BiologicalActivity
Verypotentandselective,non-competitiveantagonistofthehumanglucagonreceptor(hGR).BindswithhighaffinitytohumanGR(IC50=3.7nM),andmoderateaffinitytomurineandcanineGRs(IC50valuesare63and60nMrespectively).Incontrast,displayspooraffinityforrat,guineapig,andrabbitglucagonreceptors(IC50>1μM).Infunctionalstudies,inhibitsglucagon-stimulatedcAMPsynthesisinCHOcellsexpressinghGR(IC50=41nM),andinmurinelivermembranes.Orallyactiveinvivo.
CompoundLibraries
L-168,049isalsoofferedaspartoftheTocriscreenPlus.FindoutmoreaboutcompoundlibrariesavailablefromTocris.
TechnicalData
| M.Wt | 467.79 |
| Formula | C24H20BrClN2O |
| Storage | StoreatRT |
| Purity | ≥99%(HPLC) |
| CASNumber | 191034-25-0 |
| PubChemID | 5311276 |
| InChIKey | HHBOWXZOLYQFNY-UHFFFAOYSA-N |
| Smiles | CCCOC1=C(C=C(Br)C=C1)C1=C(NC(=C1)C1=CC=C(Cl)C=C1)C1=CC=NC=C1 |
Thetechnicaldataprovidedaboveisforguidanceonly.ForbatchspecificdatarefertotheCertificateofAnalysis.
AllTocrisproductsareintendedforlaboratoryresearchuseonly.
SolubilityData
| Solvent | MaxConc.mg/mL | MaxConc.mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 46.78 | 100 | |
| ethanol | 46.78 | 100 |
PreparingStockSolutions
Thefollowingdataisbasedontheproductmolecularweight467.79.Batchspecificmolecularweightsmayvaryfrombatchtobatchduetosolventofhydration,whichwillaffectthesolventvolumesrequiredtopreparestocksolutions.
| Concentration/SolventVolume/Mass | 1mg | 5mg | 10mg |
|---|---|---|---|
| 1mM | 2.14mL | 10.69mL | 21.38mL |
| 5mM | 0.43mL | 2.14mL | 4.28mL |
| 10mM | 0.21mL | 1.07mL | 2.14mL |
| 50mM | 0.04mL | 0.21mL | 0.43mL |
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