BiologicalActivity
Highaffinity,potentinhibitorofhumanleukocyteelastase(HLE)(IC50=3.9nM).Displaysspecies-selectivity(Kivaluesare0.017,1.70,3.01,58and>100nM forhuman,mouse,rat,rabbitandporcineelastaserespectively).InhibitsHLE-inducedlunghemorrhageinmice(ID50=2.8mg/kg)andreducesinfarctsizeinaninvivoacutemodelofcoronaryischemia-reperfusioninjury.Orallyactive.
TechnicalData
| M.Wt | 556.63 |
| Formula | C27H32N4O7S |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 344930-95-6 |
| PubChemID | 9872438 |
| InChIKey | DRZXDZYWZSKFDL-UHFFFAOYSA-N |
| Smiles | COC1=CC(C(C)C)=C2C(=O)N(COC3=CC(=O)N4C=CC=C(OCCN5CCCCC5)C4=N3)S(=O)(=O)C2=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 13.92 | 25 | |
| ethanol | 5.57 | 10 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight556.63.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.8mL | 8.98mL | 17.97mL |
| 5mM | 0.36mL | 1.8mL | 3.59mL |
| 10mM | 0.18mL | 0.9mL | 1.8mL |
| 50mM | 0.04mL | 0.18mL | 0.36mL |
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