PKG-drug-G1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPKGdrugG1Cat.No.:HY-112197CASNo.:374703-78-3分⼦式:C₁₃H₁₁N₃OS分⼦量:257.31作⽤靶点:Others作⽤通路:Others储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:75mg/mL(291.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.8864mL19.4318mL38.8636mL5mM0.7773mL3.8864mL7.7727mL10mM0.3886mL1.9432mL3.8864mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性PKGdrugG1靶向作⽤于PKGIα。PKGdrugG1通过C42PKGIα⾮依赖性机制有助于⾎管舒张和⾎压降低。IC50&TargetPKGIα[1]体内研究PKGdrugG1inducesvasodilationofisolatedresistancebloodvesselsandbloodpressureloweringina1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师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.户使⽤本产品发表的科研⽂献•NatCommun.2022Aug4;13(1):4537.•ResearchSquarePreprint.2022Jan.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BurgoyneJR,etal.ProofofPrincipleforaNovelClassofAntihypertensivesThatTargettheOxidativeActivationofPKGIα(ProteinKinaseGIα).Hypertension.2017Sep;70(3):577-586.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedical