EST73502-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEST73502hydrochlorideCat.No.:HY-134189ACASNo.:2535970-65-9分⼦式:C₁₉H₂₇ClF₂N₂O₂分⼦量:388.88作⽤靶点:SigmaReceptor;OpioidReceptor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:50mg/mL(128.57mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5715mL12.8574mL25.7149mL5mM0.5143mL2.5715mL5.1430mL10mM0.2571mL1.2857mL2.5715mL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(6.43mM);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(6.43mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.43mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性EST73502hydrochloride⼀种选择性的，具有⼝服活性的，可透过⾎脑屏障的μ-opioid受体(μ-opioidreceptor/MOR)激动剂和σ1受体(σ1R)拮抗剂，对MOR和σ1R作⽤的Ki值分别为64nM和118nM。EST73502hydrochloride可⽤于缓解疼痛研究[1]。IC50&TargetKi:64nM(MOR),118nM(σ1R)[1]体内研究EST73502hydrochloride(10-40mg/kg;p.o.)showsadose-responseanalgesiceffectreachingamaximumof64%andanEC50of14mg/kginthepawpressuretestinCD1malemice[1].EST73502hydrochloride(5mg/kg;i.p.;twiceaday;for10days)attenuatespartialsciaticnerveligation(PSNL)-inducedmechanicalallodyniainmaleCD1mice[1].AnimalModel:MaleCD1mice,PSNLmodel[1]Dosage:5mg/kgAdministration:Intraperitonealinjection,twiceaday,for10daysResult:AttenuatedtheexpressionofmechanicalallodyniainducedbyPSNL,reachingamaximaleffectof56%.REFERENCES[1].MónicaGarcía,etal.DiscoveryofEST73502,aDualμ-OpioidReceptorAgonistandσ1ReceptorAntagonistClinicalCandidatefortheTreatmentofPain.JMedChem.2020Oct16.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuse