Siramesine-hydrochloride-Lu-28-179-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemESiramesinehydrochlorideCat.No.:HY-14221ACASNo.:224177-60-0Synonyms:Lu28-179hydrochloride分⼦式:C₃₀H₃₂ClFN₂O分⼦量:491.04作⽤靶点:SigmaReceptor;Ferroptosis作⽤通路:NeuronalSignaling;Apoptosis储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:≥42mg/mL(85.53mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0365mL10.1825mL20.3649mL5mM0.4073mL2.0365mL4.0730mL10mM0.2036mL1.0182mL2.0365mL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(sealedstorage,awayfrommoisture)。-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%saline1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(5.09mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.09mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.09mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Siramesine(Lu28-179)hydrochloride⼀种有效的sigma-2受体激动剂。Siramesine对sigma-2受体具有亚纳尔亲和⼒(IC50=0.12nM)，并且对sigma-2受体的选择性sigma-1受体的140倍(IC50=17nM)。Siramesinehydrochloride通过线粒体的不稳定⽽不溶酶体触发细胞死亡。Siramesinehydrochloride显⽰出强⼤的抗癌活性。体外研究Siramesinehydrochloridedisplaysthebindingaffinities:IC50(sigma1)=17nM,IC50(sigma2)=0.12nM,IC50(5-HT1A)=21000nM,IC50(5-HT1A)=2000nM,IC50(D2)=800nM,IC50(alpha1)=330nM[1].Siramesine(0-50μM;8hours)hydrochlorideinducescelldeathinvariouscelllines(HaCaT,Hsc-4,HeLaandMCF-7,neuroblastomacelllineSH-SY5YandglioblastomacelllineU-87MG)[2].Siramesine(0-40μM;2-48hours)hydrochlorideactivatescaspasesinHaCaTandinU-87MGcells[2].户使⽤本产品发表的科研⽂献•JPharmacolExpTher.2015Aug;354(2):203-12.•Patent.US20220305013A1.Seemorecustomervalidationsonwww.MedChemEMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchus