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主营：抑制剂、激动剂、API
℡ 4000-520-616
℡ 4000-520-616
Medchemexpress/Riociguat(Synonyms: BAY 632521)/HY-14779/200mg
产品编号：HY-14779-10mM*1mLinDMSO
市  场 价：¥1580.00
场      地：美国(厂家直采)
联系QQ：1570468124
电话号码：4000-520-616
邮      箱： info@ebiomall.com
美  元  价：$79.00
品      牌： MCE
公      司：Medchemexpress
公司分类：
Medchemexpress/Riociguat(Synonyms: BAY 632521)/HY-14779/200mg
商品介绍
Riociguatisanoralstimulatorofsolubleguanylatecyclase(sGC),andusedinthetreatmentofpulmonaryhypertension.
Description

Riociguatisanoralstimulatorofsolubleguanylatecyclase(sGC),andusedinthetreatmentofpulmonaryhypertension.

InVitro

RiociguastimulatestherecombinantsGCconcentrationdependentlyfrom0.1to100 μMwithatwo-foldto73-foldeffectbyanNO-independentbuthaem-dependentmechanism[1]. Riociguatinhibitsplateletfunctioninwashedplateletsbutnotinwholeblood,andexertsnodirecteffectsoncontractilityandrelaxationofcardiacmyocytes[2].

InVivo

Riociguat(10mg/kg/d,p.o.)partiallyreversesthepulmonaryarterialhypertension,therighthearthypertrophyandthestructuralremodellingofthelungvasculatureinchronictreatmentofhypoxicmiceandMCT-injectedrats[1].

ClinicalTrial
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References

  • [1].SchermulyRT,etal.Expressionandfunctionofsolubleguanylatecyclaseinpulmonaryarterialhypertension.EurRespirJ.2008Oct;32(4):881-91.

    [2].SchermulyRT,etal.Riociguatforthetreatmentofpulmonaryhypertension.ExpertOpinInvestigDrugs.2011Apr;20(4):567-76.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.3673mL11.8366mL23.6731mL
5mM0.4735mL2.3673mL4.7346mL
10mM0.2367mL1.1837mL2.3673mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
AnimalAdmiNISTration
[1]

Riociguatisformulatedin2%methylcellulose.

Mice[1]
Forchronicinterventionstudiesfourgroupsofmiceareused:controlmiceexposedfor35daystonormoxicgas(n=10);miceexposedfor21daystohypoxicgas(n=10);miceexposedfor35daystohypoxicgasandwhoreceivesthevehicle(2%methylcellulosesolution)fromday21today35(n=10);andmiceexposedfor35daystohypoxicgasandwhoreceivesBAY63-2521(10mg/kg)onceadaybyoralapplication(n=10)fromday21today35.Forcontinuousmeasurementof Prvs andcardiacfrequencybyrADIotelemetry,aseparategroupofmiceisexposedfor35daystohypoxicgasandreceivesBAY63-2521(10mg/kg)onceadaybyoralapplicationfromday21today35.Inordertoinvestigatevascularreactivityinisolatedmouselungs,anadditionaltwogroupsofanimalsareinvestigated:controlmice(n=12)andanimalsexposedfor21daystohypoxicconditions(n=12).
Rat[1]
RatsarerandomisedforchronicBAY63-2521treatment,21daysafterMCTinjection.TheexperimentalgroupsincludesratsthatreceivesBAY63-2521(10mg/kg)orvehicle(2%methylcellulosesolution)byoralapplication,onceperday.Ratsareexamineddailyandsubjectedtohaemodynamicmeasurementsandhistologicalassessmentatday35.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].SchermulyRT,etal.Expressionandfunctionofsolubleguanylatecyclaseinpulmonaryarterialhypertension.EurRespirJ.2008Oct;32(4):881-91.

    [2].SchermulyRT,etal.Riociguatforthetreatmentofpulmonaryhypertension.ExpertOpinInvestigDrugs.2011Apr;20(4):567-76.

MolecularWeight

422.42

Formula

C₂₀H₁₉FN₈O₂

CASNo.

625115-55-1

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:99.73%