BiologicalActivity
Antifibroticagent;inhibitsfibrosisbytargetingtheMRTF/SRFgenetranscriptionpathway.SelectivelyinhibitsproliferationofSSc-deriveddermalfibroblastsbutnotthatofnormalfibroblasts.InhibitsexpressionofCTGF,α-SMA,andCOL1A2inSScfibroblastsaswellasinLPAandinTGFβ-stimulatedfibroblasts.Preventsbleomycin-inducedskinthickeningandcollagendepositioninvivo.AlsosuppressesPC-3cellmigrationinscratchwoundassays(IC50=4.2μM).
TechnicalData
| M.Wt | 408.88 |
| Formula | C23H21ClN2O3 |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 1443437-74-8 |
| PubChemID | 71681561 |
| InChIKey | HERLZBNILRVHQN-UHFFFAOYSA-N |
| Smiles | O=C(N2CCCC(C(NC3=CC=C(Cl)C=C3)=O)C2)C1=CC=CC(C4=CC=CO4)=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 20.44 | 50 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight408.88.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.45mL | 12.23mL | 24.46mL |
| 5mM | 0.49mL | 2.45mL | 4.89mL |
| 10mM | 0.24mL | 1.22mL | 2.45mL |
| 50mM | 0.05mL | 0.24mL | 0.49mL |
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