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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Losartan potassium(Synonyms: DuP-753 potassium)/HY-17512A/5g
商品详细Medchemexpress/Losartan potassium(Synonyms: DuP-753 potassium)/HY-17512A/5g
Medchemexpress/Losartan potassium(Synonyms: DuP-753 potassium)/HY-17512A/5g
Medchemexpress/Losartan potassium(Synonyms: DuP-753 potassium)/HY-17512A/5g
商品编号： HY-17512A-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1320.00
美元价： 792.00
产地： 美国(厂家直采)
公司：
产品分类： 小分子
公司分类： Small_molecule
联系Q Q： 3392242852
电话号码： 4000-520-616
电子邮箱： info@ebiomall.com
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商品介绍
Losartan(potassium)isanangiotensinIIreceptorantagoNIST,competingwiththebindingofangiotensinIItoAT1receptorswithIC50of20nM.
Description

Losartan(potassium)isanangiotensinIIreceptorantagonist,competingwiththebindingofangiotensinIItoAT1receptorswithIC50of20nM.

IC50&Target

IC50:20nM(angiotensinII)

InVitro

LosartancompeteswiththebindingofangiotensinIItoAT1receptors.Theconcentrationthatinhibits50%ofthebindingofangiotensinII(IC50)is20nM[1].Losartan(40 μM)affectsISCbutpreventstheeffectofANGIIonISC[2].LosartansignificantlyreducesAngII-mediatedcellproliferationinendometrialcancercells.Thecombinationoflosartanandanti-miR-155hasasignificantlygreaterantiproliferativeeffectcomparedtoeachdrugalone[3].

InVivo

Losartan(0.6g/L,p.o.)-treatedFbn1C1039G/+miceshowareductionindistalairspacecaliberrelativetoplacebo-treatedFbn1C1039G/+animals.Thedosesoflosartanandpropranololaretitratedtoachievecomparablehemodynamiceffects.AnalysisofpSmad2nuclearstainingrevealsthatlosartanantagonizesTGF-βsignalingintheaorticwallofFbn1C1039G/+mice.Losartancanimprovediseasemanifestationsinthelungs,aneventthatcannotplausIBLyrelatetoimprovedhemodynamics[4].Losartan(10mg/kg,intraarterialinjection)increasesbloodangiotensinlevelsfour-tosixfold.Losartan(10mg/kg,i.p.)increasesplasmareninlevels100-fold;plasmaangiotensinogenlevelsdecreasesto24%ofcontrol;andplasmaaldosteronelevelsareunchanged[5].

ClinicalTrial
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References

  • [1].Burnier,M.AngiotensinIItype1receptorblockers.Circulation,2001.103(6):p.904-12.

    [2].Ashry,O.,etal.EvidenceforexpressionandfunctionofangiotensinIIreceptortype1inpulmonaryepithelialcells.RespirPhysiolNeurobiol,2014.

    [3].Choi,C.H.,etal.AngiotensinIItypeIreceptorandmiR-155inendometrialcancers:synergisticantiproliferativeeffectsofanti-miR-155andlosartanonendometrialcancercells.GynecolOncol,2012.126(1):p.124-31.

    [4].Habashi,J.P.,etal.Losartan,anAT1antagonist,preventsaorticaneurysminamousemodelofMarfansyndrome.Science,2006.312(5770):p.117-21.

    [5].Campbell,D.J.,etal.Effectsoflosartanonangiotensinandbradykininpeptidesandangiotensin-convertingenzyme.JCardiovascPharmacol,1995.26(2):p.233-40.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.1692mL10.8460mL21.6920mL
5mM0.4338mL2.1692mL4.3384mL
10mM0.2169mL1.0846mL2.1692mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[3]

AnMTTassayisusedtomeasurecellproliferationandviABIlity.Fortheassay,5000cellsin200 μLmediaperwellareseededina96wellplate.Afterovernightincubationtoallowforcellattachment,themediumisremovedbysuction.MTTat1 mg/mLconcentrationinserum-freemediumisaddedandthenincubatedfor4 hat37°C.AfterremovalofMTTsolution,100 μLofDMSOisaddedtodissolveformazancrystals.Absorbanceat570 nmandat600 nmasareferenceisthenmeasuredusingamicroplatereader.Thedifferenceinabsorbanceisthusrelativetotheextentofcellsurvival.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[4]

Losartanisformulatedinwater.

FemaleFbn1C1039G/+miceundergotimedmatingswithwild-typemalemice.At14.5dpost-coitum,pregnantfemaleFbn1C1039G/+micearetreatedwithorallosartan(0.6g/Lindrinkingwater;n=10),propranolol(0.5g/L;n=6)orplacebo(n=12).Therapyiscontinuedthroughoutlactationandafterweaninguntil10monthsofage.Micearesacrificedandexaminedusingthetechniquesdescribedabove.Propranololisusedforcomparisonwithlosartanbecauseβ-adrenergicreceptorblockadeisthecurrentalbeitcontroversialstandardofcaretomodulateabnormalgrowthoftheaorticrootinMFS.Beginningat7weeksofage,wild-typeandFbn1C1039G/+micearetreatedwithorallosartan(0.6g/Lindrinkingwater;n=5),propranolol(0.5g/L;n=7)orplacebo(n=10).Micearecontinuedonoraltherapyfor6monthsandthensacrificed.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].Burnier,M.AngiotensinIItype1receptorblockers.Circulation,2001.103(6):p.904-12.

    [2].Ashry,O.,etal.EvidenceforexpressionandfunctionofangiotensinIIreceptortype1inpulmonaryepithelialcells.RespirPhysiolNeurobiol,2014.

    [3].Choi,C.H.,etal.AngiotensinIItypeIreceptorandmiR-155inendometrialcancers:synergisticantiproliferativeeffectsofanti-miR-155andlosartanonendometrialcancercells.GynecolOncol,2012.126(1):p.124-31.

    [4].Habashi,J.P.,etal.Losartan,anAT1antagonist,preventsaorticaneurysminamousemodelofMarfansyndrome.Science,2006.312(5770):p.117-21.

    [5].Campbell,D.J.,etal.Effectsoflosartanonangiotensinandbradykininpeptidesandangiotensin-convertingenzyme.JCardiovascPharmacol,1995.26(2):p.233-40.

MolecularWeight

461.0

Formula

C₂₂H₂₂ClKN₆O

CASNo.

124750-99-8

Storage
Powder-20°C3years
 4°C2years
Insolvent-80°C6months
 -20°C1month
Shipping

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

*"<1 mg/ml"="" means="" slightly="" soluble="" or="" insoluble.="" "≥"="" means="" soluble,="" but="" saturation="">

Purity:99.91%