Exemestane-13C-d2-FCE-24304-sup-13-sup-C-d-sub-2-sub-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEExemestane-13C,d2Cat.No.:HY-13632S5Synonyms: FCE24304-13C,d2;EXE-13C,d2分子式: C₁₉₁₃CH₂₂D₂O₂分子量: 299.41作用靶点: CytochromeP450;Isotope-LabeledCompounds作用通路: MetabolicEnzyme/Protease;Others储存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Exemestane-13C,d2是13C和氘代标记的Exemestane(HY-13632)。Exemestane(FCE24304)是一种选择性，不可逆和具有口服活性的甾体芳香酶(aromatase)抑制剂，对人胎盘和大鼠卵巢芳香酶的IC50分别为30nM和40nM。Exemestane可用于激素依赖性乳腺癌研究。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].Exemestane(EXE;1-1000nM;72hours;hFOB,Saos-2cells[3].?Exemestane(72hours)increasesalkalinephosphataseactivityinhFOBandSaos-2cellsandinducestheexpressionofMYBL2,OSTM1,HOXD11,ADCYAP1R1,andglypican2inhFOBcells[3].?Exemestanecompetitivelyinhibitsandtime-dependentlyinactivatesofhumanplacentalaromatasewithKiof4.3nM.Exemestanedisplaces[3H]5α-dihydrotestosteronefromratprostateandrogenreceptorwithIC50of0.9μM[2].体内研究Exemestane(EXE;20-100mg/kg;intramuscularinjection;onceweekly;for16weeks)treatmentsignificantlyincreasesthelumbarvertebralandfemoralBMD,bendingstrengthofthefemur,compressivestrengthofthefifthlumbarvertebra,andtrabecularbonevolume.Exemestanesignificantlyreducesanovariectomy-inducedincreaseinserumpyridinolineandserumosteocalcin.Exemestanecausessignificantreductionsofserumcholesterolandlow-densitylipoproteincholesterol[4].?Exemestane(20mg/kg/days.c.)induces26%complete(CR)and18%partial(PR)tumorregressionsinratswith7,12-dimethylbenzanthracene(DMBA)-inducedmammarytumors[5].REFERENCES1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEDiSalle,E.,etal.,Novelaromataseand5alpha-reductaseinhibitors.JSteroidBiochemMolBiol,1994.49(4-6):p.289-94.Miki,Y,etal.Effectsofaromataseinhibitorsonhumanosteoblastandosteoblast-likecells:apossibleandrogenicboneprotectiveeffectsinducedbyexemestane.Bone.2004Sep1;10(17):5717-23.Goss,P.E.,etal.,Effectsofthesteroidalaromataseinhibitorexemestaneandthenonsteroidalaromataseinhibitorletrozoleonboneandlipidmetabolisminovariectomizedrats.ClinCancerRes,2004.10(17):p.5717-23.Zaccheo,T.,D.Giudici,andE.DiSalle,InhibitoryeffectofcombinedtreatmentwiththearomataseinhibitorexemestaneandtamoxifenonDMBA-inducedmammarytumorsinrats.JSteroidBiochemMolBiol,1993.44(4-6):p.677-80.RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor