BiologicalActivity
PotentNLRP3inflammasomeinhibitor;inhibitsIL-1β(IC50=7.2nM),IL-1α(IC50=12-18nM)andIL-18(IC50=10.3nM)production.SelectiveforNLRP3inflammasomeoverNLRC4inflammasomeandToll-likereceptorsignaling.InhibitsinflammasomeactivationbysolubleandcrystallineNLRP3stimuli.Reducesseverityofexperimentalautoimmuneencephalomyelitis,skininflammationandairwayinflammationinmice.AlsoglutathioneS-transferaseomega1inhibitor.Orallybioavailable.
LicensingInformation
SoldforresearchpurposesunderagreementfromPfizerInc
TechnicalData
| M.Wt | 426.46 |
| Formula | C20H23N2NaO5S |
| Storage | Storeat+4°C |
| Purity | ≥97%(HPLC) |
| CASNumber | 256373-96-3 |
| PubChemID | 91826093 |
| InChIKey | LFQQNXFKPNZRFT-UHFFFAOYSA-M |
| Smiles | O=C(N(S(C4=CC(C(C)(O)C)=CO4)(=O)=O)[Na])NC1=C3C(CCC3)=CC2=C1CCC2 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.65 | 100 | |
| water | 42.65 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight426.46.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.34mL | 11.72mL | 23.45mL |
| 5mM | 0.47mL | 2.34mL | 4.69mL |
| 10mM | 0.23mL | 1.17mL | 2.34mL |
| 50mM | 0.05mL | 0.23mL | 0.47mL |
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