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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/盐酸维拉帕米（同义词：（±）-盐酸维拉帕米）/HY-A0064/10mM*1mL二甲基亚砜
商品详细Medchemexpress/盐酸维拉帕米（同义词：（±）-盐酸维拉帕米）/HY-A0064/10mM*1mL二甲基亚砜
Medchemexpress/盐酸维拉帕米（同义词：（±）-盐酸维拉帕米）/HY-A0064/10mM*1mL二甲基亚砜
Medchemexpress/盐酸维拉帕米（同义词：（±）-盐酸维拉帕米）/HY-A0064/10mM*1mL二甲基亚砜
商品编号： HY-A0064-10mM*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
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商品介绍
VerapamilhydrochlorideisanL-typecalciumchannelantagoNIST.
Description

VerapamilhydrochlorideisanL-typecalciumchannelantagonist.

IC50&Target

Calciumchannel[1]

InVitro

Verapamil(hydrochloride)isanL-typecalciumchannelantagonist.ThecombinationofBortezomibandVerapamil(70µM)markedlydeclinestheviABIlityoftheJK-6L,RPMI8226,andARH-77celllinesafter16hoursofculture[1].Theenzymehydrolaseactivityofrecombinanthumancarboxylesterase(CES2)issubstantiallyinhibitedbyVerapamilwithKiof3.84±0.99μM[2].

InVivo

Verapamil,acalciumchannelantagonist,isinjectedi.v.intoafemoralveinpriortoischemia.Verapamil(1mg/kg)significantlydecreasestheincidenceofventriculararrhythmiasincludingprematureventricularcontractions(PVC),ventriculartachycardia(VT)andventricularfibrillation(VF)for45-mincoronaryarteryocclusion.Totalarrhythmiascoresaresignificantlyincreasedwhentheheartissubjectedtoischemia(P<0.01 vs.="" sham).="" verapamil="" (1="" mg/kg)="" significantly="" prevented="" the="" enhancement="" of="" total="" arrhythmia="" scores="" induced="" by="" ischemia=""><0.01 vs.="" ischemia).="" results="" indicate="" that="" verapamil="" exerts="" an="" anti-arrhythmic="">[3].

References

  • [1].MeisterS,etal.CalciumchannelblockerVerapamilenhancesendoplasmicreticulumstressandcelldeathinducedbyproteasomeinhibitioninmyelomacells.Neoplasia.2010Jul;12(7):550-61.

    [2].YanjiaoX,etal.Evaluationoftheinhibitoryeffectsofantihypertensivedrugsonhumancarboxylesteraseinvitro.DrugMetabPharmacokinet.2013;28(6):468-74.

    [3].ZhouP,etal.Anti-arrhythmiceffectofVerapamilisaccompaniedbypreservationofcx43proteininratheart.PLoSOne.2013Aug12;8(8):e71567.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM2.0364mL10.1821mL20.3641mL
5mM0.4073mL2.0364mL4.0728mL
10mM0.2036mL1.0182mL2.0364mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

VerapamilisdissolvedinDMSOandstored,andthendilutedwithappropriatemediabeforeuse[1].

Cells(1×105)aretreatedwith10nMBortezomiband/or70µMVerapamilfor16hoursandincubatedforanother4hourswithAlamar-Blue.Activityofthemitochondrialdehydrogenaseresultsinconversionofthecoloring,whichisfollowedbymeasurementoftheabsorptionusingaspectrophotometer[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[3]

VerapamilhydrochlorideisdissolvedinDMSOandthendilutedwithPBSorsaline[3].

Rat[3]
AdultmaleSprague-Dawley(SD)rats(250−350g)areused.Verapamil(1mg/kg)isinjectedi.v.intoafemoralvein10minpriortoischemia.Ashamgroupundergoesthesamesurgicalprocedures,exceptthesutureunderneaththeLADisleftuntied.Inanotherseriesofexperiment,arrhythmiaisinducedbyBayK8644,anL-typecalciumchannelagonist,atadoseof0.1mg/kggiveni.v.intotheFV.Verapamil(1mg/kg)isadministered10minpriortoBayK8644.Allinjectionsareperformedwithin30sec.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].MeisterS,etal.CalciumchannelblockerVerapamilenhancesendoplasmicreticulumstressandcelldeathinducedbyproteasomeinhibitioninmyelomacells.Neoplasia.2010Jul;12(7):550-61.

    [2].YanjiaoX,etal.Evaluationoftheinhibitoryeffectsofantihypertensivedrugsonhumancarboxylesteraseinvitro.DrugMetabPharmacokinet.2013;28(6):468-74.

    [3].ZhouP,etal.Anti-arrhythmiceffectofVerapamilisaccompaniedbypreservationofcx43proteininratheart.PLoSOne.2013Aug12;8(8):e71567.

MolecularWeight

491.06

Formula

C₂₇H₃₉ClN₂O₄

CASNo.

152-11-4

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

DMSO:≥31mg/mL

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

Purity:99.97%