BiologicalActivity
PotentandselectiveTRPV1antagonist.BlocksCa2+uptakebyCHOcellsexpressingTRPV1receptors(IC50valuesare0.6and0.8nMforcapsaicin(Cat.No.0462)andacid-inducedCa2+uptake,respectively).Exhibits>4000-foldselectivityforTRPV1overotherTRPchannels.Blockscapsaicin-inducedflinchresponseandcauseshyperthermiainrats.Orallyavailableandnon-CNSpenetrant.
TechnicalData
| M.Wt | 472.42 |
| Formula | C22H19F3N6O3 |
| Storage | Storeat-20°C |
| Purity | ≥97%(HPLC) |
| CASNumber | 939040-79-6 |
| PubChemID | 24858024 |
| InChIKey | TUMYQRZCVIQKOQ-UHFFFAOYSA-N |
| Smiles | NC(C(N4)=O)=NC(C4=CC=C3)=C3OC1=CC(C2=CC=C(C(F)(F)F)C=C2)=NC(NCCOC)=N1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 23.62 | 50 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight472.42.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.12mL | 10.58mL | 21.17mL |
| 5mM | 0.42mL | 2.12mL | 4.23mL |
| 10mM | 0.21mL | 1.06mL | 2.12mL |
| 50mM | 0.04mL | 0.21mL | 0.42mL |
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