请使用支持JavaScript的浏览器! Medchemexpress/Raloxifene hydrochloride(Synonyms: LY156758 hydrochloride)/HY-13738A/100mg_蚂蚁淘,【正品极速】生物医学科研用品轻松购|ebiomall 蚂蚁淘商城
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Medchemexpress/Raloxifene hydrochloride(Synonyms: LY156758 hydrochloride)/HY-13738A/100mg
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Medchemexpress/Raloxifene hydrochloride(Synonyms: LY156758 hydrochloride)/HY-13738A/100mg
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4000-520-616
RaloxifeneHcl(LY156758Hcl)isasecondgenerationselectiveestrogenreceptorantagoNIST.
Description

RaloxifeneHcl(LY156758Hcl)isasecondgenerationselectiveestrogenreceptorantagonist.Target:EstrogenreceptorApproved:September14,2007RaloxifeneactivatesTGFbeta3promoterasafullagonistatnanomolarconcentrations,andraloxifeneinhibitstheestrogenresponseelement-containingvitellogeninpromoterexpressionasapureestrogenantagonistintransienttransfectionassays[1].Raloxifene,hasbeendemonstratedasapotentuncompetitiveinhibitorofhumanliveraldehydeoxidase-catalyzedoxidationofphthalazine,vanillin,andnicotine-Delta1"(5")-iminiumion,withKivaluesof0.87nM,1.2nMand1.4nM.Raloxifenehasalsobeenshowntobeanoncompetitiveinhibitorofanaldehydeoxidase-catalyzedreductionreactionofahydroxamicacid-containingcompound,withaKiof51nM[2].Raloxifene(3mg/kg/day)haspotentestrogenicactivityonboneresorptionandserumcholesterol,alessereffectonboneformation,andminimalactivityonuterinewetweightinovariectomized(OVX)rats.[3].Raloxifene(0.1mg/kg-10mg/kg,orallyfor5weeks)increasesbonemineraldensityinthedistalfemurandproximaltibiainovariectomized(OVX)rat.RaloxifenereducesserumcholesteroloralwithED50of0.2mg/kginovariectomized(OVX)rat.Raloxifenedivergesdramaticallyfromestrogeninitslackofsignificantestrogeniceffectsonuterinetissue[4].RaloxifenepreventscancellousosteopeniaaswellasthechangesinrADIalbonegrowth,boneresorption,andbloodcholesterol,butislesseffectiveinreducingcancellousboneformationanddoesnotpreventuterineatrophyinovariectomized(OVX)rats[5].

ClinicalTrial
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References
  • [1].Yang,N.N.,etal.,Estrogenandraloxifenestimulatetransforminggrowthfactor-beta3geneexpressioninratbone:apotentialmechanismforestrogen-orraloxifene-mediatedbonemaintenance.Endocrinology,1996.137(5):p.2075-84.

    [2].Obach,R.S.,Potentinhibitionofhumanliveraldehydeoxidasebyraloxifene.DrugMetabDispos,2004.32(1):p.89-97.

    [3].Sato,M.,M.K.Rippy,andH.U.Bryant,Raloxifene,tamoxifen,nafoxidine,orestrogeneffectsonreproductiveandnonreproductivetissuesinovariectomizedrats.FASEBJ,1996.10(8):p.905-12.

    [4].Black,L.J.,etal.,Raloxifene(LY139481HCI)preventsbonelossandreducesserumcholesterolwithoutcausinguterinehypertrophyinovariectomizedrats.JClinInvest,1994.93(1):p.63-9.

    [5].Evans,G.,etal.,Theeffectsofraloxifeneontibiahistomorphometryinovariectomizedrats.Endocrinology,1994.134(5):p.2283-8.

PreparingStockSolutions
ConcentrationVolumeMass1mg5mg10mg
1mM1.9606mL9.8032mL19.6063mL
5mM0.3921mL1.9606mL3.9213mL
10mM0.1961mL0.9803mL1.9606mL
Pleaserefertothesolubilityinformationtoselecttheappropriatesolvent.
References
  • [1].Yang,N.N.,etal.,Estrogenandraloxifenestimulatetransforminggrowthfactor-beta3geneexpressioninratbone:apotentialmechanismforestrogen-orraloxifene-mediatedbonemaintenance.Endocrinology,1996.137(5):p.2075-84.

    [2].Obach,R.S.,Potentinhibitionofhumanliveraldehydeoxidasebyraloxifene.DrugMetabDispos,2004.32(1):p.89-97.

    [3].Sato,M.,M.K.Rippy,andH.U.Bryant,Raloxifene,tamoxifen,nafoxidine,orestrogeneffectsonreproductiveandnonreproductivetissuesinovariectomizedrats.FASEBJ,1996.10(8):p.905-12.

    [4].Black,L.J.,etal.,Raloxifene(LY139481HCI)preventsbonelossandreducesserumcholesterolwithoutcausinguterinehypertrophyinovariectomizedrats.JClinInvest,1994.93(1):p.63-9.

    [5].Evans,G.,etal.,Theeffectsofraloxifeneontibiahistomorphometryinovariectomizedrats.Endocrinology,1994.134(5):p.2283-8.

MolecularWeight

510.04

Formula

C₂₈H₂₈ClNO₄S

CASNo.

82640-04-8

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:99.64%