PotentandselectiveinhibitoroftheTGF-βtypeIreceptor/ALK5(IC50=2.5nM).Exhibits~5000-foldselectivityoverp38MAPK.Suppressesdevelopmentofrenalfibrosisinaunilateralureteralobstructionmodel.Alsoreducesproteinuria,glomerulosclerosisandimprovesrenalfunctioninananti-Thy1glomerulonephritismodel.Orallybioavailable.
R268712isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
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.
Solvent | MaxConc.mg/mL | MaxConc.mM | |
---|---|---|---|
Solubility | |||
DMSO | 36.34 | 100 | |
ethanol | 18.17 | 50 |
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 |