BiologicalActivity
Potent,selectiveandcompetitivecorticotropin-releasingfactorCRF2receptorantagonist(Kdvaluesare1.4and153.6nMforbindingtomouseCRF2βandratCRF1receptorsrespectively).Inhibitssauvagine-stimulatedcAMPaccumulationinHEK-mCRF2βcells(pA2=8.49).Preventsstress-enhancedfearconditioningandMEK1/2-dependentactivationofERK1/2inmiceinvivo.
LicensingInformation
SoldwiththepermissionoftheMaxPlanckInstitute
TechnicalData
| M.Wt | 3650.29 |
| Formula | C161H274N48O46S |
| Sequence | FHLLRKMIEIEKQEKEKQQAANNRLLLDTI (Modifications:Phe-1=D-Phe,Ile-30=C-terminalamide) |
| Storage | Desiccateat-20°C |
| CASNumber | 220673-95-0 |
| PubChemID | 16138449 |
| InChIKey | INBLUEDNNZCTNZ-JBNJRNGTSA-N |
| Smiles | [H]N[C@H](CC1=CC=CC=C1)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCSC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H]([C@@H](C)CC)C(N)=O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solubility | Solubleto1mg/mlinwater |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight3650.29.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 0.27mL | 1.37mL | 2.74mL |
| 5mM | 0.05mL | 0.27mL | 0.55mL |
| 10mM | 0.03mL | 0.14mL | 0.27mL |
| 50mM | 0.01mL | 0.03mL | 0.05mL |

