PotentandselectiveGPERagonist(Ki=11nM,EC50=2nM);displaysnoactivityatERαandERβatconcentrationsupto10μM.IncreasescytosolicCa2+andinhibitsmigrationofSKBr3cellsandMCF-7cellsinresponsetochemoattractants(IC50valuesare0.7and1.6nMrespectively)invitro.BlocksMCF-1cellcycleprogressionattheG1phase.DisplaystherapeuticeffectsinthemouseEAEmodelofmultiplesclerosis.
M.Wt | 412.28 |
Formula | C21H18BrNO3 |
Storage | Storeat-20°C |
Purity | ≥98%(HPLC) |
CASNumber | 881639-98-1 |
PubChemID | 5322399 |
InChIKey | VHSVKVWHYFBIFJ-HKZYLEAXSA-N |
Smiles | CC(C5=CC([C@@]4([H])[C@@]([H])3CC=C4)=C(C=C5)N[C@H]3[C@]1=CC(OCO2)=C2C=C1Br)=O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Solvent | MaxConc.mg/mL | MaxConc.mM | |
---|---|---|---|
Solubility | |||
DMSO | 41.23 | 100 |
Thefollowingdataisbasedontheproductmolecularweight412.28.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
---|---|---|---|
1mM | 2.43mL | 12.13mL | 24.26mL |
5mM | 0.49mL | 2.43mL | 4.85mL |
10mM | 0.24mL | 1.21mL | 2.43mL |
50mM | 0.05mL | 0.24mL | 0.49mL |