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.
Product information
CAS Number: 192755-52-5
Molecular Weight: 523.54
Formula: C26H29N5O7
Synonym:
VX-740
HMR 3480
Chemical Name: N-[(4S, 7S)-4-{[(2R, 3S)-2-ethoxy-5-oxooxolan-3-yl]carbamoyl}-6, 10-dioxo-octahydro-1H-pyridazino[1, 2-a][1, 2]diazepin-7-yl]isoquinoline-1-carboxamide
Smiles: CCO[C@@H]1OC(=O)C[C@@H]1NC(=O)[C@@H]1CCCN2C(=O)CC[C@H](NC(=O)C3=NC=CC4=CC=CC=C43)C(=O)N21
InChiKey: CXAGHAZMQSCAKJ-WAHHBDPQSA-N
InChi: InChI=1S/C26H29N5O7/c1-2-37-26-18(14-21(33)38-26)29-23(34)19-8-5-13-30-20(32)10-9-17(25(36)31(19)30)28-24(35)22-16-7-4-3-6-15(16)11-12-27-22/h3-4,6-7,11-12,17-19,26H,2,5,8-10,13-14H2,1H3,(H,28,35)(H,29,34)/t17-,18-,19-,26+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
References:
- 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.
- 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.
Products are for research use only. Not for human use.
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