HPi1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemEHPi1Cat.No.:HY-120536CASNo.:13080-21-2分⼦式:C₈H₈N₄S分⼦量:192.24作⽤靶点:Bacterial作⽤通路:Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:62.5mg/mL(325.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM5.2018mL26.0092mL52.0183mL5mM1.0404mL5.2018mL10.4037mL10mM0.5202mL2.6009mL5.2018mL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，并请注意储备液的保存⽅式和期限。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案，配制前请先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的⼯作液，建议您现⽤现配，当天使⽤；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分⽐指该溶剂在您配制终溶液中的体积占⽐)：1.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(10.82mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性HPi1⼀种针对幽门螺杆(Helicobacterpylori)的有效，选择性和具有⼝服活性的抗剂，IC50为0.24μ1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemEM，MIC为0.08-0.16μg/mL。HPi1对其他细⽆活性，包括肠道⼲酪乳杆，罗伊⽒乳杆和长双歧杆菌。IC50&TargetIC50:0.24μM(Helicobacterpylori)[1]MIC:0.08-0.16μg/mL(Helicobacterpylori)[1]体外研究TheMICagainstH.pyloriisolatesrangedfrom0.002-0.032μg/mL(0.01-0.17μM)intheagardilutionassay.HPi1iseffectiveagainsttheclarithromycin-resistantstrainsARHp172(MICof0.004–0.016μg/mL)andARHp246(MICof0.008–0.032μg/mL)[1].HPi1hassomeactivityagainsttheBacteroidesspecies,butatconcentrationsatleast18-foldhigherthantheH.pyloriMIC.MorepotentactivityisdetectedforCampylobacterjejuniwithanMICof0.3μg/mL[1].HPi1hasgoodphysicochemicalandpharmacologicalproperties,includingdeterminingtheaqueoussolubility(19μg/mL),humanplasmaproteinbinding(93%bound),stabilitywithhumanlivermicrosomes(T1/2of1.3hours)andtheabilitytopassivelypermeatemembranes[1].体内研究HPi1(6.25-50mg/kg;Oralgavage;onceaday;for3days;femaleC57BL/6mice)treatmentdecreasescolonycountsbelowthelimitofdetectionatdosesof25or50mg/kg/day[1].AnimalModel:Adultspecific-pathogen-freefemaleC57BL/6mice(6-8-week-old)fedwithH.pyloriSS1suspension[1]Dosage:6.25mg/kg,12.5mg/kg,25mg/kg,50mg/kgAdministration:Oralgavage;onceaday;for3daysResult:Reducedcolonycountstobelowthelimitofdetection.REFERENCES[1].GavrishE,etal.InvitroandinvivoactivitiesofHPi1,aselectiveantimicrobialagainstHelicobacterpylori.AntimicrobAgentsChemother.2014Jun;58(6):3255-60.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For