheumatoid arthritis.

Chemical Information
Molecular Weight 523.54
Formula C₂₆H₂₉N₅O₇
CAS Number 92755-52-5
Solubility (25°C) DMSO ≥ 200 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Christian Bauer, et al. Gut. Colitis induced in mice with dextran sulfate sodium (DSS) is mediated by the NLRP3 inflammasome

[2] Christian Bauer, et al. Dig Dis Sci. The ICE inhibitor pralnacasan prevents DSS-induced colitis in C57BL/6 mice and suppresses IP-10 mRNA but not TNF-alpha mRNA expression

[3] Florian Loher, et al. J Pharmacol Exp Ther. The interleukin-1 beta-converting enzyme inhibitor pralnacasan reduces dextran sulfate sodium-induced murine colitis and T helper 1 T-cell activation

[4] K Rudolphi, et al. Osteoarthritis Cartilage. Pralnacasan, an inhibitor of interleukin-1beta converting enzyme, reduces joint damage in two murine models of osteoarthritis

[5] Britta Siegmund, et al. IDrugs. Pralnacasan (vertex pharmaceuticals)

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Keywords: Pralnacasan, VX-740 supplier, Caspase, inhibitors, activators


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