BiologicalActivity
Potent,orallyactiveandnon-peptidegonadotropin-releasinghormone(GnRH,LHRH)receptorantagonist(IC50valuesare0.2,4.0and60nMforhuman,monkeyandratGnRHreceptorsrespectively).InhibitsLHreleaseinvitro(IC50=100nM)andreducesplasmaLHconcentrationincastratedmalecynomolgusmonkeys.
TechnicalData
| M.Wt | 657.77 |
| Formula | C37H37F2N3O4S |
| Storage | Desiccateat+4°C |
| Purity | ≥98%(HPLC) |
| CASNumber | 199119-18-1 |
| PubChemID | 9874838 |
| InChIKey | RANJJVIMTOIWIN-UHFFFAOYSA-N |
| Smiles | CC(C)OC(=O)C1=CN(CC2=C(F)C=CC=C2F)C2=C(C(CN(C)CC3=CC=CC=C3)=C(S2)C2=CC=C(NC(=O)C(C)C)C=C2)C1=O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 32.89 | 50 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight657.77.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 1.52mL | 7.6mL | 15.2mL |
| 5mM | 0.3mL | 1.52mL | 3.04mL |
| 10mM | 0.15mL | 0.76mL | 1.52mL |
| 50mM | 0.03mL | 0.15mL | 0.3mL |
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