NV-5138-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENV-5138hydrochlorideCat.No.:HY-114384B分⼦式:C₇H₁₄ClF₂NO₂分⼦量:217.64作⽤靶点:mTOR作⽤通路:PI3K/Akt/mTOR储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:250mg/mL(1148.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM4.5947mL22.9737mL45.9474mL5mM0.9189mL4.5947mL9.1895mL10mM0.4595mL2.2974mL4.5947mL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:≥2.08mg/mL(9.56mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(9.56mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(9.56mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性NV-5138hydrochloride⼀种亮氨酸类似物，⾸个具有选择性的、⼝服活性的脑内的mTORC1的激动剂，与Sestrin2结合。NV-5138hydrochloride可⽤于抗抑郁的⽣物研究。IC50&TargetmTORC1[1].体内研究NV-5138isfoundtobeessentially100%orallybioavailablewithaneliminationhalf-lifeinplasmaof~3hdeterminedfollowingintravenousandoraldosinginrats[1].NV-5138(160mg/kg,po,singledose)rapidlyincreaseslevelsofphospho-mTORaswellasthedownstreamtargets,phospho-p70S6K1,andphosphor-4EB-P1,insynaptosomalpreparationsofPFC[2].NV-5138(80mg/kg,po,dailyforatotalof7days)alsoproducesantidepressanteffects[2].AnimalModel:MaleSprague-Dawleyratsweighing250-260g[2].Dosage:40,80,160mg/kg.Administration:PO,singledose(160mg/kg)ordailyforatotalof7days(40,80mg/kg).Result:Producedantidepressanteffects.AnimalModel:MaleSprague-Dawley(SD)ratsweighed250-400g[1].Dosage:1mg/kg,5mg/kg(PharmacokineticDesign).Administration:I.Vat1mg/kgandPOat5mg/kg.Result:Essentially100%orallybioavailablewithaneliminationhalf-lifeinplasmaof~3h.REFERENCES[1].SenguptaS,etal.DiscoveryofNV-5138,thefirstselectiveBrainmTORC1activator.SciRep.2019Mar11;9(1):4107.[2].KatoT,etal.SestrinmodulatorNV-5138producesrapidantidepressanteffectsviadirectmTORC1activation.JClinInvest.2019Apr16;129(6):2542-2554.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F