BiologicalActivity
Potent,selectiveblockerofthevolume-sensitiveanionchannel(VSAC)inratpancreaticβ-cells(IC50~2μM)andICl,swellinvariouscardiovasculartissues(IC50=4.1μMinCPAEcells);blockadeisvoltage-independent.DisplaysminimalinhibitionofotherCl-andK+currents(<10%inhibitionat10μM).Inhibitsglucose-stimulatedinsulinsecretioninintactβ-cellsviaVSACinhibitionandindirectKATPchannelactivation.Reversescellswelling-inducedactionpotentialdurationshorteninginatrialmyocytesandinhibitsastroglialswellinginvitro.
TechnicalData
| M.Wt | 427.37 |
| Formula | C22H28Cl2O4 |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 82749-70-0 |
| PubChemID | 10071166 |
| InChIKey | KHKGTPJPBOQECW-UHFFFAOYSA-N |
| Smiles | CCCCC1(CC2=C(C1=O)C(Cl)=C(Cl)C(OCCCC(O)=O)=C2)C1CCCC1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| ethanol | 42.74 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight427.37.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.34mL | 11.7mL | 23.4mL |
| 5mM | 0.47mL | 2.34mL | 4.68mL |
| 10mM | 0.23mL | 1.17mL | 2.34mL |
| 50mM | 0.05mL | 0.23mL | 0.47mL |
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