BiologicalActivity
Potent,selectiveandcompetitivenon-peptideendothelinETAreceptorantagonist(Ki=48nM).Displays>1000-foldselectivityoverETBreceptors.InhibitsET-1-inducedpressorresponsefollowingoralorintravenousadministrationinvivo.InhibitsET-1-inducedlongitudinalmusclecontractioninthemousecoloninvitro.
LicensingInformation
SoldwiththepermissionofBristol-MyersSquibbCompany,subjecttoU.S.PatentNo.5,378,715andotherUSandforeignpatents
CompoundLibraries
BMS182874hydrochlorideisalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 381.88 |
| Formula | C17H19N3O3S.HCl |
| Storage | StoreatRT |
| Purity | ≥98%(HPLC) |
| CASNumber | 1215703-04-0 |
| PubChemID | 56972163 |
| InChIKey | UZZFRNZGYDOBAO-UHFFFAOYSA-N |
| Smiles | Cl.CN(C)C1=C2C=CC=C(C2=CC=C1)S(=O)(=O)NC1=C(C)C(C)=NO1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solubility | Solubleto100mMinDMSO |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight381.88.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.62mL | 13.09mL | 26.19mL |
| 5mM | 0.52mL | 2.62mL | 5.24mL |
| 10mM | 0.26mL | 1.31mL | 2.62mL |
| 50mM | 0.05mL | 0.26mL | 0.52mL |
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ProductDatasheets
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