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当前位置： 首页 > 产品中心 > Small_molecule > Medchemexpress/Senicapoc（同义词：ICA-17043）/HY-50694/10mg
商品详细Medchemexpress/Senicapoc（同义词：ICA-17043）/HY-50694/10mg
Medchemexpress/Senicapoc（同义词：ICA-17043）/HY-50694/10mg
Medchemexpress/Senicapoc（同义词：ICA-17043）/HY-50694/10mg
商品编号： HY-50694-10mM*1mLinDMSO
品牌： MedChemExp
市场价： ¥2380.00
美元价： 1428.00
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
SenicapocisapotentandselectiveGardoschannelblockerwithIC50valueof11nM,andblocksCa2+-inducedrubidiumfluxfromhumanRBCswithanIC50valueof11nMandinhibitsRBCdehydrationwithIC50of30nM.

CustomerValidation

  • •Haematologica.2017Oct;102(10):e415-e418.
  • •EurJPharmacol.2017Jan15;795:1-7.
Description

SenicapocisapotentandselectiveGardoschannelblockerwithIC50valueof11nM,andblocksCa2+-inducedrubidiumfluxfromhumanRBCswithanIC50valueof11nMandinhibitsRBCdehydrationwithIC50of30nM.

IC50&Target

IC50:11nM(Gardoschannel)

InVitro

ICA-17043isshowntoblocktheGardoschannelofmouse(C57Black)RBCswithanIC50of50±6nM.ICA-17043blocksthisincreaseincellularhemoglobinconcentrationinhumanRBCsinaconcentration-dependentfashion[1].

InVivo

ICA-17043 (10mg/kg,p.o.)admiNISTrationproducesasignificantdecreaseinGardoschannelactivitymeasuredatday11and21andisassociatedwithacorrespondingincreaseinredcellK+contentwithoutchangesinNa+content.ICA-17043(10mg/kg,twiceaday)inducesasignificantincreaseinHctafter11daysofdosingintheSADmouse[1].Senicapoc(30mg/kg,p.o.)reducesairwayhyperresponsiveness,eosinophilnumbersinbronchoalveolarlavagetaken48hourspost-allergenchallenge,andvascularremodellinginthesheep[2].

ClinicalTrial
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References

  • [1].StockerJW,etal.ICA-17043,anovelGardoschannelblocker,preventssickledredbloodcelldehydrationinvitroandinvivoinSADmice.Blood.2003Mar15;101(6):2412-8.

    [2].VanDerVeldenJ,etal.K(Ca)3.1channel-blockadeattenuatesairwaypathophysiologyinasheepmodelofchronicasthma.PLoSOne.2013Jun24;8(6):e66886.

    [3].StaalRG,etal.InhibitionofthepotassiumchannelKCa3.1bysenicapocreversestactileallodyniainratswithperipheralnerveinjury.EurJPharmacol.2017Jan15;795:1-7.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM3.0927mL15.4636mL30.9272mL
5mM0.6185mL3.0927mL6.1854mL
10mM0.3093mL1.5464mL3.0927mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
CellAssay
[1]

SenicapocisdissolvedinDMSOor100%ethanol.

Thewholebloodisinitiallydiluted1:1withModifiedFluxBuffer(MFB),consistingof140mMNaCl,5mMKCl,10mMTris(tris(hydroxymethyl)aminomethane),0.1mMEGTA(ethyleneglycoltetraaceticacid)(pH=7.4).Thebloodiscentrifugedat1000rpm,andthepelletcomprisedprimarilyofRBCsiswashed3timeswithMFB.Thecellsarethenloadedwith 86Rb+ byincubatingthewashedcellswith86Rb+ atafinalconcentrationof0.185MBq/mL(5μCi/mL)inMFBforatleast3hoursat37°C.AfterloADIngwith86Rb+,theRBCsarewashed3timeswithchilledMFB.Thecellsarethenincubatedfor10minuteswithtestcompound(senicapoc)atconcentrationsthatrangedfrom1nMto10000nM.Effluxof 86Rb+ isinitiatedbyraisingintracellularcalciumlevelsintheRBCswiththeadditionofCaCl2 andA23187(acalciumionophore)tofinalconcentrationsof2mMand5μM,respectively.After10minutesofincubationatroomtemperature,theRBCsarepelletedinamicrocentrifuge,andthesupernatantisremovedandcountedinaWallacMicroBetaliquidscintillationcounter. MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

AnimalAdministration
[1]

Senicapocisdissolvedinacremophore/PEG-400/water(10:10:80)mixture.

TransgenicHbbsingle/single SAD1(SAD)femaleandmalemice between3and6monthsofage,weighing25to30g,areusedforthisstudy.TheSADmicearedividedinto2groups,andeithervehicle(n=6)orsenicapoc(10mg/kg)(n=6)isadministeredorallybygavagetwicedaily.C57B6/2Jmiceareusedascontrols(wild-typemice).Hematologicparametersareevaluatedatbaselineandafter11and21daysoftherapy.Bloodsamplingandvehicleadministrationhavepreviouslybeenshownnottoaffectthebloodparametersmeasuredinthisstudy.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.

References

  • [1].StockerJW,etal.ICA-17043,anovelGardoschannelblocker,preventssickledredbloodcelldehydrationinvitroandinvivoinSADmice.Blood.2003Mar15;101(6):2412-8.

    [2].VanDerVeldenJ,etal.K(Ca)3.1channel-blockadeattenuatesairwaypathophysiologyinasheepmodelofchronicasthma.PLoSOne.2013Jun24;8(6):e66886.

    [3].StaalRG,etal.InhibitionofthepotassiumchannelKCa3.1bysenicapocreversestactileallodyniainratswithperipheralnerveinjury.EurJPharmacol.2017Jan15;795:1-7.

MolecularWeight

323.34

Formula

C₂₀H₁₅F₂NO

CASNo.

289656-45-7

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

RoomtemperatureincontinentalUS;mayvaryelsewhere

Solvent&Solubility

10mMinDMSO

Senicapocisformulatedwith20%2-Hydroxypropyl-β-cyclodextrinasasUSPension[3].

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

References

  • [1].StockerJW,etal.ICA-17043,anovelGardoschannelblocker,preventssickledredbloodcelldehydrationinvitroandinvivoinSADmice.Blood.2003Mar15;101(6):2412-8.

    [2].VanDerVeldenJ,etal.K(Ca)3.1channel-blockadeattenuatesairwaypathophysiologyinasheepmodelofchronicasthma.PLoSOne.2013Jun24;8(6):e66886.

    [3].StaalRG,etal.InhibitionofthepotassiumchannelKCa3.1bysenicapocreversestactileallodyniainratswithperipheralnerveinjury.EurJPharmacol.2017Jan15;795:1-7.

Purity:99.83%