[CAS NO. 192755-52-5] Pralnacasan
PRODUCTS SPECIFICATIONS [192755-52-5]
DESCRIPTION [192755-52-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 523.54 |
| Molecular Formula | C26H29N5O7 |
| SMILES | O=C([C@@H]1CCCN2N1C([C@@H](NC(C3=NC=CC4=C3C=CC=C4)=O)CCC2=O)=O)N[C@@H](C5)[C@H](OCC)OC5=O |
Summary
Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a K i 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] .
IC50 & 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 220 mg/mL ( 420.22 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9101 mL | 9.5504 mL | 19.1007 mL |
| 5 mM | 0.3820 mL | 1.9101 mL | 3.8201 mL |
| 10 mM | 0.1910 mL | 0.9550 mL | 1.9101 mL |
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.