ML-SI3-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEML-SI3Cat.No.:HY-139426CASNo.:891016-02-7分⼦式:C₂₃H₃₁N₃O₃S分⼦量:429.58作⽤靶点:TRPChannel作⽤通路:MembraneTransporter/IonChannel;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(116.39mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3279mL11.6393mL23.2786mL5mM0.4656mL2.3279mL4.6557mL10mM0.2328mL1.1639mL2.3279mL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>>90%cornoilSolubility:≥2.5mg/mL(5.82mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性ML-SI3⼀种TRPML通道抑制剂。ML-SI3可阻断TRPML1和TRPML2，IC50s分别为4.7µM和1.7µM。ML-SI3抑制溶酶体钙外流并阻断下游TRPML1介导的⾃噬。IC50&TargetTRPML1TRPML2TRPML34.7μM(IC50)1.7μM(IC50)12.5μM(IC50)体外研究ML-SI3(10μM)inhibitsML-SA1-evokedCa2+signalsinHeLacells[2].ML-SI3(25-75μM,24h)disruptstegumentalintegrityofadultschistosomes[3].ML-SI3(10μM)blocksRapamycin(HY-10219)-evokedITRPML1inmimicoflysosomallumen[4].ML-SI3(3µM,6h)abolishestheincreaseinbothLC3IIandp62levelsinducedbyhypoxia/reoxygenation(H/R)(4hH/2hR)inneonatalratventricularmyocytes(NRVM)[5].体内研究ML-SI3(1.5mg/kg,i.p.,fourtimes)attenuatesI/Rinjuryinmousecardiomyocytes[5].AnimalModel:MyocardialIschemia/reperfusion(I/R)injurymice[5]Dosage:1.5mg/kgAdministration:Intraperitonealinjection(i.p.),fourtimesbeforeandduringtheinvivoI/R(ischemia30minandreperfusion1day)Result:RestoredtheblockedautophagicfuxinthecardiomyocytessubjectedtoI/R.REFERENCES[1].RühlP,etal.Estradiolanalogsattenuateautophagy,cellmigrationandinvasionbydirectandselectiveinhibitionofTRPML1,independentofestrogenreceptors.SciRep.2021Apr15;11(1):8313.[2].KilpatrickBS,etal.Endo-lysosomalTRPmucolipin-1channelstriggerglobalERCa2+releaseandCa2+influx.JCellSci.2016Oct15;129(20):3859-3867.[3].BaisS,etal.SchistosomeTRPMLchannelsplayaroleinneuromuscularactivityandtegumentalintegrity.Biochimie.2022Mar;194:108-117.[4].ZhangX,etal.RapamycindirectlyactivateslysosomalmucolipinTRPchannelsindependentofmTOR.PLoSBiol.2019May21;17(5):e3000252.[5].XingY,etal.BluntingTRPML1channelsprotectsmyocardialischemia/reperfusioninjurybyrestoringimpairedcardiomyocyteautophagy.BasicResCardiol.2022Apr7;117(1):20.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical