NV-5138-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENV-5138hydrochlorideCat.No.:HY-114384B分?式:C?H??ClF?NO?分?量:217.64作?靶點(diǎn):mTOR作?通路:PI3K/Akt/mTOR儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(1148.69mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM4.5947mL22.9737mL45.9474mL5mM0.9189mL4.5947mL9.1895mL10mM0.4595mL2.2974mL4.5947mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(9.56mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(9.56mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(9.56mM);ClearsolutionBIOLOGICALACTIVITY?物活性NV-5138hydrochloride?種亮氨酸類似物，?個(gè)具有選擇性的、?服活性的腦內(nèi)的mTORC1的激動(dòng)劑，與Sestrin2結(jié)合。NV-5138hydrochloride可?于抗抑郁的?物研究。IC50&TargetmTORC1[1].體內(nèi)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