BiologicalActivity
Potent,selectivenon-peptideCCR1antagonist(Ki=1nMforhumanCCR1).Exhibits250-foldselectivityforCCR1overCCR2,CCR5andCXCR4.InhibitsMIP-α/CCL3-inducedintracellularCa2+mobilization.Orallyactive;effectivelyreducesdiseaseseverityinaratmodelofmultiplesclerosis.Decreasesrenalfibrosisinamousemodelofobstructivenephropathy.
CompoundLibraries
BX471isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 434.89 |
| Formula | C21H24ClFN4O3 |
| Storage | Storeat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 217645-70-0 |
| PubChemID | 512282 |
| InChIKey | XQYASZNUFDVMFH-CQSZACIVSA-N |
| Smiles | FC1=CC=C(CN2C[C@@H](C)N(C(COC3=CC=C(Cl)C=C3NC(N)=O)=O)CC2)C=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.49 | 100 | |
| ethanol | 21.74 | 50 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight434.89.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.3mL | 11.5mL | 22.99mL |
| 5mM | 0.46mL | 2.3mL | 4.6mL |
| 10mM | 0.23mL | 1.15mL | 2.3mL |
| 50mM | 0.05mL | 0.23mL | 0.46mL |
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ProductDatasheets
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