Hydrochlorothiazide-15N2-13C-d2-HCTZ-sup-15-sup-N-sub-2-sub-sup-13-sup-C-d-sub-2-sub-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEHydrochlorothiazide-15N2,13C,d2Cat.No.:HY-B0252S3CASNo.:2140316-81-8Synonyms:HCTZ-15N2,13C,d2分子式:C₆₁₃CH₆D₂ClN₁₅N₂O₄S₂分子量:302.73作用靶点:PotassiumChannel;TGF-beta/Smad;Isotope-LabeledCompounds作用通路:MembraneTransporter/IonChannel;StemCell/Wnt;TGF-beta/Smad;Others储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Hydrochlorothiazide-15N2,13C,d2是15N和氘代标记的Hydrochlorothiazide(HY-B0252)。Hydrochlorothiazide(HCTZ)是一种口服有效的噻嗪类的利尿药，可抑制转化TGF-β/Smad信号通路。Hydrochlorothiazide通过打开钙激活钾(KCA)通道具有直接的血管松弛作用。Hydrochlorothiazide改善心脏功能，减少纤维化并具有降压作用。体外研究Stableheavyisotopesofhydrogen,carbon,andotherelementshavebeenincorporatedintodrugmolecules,largelyastracersforquantitationduringthedrugdevelopmentprocess.Deuterationhasgainedattentionbecauseofitspotentialtoaffectthepharmacokineticandmetabolicprofilesofdrugs[1].Hydrochlorothiazidebelongstothiazideclassofdiuretics.Itreducesbloodvolumebyactingonthekidneystoreducesodium(Na)reabsorptioninthedistalconvolutedtubule.ThemajorsiteofactioninthenephronappearsonanelectroneutralNa+-Clco-transporterbycompetingforthechloridesiteonthetransporter.ByimpairingNatransportinthedistalconvolutedtubule,hydrochlorothiazideinducesanatriuresisandconcomitantwaterloss.Thiazidesincreasethereabsorptionofcalciuminthissegmentinamannerunrelatedtosodiumtransport.Additionally,byothermechanisms,Hydrochlorothiazideisbelievedtolowerperipheralvascularresistance[2].体内研究Hydrochlorothiazide(HCTZ;orallybygavage;12.5mg/kg/d;8weeks)hasimprovedcardiacfunction,reducedcardiacinterstitialfibrosisandcollagenvolumefraction,decreasedexpressionofAT1,TGF-βandSmad2inthecardiactissuesinadultmaleSpragueDawleyrats.Inaddition,hydrochlorothiazidereducesplasmaangiotensinIIandaldosteronelevels.Furthermore,hydrochlorothiazideinhibitsangiotensinII-inducedTGF-1/2 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEβ1andSmad2proteinexpressionintheneonatalratventricularfibroblasts[3].REFERENCESMagdyMAbdelquader,etal.InhibitionofCo-CrystallizationofOlmesartanMedoxomilandHydrochlorothiazideforEnhancedDissolutionRateinTheirFixedDoseCombination.AAPSPharmSciTech.2018Dec17;20(1):3.Duarte,J.D.andR.M.Cooper-DeHoff,Mechanismsforbloodpressureloweringandmetaboliceffectsofthiazideandthiazide-likediuretics.ExpertRevCardiovascTher,2010.8(6):p.793-802.JinghongLuo,etal.Hydrochlorothiazidemodulatesischemicheartfailure-inducedcardiacremodelingviainhibitingangiotensinIItype1receptorpathwayinrats.CardiovascTher.2017Apr;35(2).RussakEM,etal.ImpactofDeuteriumSubstitutiononthePharmacokineticsofPharmaceuticals.AnnPharmacother.2019Feb;53(2):211-216.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfor