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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Macitentan(Synonyms: ACT-064992)/HY-14184/10mg
商品详细Medchemexpress/Macitentan(Synonyms: ACT-064992)/HY-14184/10mg
Medchemexpress/Macitentan(Synonyms: ACT-064992)/HY-14184/10mg
Medchemexpress/Macitentan(Synonyms: ACT-064992)/HY-14184/10mg
商品编号： HY-14184-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥1300.00
美元价： 780.00
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
Macitentanisanorallyactive,non-peptidedualendothelinETAandETBreceptorantagoNISTforthepotentialtreatmentofidiopathicpulmonaryfibrosis(IPF)andpulmonaryarterialhypertension(PAH).
Description

Macitentanisanorallyactive,non-peptidedualendothelinETAandETBreceptorantagonistforthepotentialtreatmentofidiopathicpulmonaryfibrosis(IPF)andpulmonaryarterialhypertension(PAH).

InVitro

TubeformationABIlityisrestoredwhenmicrovascularendothelialcellsarepreincubatedwithBOSormacitentan,alsoreducingtheexpressionofmesenchymalMarkersandrestoringCD31expressionandtheimbalancebetweenVEGF-AandVEGF-A165b[1].MacitentaninhibitsOATP1B1-mediateduptakeofatorvastatinandOATP1B3-mediateduptakeofestrone-3-sulfatewithIC50 ± SEvaluesof6.3 ± 0.7and11.8 ± 5.0 μM,respectively[3].TreatmentwithmacitentanorwithACT-132577doesnotleadtointracellularaccumulationofR123inHeyA8-MDR,showingthatthesecompoundsarenotP-gpinhibitors[4].

InVivo

Macitentan(25mg/kg/day,p.o.)preventsincreasedproductionofvasoactiveandfibrogenicfactors,NF-κBactivation,structuralandfunctionalchanges,andincreasesextracellularmatrixproteinproductionintype2diabetesintype2diabetes[2].Macitentan(10mg/kg,p.o.)coupledwithonce-per-week5mg/kgtaxol,significantlyreducestheweight(size)ofHeyA8-MDRtumorsinmice.Combinationtherapywithmacitentan(10or50mg/kg,butnot5mg/kg)andtaxolormacitentan(10mg/kg)andcisplatinumsignificantlyreducesthenumberofproliferatingKi-67-positivecells[4].

ClinicalTrial
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References

  • [1].CoralloC,etal.Bosentanandmacitentanpreventtheendothelial-to-mesenchymaltransition(EndoMT)insystemicsclerosis:invitrostudy.ArthritisResTher.2016Oct6;18(1):228.

    [2].SenS,etal.Renal,retinalandcardiacchangesintype2diabetesareattenuatedbymacitentan,adualendothelinreceptorantagonist.LifeSci.2012Apr13.

    [3].BrudererS,etal.Effectofcyclosporineandrifampinonthepharmacokineticsofmacitentan,atissue-targetingdualendothelinreceptorantagonist.AAPSJ.2012Mar;14(1):68-78.

    [4].KimSJ,etal.Antivasculartherapyformultidrug-resistantovariantumorsbymacitentan,adualendothelinreceptorantagonist.TranslOncol.2012Feb;5(1):39-47.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.6999mL8.4995mL16.9990mL
5mM0.3400mL1.6999mL3.3998mL
10mM0.1700mL0.8499mL1.6999mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
AnimalAdministration
[2]

Macitentanispreparedinfoodadmix.

Maledb/dbmiceandageandsex-matchedcontrols(27-32 g)areusedfortheassay.RandomLyselecteddiabeticanimalsaremonitoredforeither2 monthsorfor4 monthsafteronsetofdiabetes.Groups(n=7/group)ofthediabeticmicearesubjectedtooralmacitentantreatmentforthesameperiod(25 mg/kg/day,foodadmix).Theanimalsaremonitoredthroughassessmentofbodyweightandbloodglucose.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].CoralloC,etal.Bosentanandmacitentanpreventtheendothelial-to-mesenchymaltransition(EndoMT)insystemicsclerosis:invitrostudy.ArthritisResTher.2016Oct6;18(1):228.

    [2].SenS,etal.Renal,retinalandcardiacchangesintype2diabetesareattenuatedbymacitentan,adualendothelinreceptorantagonist.LifeSci.2012Apr13.

    [3].BrudererS,etal.Effectofcyclosporineandrifampinonthepharmacokineticsofmacitentan,atissue-targetingdualendothelinreceptorantagonist.AAPSJ.2012Mar;14(1):68-78.

    [4].KimSJ,etal.Antivasculartherapyformultidrug-resistantovariantumorsbymacitentan,adualendothelinreceptorantagonist.TranslOncol.2012Feb;5(1):39-47.

MolecularWeight

588.27

Formula

C₁₉H₂₀Br₂N₆O₄S

CASNo.

441798-33-0

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:99.95%