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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/盐酸阿米洛利（同义词：MK-870盐酸盐）/HY-B0285A/500mg
商品详细Medchemexpress/盐酸阿米洛利（同义词：MK-870盐酸盐）/HY-B0285A/500mg
Medchemexpress/盐酸阿米洛利（同义词：MK-870盐酸盐）/HY-B0285A/500mg
Medchemexpress/盐酸阿米洛利（同义词：MK-870盐酸盐）/HY-B0285A/500mg
商品编号： HY-B0285A-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1320.00
美元价： 792.00
产地： 美国(厂家直采)
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产品分类： 小分子
公司分类： Small_molecule
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商品介绍
Amiloride(hydrochloride)isarelativelyselectiveinhibitoroftheepithelialsodiumchannel(ENaC),usedinthemanagementofhypertensionandcongestiveheartfailure.
Description

Amiloride(hydrochloride)isarelativelyselectiveinhibitoroftheepithelialsodiumchannel(ENaC),usedinthemanagementofhypertensionandcongestiveheartfailure.

InVitro

AmilorideblocksδβγchannelswithanIC50of2.6μM.TheKiofamilorideforδβγENaCis26-foldthatofαβγchannels(0.1μMforαβγENaC).AmilorideblockadeofδβγENaCismuchmorevoltagedependentcomparedwiththeαβγchannel.TheKiofamilorideforδαβγchannelsis920and13.7μMat−120and+80mV,respectively,whichsignificantlydiffersfromthatofbothαβγandδβγchannels[1].Amilorideisarelativelyselectiveinhibitoroftheepithelialsodiumchannel(ENaC)withanIC50(theconcentrationrequiredtoreach50%inhibitionofanionchannel)intheconcentrationrangeof0.1to0.5μM.AmilorideisarelativelypoorinhibitorofthetheNa+/H+exchanger(NHE)withanIC50aslowas3μMinthepresenceofalowexternal[Na+]butashighas1mMinthepresenceofahigh[Na+].AmilorideisanevenweakerinhibitoroftheNa+/Ca2+exchanger(NCX),withanIC50of1mM.Amiloride(1μM)andsubmicromolardosesofBenzamil(30nM),dosesknowntoinhibittheENaC,inhibitthemyogenicvasoconstrictionresponsetoincreasingperfusionpressurebyblockingtheactivityofENaCproteins.AmiloridecompletelyinhibitsNa+influxindosesknowntoberelativelyspecificforENaC(1.5μM)invascularsmoothmusclecells(VSMC)[2].

InVivo

Amiloride(1mg/kg/day)subcutaneouslyisfoundtoreversetheinitialincreasesincollagendepositionandpreventanyfurtherincreasesintheDOCA-salthypertensiverat.Amiloridedelaystheonsetofproteinuriaandimprovedbrainandkidneyhistologicscoresinthesaline-drinking,stroke-pronespontaneouslyhypertensiverats(SHRSP)comparedwithcontrols.Amilorideantagonizesorpreventsactionsofaldosteroneinthesecellsandincardiovascularandrenaltissuesinanimalswithsalt-dependentformsofhypertension[2]. 

ClinicalTrial
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References

  • [1].Ji,H.L.,etal.deltaENaC:anoveldivergentamiloride-inhibitablesodiumchannel.AmJPhysiolLungCellMolPhysiol,2012.303(12):p.L1013-26.

    [2].TeiwesJ,etal.Epithelialsodiumchannelinhibitionincardiovasculardisease.Apotentialroleforamiloride.AmJHypertens.2007Jan;20(1):109-17.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM3.7581mL18.7906mL37.5813mL
5mM0.7516mL3.7581mL7.5163mL
10mM0.3758mL1.8791mL3.7581mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
References

  • [1].Ji,H.L.,etal.deltaENaC:anoveldivergentamiloride-inhibitablesodiumchannel.AmJPhysiolLungCellMolPhysiol,2012.303(12):p.L1013-26.

    [2].TeiwesJ,etal.Epithelialsodiumchannelinhibitionincardiovasculardisease.Apotentialroleforamiloride.AmJHypertens.2007Jan;20(1):109-17.

MolecularWeight

266.09

Formula

C₆H₉Cl₂N₇O

CASNo.

2016-88-8

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥90mg/mL

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

Purity:>98.0%