CCG258208-hydrochloride-GRK2-IN-1-hydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECCG258208hydrochlorideCat.No.:HY-109562ASynonyms:GRK2-IN-1hydrochloride分?式:C??H??ClFN?O?分?量:488.94作?靶點(diǎn):GProtein-coupledReceptorKinase(GRK)作?通路:GPCR/GProtein儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(511.31mM;Needultrasonic)H2O:50mg/mL(102.26mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.0452mL10.2262mL20.4524mL5mM0.4090mL2.0452mL4.0905mL10mM0.2045mL1.0226mL2.0452mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.25mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(4.25mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.25mM);Clearsolution4.請(qǐng)依序添加每種溶劑：PBSSolubility:50mg/mL(102.26mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性CCG258208(GRK2-IN-1)hydrochloride?種強(qiáng)效和選擇性的GRK2(G蛋?偶聯(lián)受體激酶2)抑制劑(IC50=30nM)，對(duì)GRK5(IC50=7.09μM)顯?出230倍的選擇性，對(duì)GRK1(IC50=87.3μM)、PKA和ROCK1有超過2500倍的選擇性。CCG258208hydrochloride可?于?衰的研究。IC50&TargetGRK2GRK530nM(IC50)7.1μM(IC50)體外研究CCG258208(Compound14as)(0-1μM;10min)showssignificantimprovementinβAR-stimulatedcontractilityinmousecardiomyocytes[1].CellViabilityAssay[1]CellLine:MousecardiomyocytesConcentration:0,0.1,0.5,and1μMIncubationTime:10minResult:Showedasignificantincreaseincontractilityataconcentrationofonly0.1μM.體內(nèi)研究CCG258208(Compound14as)(intraperitonealinjection;10mg/kg;once)treatmentshowssuperiorhalf-lifeinvivo[1].AnimalModel:CD-1mice[1]Dosage:10mg/kgAdministration:Intraperitonealinjection;10mg/kg;onceResult:ShowedtotalplasmadruglevelsaftersingleIPadministrationthatexceedtheGRK2IC50forsevenhours.REFERENCES[1].WaldschmidtHV,etal.Structure-BasedDesignofHighlySelectiveandPotentGProtein-CoupledReceptorKinase2InhibitorsBasedonParoxetine.JMedChem.2017Apr13;60(7):3052-3069.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplicati