Methyclothiazide-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEMethyclothiazideCat.No.:HY-B0562CASNo.:135-07-9分?式:C?H??Cl?N?O?S?分?量:360.24作?靶點:CarbonicAnhydrase作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:72mg/mL(199.87mM;Needultrasonicandwarming)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.7759mL13.8796mL27.7593mL5mM0.5552mL2.7759mL5.5519mL10mM0.2776mL1.3880mL2.7759mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。BIOLOGICALACTIVITY?物活性Methyclothiazide?種?服降壓試劑(antihypertensive)和利尿劑(diureticagent)。Methyclothiazide減少內(nèi)性?管收縮刺激(如，去甲腎上腺素:HY-13715)引起的?管反應。Methyclothiazide拮抗體外的電壓依賴性鈣通道的(VDCC)活性。IC50&TargetIC50:voltage-dependentCa-channel(VDCC)1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE體外研究Methyclothiazide(0-100μM)inducesendothelium-dependentinhibitionofthevasoconstrictorresponsestoNEandAVPonlyinaortasfromSHR,andthemaximalvasoconstrictiveeffectofNorepinephrine(HY-13715)andargininevasopressin(AVP)isdecreasedby59%and32.3%,respectively[1].Methyclothiazide(0-100μM)inducesinhibitoryeffectonthecontractileresponsetoNorepinephrine(HY-13715)isabolishedbyN-nitro-L-arginine(NOLA)butnotindomethacin[1].Methyclothiazide(100μM)affectsthevascularresponsestoextracellularCa2+underhigh-K+depolarizingconditions.ItcanreduceCa2+contractureinahigh-K+,Ca2+-freesolution.Themaximalcontractureisreducedby90.4%[1].REFERENCES[1].Colas,B.,etal.,Mechanismsofmethyclothiazide-inducedinhibitionofcontractileresponsesinrataorta.EurJPharmacol,2000.408(1):p.63-7.[2].Colas,B.,etal.,Directvascularactionsofmethyclothiazideandindapamideinaortaofspontaneouslyhypertensiverats.FundamClinPharmacol,2000.14(4):p.363-8.[3].Sasaki,S.andR.D.Bunag,Methyclothiazideattenuatessalt-inducedhypertensionwithoutaffectingsympatheticresponsivenessinDahlrats.JCardiovascPharmacol,1983.5(3):p.378-83.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseon