BiologicalActivity
PotentandselectiveTRPV4antagonist(IC50valuesare2and40nMforratandhumanreceptors,respectively);inhibitsCa2+influxthroughTRPV4channels.Preventsandreversespulmonaryedemaaftermyocardialinfarctioninvivomodels.Selectiveoverapanelof~200humanreceptors,channelsandenzymes.Orallyactive.
LicensingInformation
SoldforresearchpurposesunderagreementfromGlaxoSmithKline
CompoundLibraries
GSK2193874isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 691.62 |
| Formula | C37H38BrF3N4O |
| Storage | Storeat+4°C |
| CASNumber | 1336960-13-4 |
| PubChemID | 53464483 |
| InChIKey | UIVOZBSCHXCGPS-UHFFFAOYSA-N |
| Smiles | O=C(NC6(CC6)C5=CC=CC=C5)C2=C(CN4CCC(N7CCCCC7)CC4)C(C3=CC(C(F)(F)F)=CC=C3)=NC1=CC(Br)=CC=C12 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| 1eq.HCl | 13.83 | 20 | |
| DMSO | 34.58 | 50 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight691.62.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.45mL | 7.23mL | 14.46mL |
| 5mM | 0.29mL | 1.45mL | 2.89mL |
| 10mM | 0.14mL | 0.72mL | 1.45mL |
| 50mM | 0.03mL | 0.14mL | 0.29mL |
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ProductDatasheets
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