PKG-drug-G1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPKGdrugG1Cat.No.:HY-112197CASNo.:374703-78-3分?式:C??H??N?OS分?量:257.31作?靶點:Others作?通路:Others儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:75mg/mL(291.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.8864mL19.4318mL38.8636mL5mM0.7773mL3.8864mL7.7727mL10mM0.3886mL1.9432mL3.8864mL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；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性PKGdrugG1靶向作?于PKGIα。PKGdrugG1通過C42PKGIα?依賴性機制有助于?管舒張和?壓降低。IC50&TargetPKGIα[1]體內(nèi)研究PKGdrugG1inducesvasodilationofisolatedresistancebloodvesselsandbloodpressureloweringina1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEmousemodelofangiotensinII–inducedhypertension.PKGdrugG1efficientlyrelaxesWTbutnotknockin(KI)vessels,whichisthenassessedinamurinemodelofhypertension.PKGdrugG1lowersbloodpressureinhypertensiveWT,butnotKI,miceinvivo.PKGdrugG1istestedinvivoinhealthymiceimplantedwithtelemetricdevicesthatallowbloodpressureandheartratetobeconstantlymonitored.PKGdrugG1orvehiclecontrolisadministratedbyintraperitonealinjection,andtheacuteimpactonhemodynamicsassessed.PKGdrugG1administeredat7.4mg/kgdoesnotdecreasebloodpressure,butthereisaconcomitantreflextachycardia.Whenthisisrepeatedusing14.8mg/kgdoseofPKGdrugG1,againbloodpressureisnotaltered-butthishigherdoseinducesapotentiatedincreaseinheartrate[1].PROTOCOLAnimalMice[1]Administration[1]MiceconstitutivelyexpressingPKGIαCys42SeraregeneratedonapureC57BL/6background.Age-matchedandbodyweight–matchedWTorPKGIαCys42SerKImalemiceareusedinallstudies.Bloodpressureandheartrateareassessedbyradiotelemetryinconsciousfreelymovingmice.Alzetosmoticmini-pumpsareusedtodeliverangiotensinIIat1.1mg/kgperdayinsomestudies.PKGdrugG1isdeliveredintraperitoneally(3.7-14.8mg/kg)ororally(20mg/kg)insomestudies.TodeliverPKGdrugG1orally,withoutstressorriskofdislodgingthetelemetricprobecatheter,itisprovidedsuspendedinwaterandsetingelatinflavoredwithsodiumsaccharin[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻?NatCommun.2022Aug4;13(1):4537.?ResearchSquarePreprint.2022Jan.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BurgoyneJR,etal.ProofofPrincipleforaNovelClassofAntihypertensivesThatTargettheOxidativeActivationofPKGIα(ProteinKinaseGIα).Hypertension.2017Sep;70(3):577-586.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical