BiologicalActivity
PotentandselectiveinhibitoroftheTGF-βtypeIreceptor/ALK5(IC50=2.5nM).Exhibits~5000-foldselectivityoverp38MAPK.Suppressesdevelopmentofrenalfibrosisinaunilateralureteralobstructionmodel.Alsoreducesproteinuria,glomerulosclerosisandimprovesrenalfunctioninananti-Thy1glomerulonephritismodel.Orallybioavailable.
CompoundLibraries
R268712isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 363.39 |
| Formula | C20H18FN5O |
| Storage | Storeat-20°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 879487-87-3 |
| PubChemID | 11703284 |
| InChIKey | JQGOCCALXFSRHZ-UHFFFAOYSA-N |
| Smiles | OCCN1N=CC(C2=C(F)C=CC(C3=CNN=C3C4=CC=CC(C)=N4)=C2)=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 36.34 | 100 | |
| ethanol | 18.17 | 50 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight363.39.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.75mL | 13.76mL | 27.52mL |
| 5mM | 0.55mL | 2.75mL | 5.5mL |
| 10mM | 0.28mL | 1.38mL | 2.75mL |
| 50mM | 0.06mL | 0.28mL | 0.55mL |
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ProductDatasheets
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