Selective,highaffinity,non-competitiveα1Aadrenoceptorantagonist(Ki=0.35nM).ExhibitsnosignificantactivityagainstarangeofotherGPCRs,includingα2A,β1andβ2adrenoceptors.Antagonizeseffectsofphenylephrine(Cat.No.2838)onisolatedrabbitprostatemuscleinvitroandonintra-urethralpressureinrats.
M.Wt | 7283.22 |
Formula | C310H481N87O100S8 |
Sequence | LTCVTSKSIFGITTEDCPDGQNLCFKRRHYVVPKIYDSTRGCAATCPIPENYDSIHCCKTDKCNE (Modifications:Disulfidebridge:3-24,17-42,46-57,58-63) |
Storage | Storeat-20°C |
InChIKey | AOQYEPFDDFPKMV-UHFFFAOYSA-N |
Smiles | [H]N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CC(O)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CSSC[C@H](NC(=O)CNC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC3=CC=C(O)C=C3)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@@H]3CCCN3C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CC3=CC=C(O)C=C3)NC(=O)[C@H](CC3=CNC=N3)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC3=CC=CC=C3)NC2=O)C(C)C)C(C)C)[C@@H](C)CC)[C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CC3=CNC=N3)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC3=CC=C(O)C=C3)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@@H](NC(=O)[C@@H]3CCCN3C2=O)[C@@H](C)CC)[C@@H](C)CC)C(=O)N[C@H]2CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC2=O)[C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@@H](NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)C(C)C)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)O)[C@@H](C)O |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
Solubility | Solubleto1mg/mlinwater |
Thefollowingdataisbasedontheproductmolecularweight7283.22.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
---|---|---|---|
1mM | 0.14mL | 0.69mL | 1.37mL |
5mM | 0.03mL | 0.14mL | 0.27mL |
10mM | 0.01mL | 0.07mL | 0.14mL |
50mM | 0mL | 0.01mL | 0.03mL |