Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemE(S)-(-)-Bay-K-8644Cat.No.:HY-15124CASNo.:98625-26-4分?式:C??H??F?N?O?分?量:356.3作?靶點(diǎn):CalciumChannel作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(280.66mM;Needultrasonic)H2O:<0.1mg/mL(ultrasonic;warming;heatto60°C)(insoluble)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.8066mL14.0331mL28.0662mL5mM0.5613mL2.8066mL5.6132mL10mM0.2807mL1.4033mL2.8066mL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。-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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(5.84mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(7.02mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性(S)-(-)-Bay-K-8644L型鈣離?通道激動(dòng)劑。(S)-(-)-Bay-K-8644激活Ba2+電流(IBa)，EC50為32nM。IC50&TargetEC50:32nM(IBa)[1]體外研究(±)-BayK8644,aconventionalracemicmixtureofBayK8644,iswidelyusedasanL-typeCa2+channelagonist.EachopticalisomerpossessesoppositeeffectsonIBa(R(+)-BayK8644asanantagonistand(S)-(-)-Bay-K-8644asanagonist.(S)-(-)-Bay-K-8644canpreventtheinhibitoryactionsoftwodistinctcyclicnucleotidepathwaysonIBaingastricmyocytesoftheguineapigantrum[1].TheCa2+channelactivityisenhancedby3–30μM(S)-(-)-Bay-K-8644anagonistofL-typeCa2+channels[2].TheinteractionsoftwoCa2+channelactivators(S)-(-)-Bay-K-8644andFPL64176isexaminedonsmoothmuscleL-typeCa2+channels.FPL64176(300nM)causesasustainedcontractionofrattailarterystrips.Thiscontractileresponseisinhibitedbyapproximately70%by(S)-(-)-Bay-K-8644(EC50=14nM).(S)-(-)-Bay-K-8644(100nM)increaseswhole-cellCa2+currentsinA7r5smoothmusclecellsbuteffectivelyblocksfurtherstimulationby1μMFPL64176[3].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?LifeSci.2019Mar15;221:135-142.?EurJPharmacol.2020Nov5;886:173513.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhuHL,etal.AntagonisticactionsofS(-)-BayK8644oncyclicnucleotide-inducedinhibitionofvoltage-dependentBa(2+)currentsinguineapiggastricantrum.NaunynSchmiedebergsArchPharmacol.2008Dec;378(6):609-15.[2].MironovSL,etal.L-typeCa2+channelsininspiratoryneuronesofmiceandtheirmodulationbyhypoxia.JPhysiol.1998Oct1;512(Pt1):75-87.[3].RampeD,etal.FunctionalinteractionsbetweentwoCa2+channelactivators,(S)-BayK8644andFPL64176,insmoothmuscle.MolPharmacol.1992Apr;41(4):599-602.McePdfHeightCaution:Producthasnotbeenfullyvalidatedfo