EST64454-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEST64454hydrochlorideCat.No.:HY-131914ACASNo.:1950569-11-5分⼦式:C₁₈H₂₃ClF₂N₄O₂分⼦量:400.85作⽤靶点:SigmaReceptor作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(249.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.4947mL12.4735mL24.9470mL5mM0.4989mL2.4947mL4.9894mL10mM0.2495mL1.2473mL2.4947mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(6.24mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.24mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.24mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性EST64454hydrochloride⼀种选择性且具有⼝服活性的sigma-1受体拮抗剂，Ki为22nM。EST64454hydrochloride具有研究疼痛的潜⼒。体内研究EST64454(10mg/kg;p.o.;maleWistarrats)treatmentshowstheCmax,t1/2,AUC0-∞,VssandF%are771ng/mL,3.4hours,1431ngh/mL,4.4l/kgand69%,respectively[1].EST64454(10mg/kg;p.o.;maleCD1mice)treatmentshowstheCmax,t1/2,AUC0-∞,VssandF%were1178ng/mL,[1].AnimalModel:MaleWistarrats(250-300g)[1]Dosage:10mg/kgAdministration:P.o.(PharmacokineticAnalysis)Result:TheCmax,t1/2,AUC0-∞,VssandF%were771ng/mL,3.4hours,1431ngh/mL,4.4l/kgand69%,respectively.REFERENCES[1].DíazJL,etal.EST64454:aHighlySolubleσ1ReceptorAntagonistClinicalCandidateforPainManagement.JMedChem.2020;63(23):14979-14988.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:4