Ivermectin-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEIvermectinCat.No.:HY-15310CASNo.:70288-86-7分?式:C??H??O??分?量:875.09作?靶點(diǎn):Parasite;HIV;Mitophagy;HSV;SARS-CoV;Antibiotic;Autophagy作?通路:Anti-infection;Autophagy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:≥50mg/mL(57.14mM)掃描?維碼，H2O:0.1mg/mL(0.11mM;Needultrasonic)運(yùn)?溶解?案計(jì)算器*"≥"meanssoluble,butsaturationunknown.獲得適合您實(shí)驗(yàn)體系的溶解?案MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.1427mL5.7137mL11.4274mL5mM0.2285mL1.1427mL2.2855mL10mM0.1143mL0.5714mL1.1427mL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，并請(qǐng)注意儲(chǔ)備液的保存?式和期限。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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶1.請(qǐng)依序添加每種溶劑：10%DMSO40%PEG3005%Tween-8045%salineSolubility:≥2.5mg/mL(2.86mM);Clearsolution此?案可獲得≥2.5mg/mL(2.86mM，飽和度未知)的澄溶液。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到400μLPEG300中，混合均勻；向上述1/3www.MedChemEwww.MedChemE2.體系中加?50μLTween-80，混合均勻；然后繼續(xù)加?450μL?理鹽?定容?1mL。請(qǐng)依序添加每種溶劑：10%DMSO90%cornoilSolubility:≥2.08mg/mL(2.38mM);Clearsolution此?案可獲得≥2.08mg/mL(2.38mM，飽和度未知)的澄溶液，此?案不適?于實(shí)驗(yàn)周期在半個(gè)?以上的實(shí)驗(yàn)。以1mL?作液為例，取100μL20.8mg/mL的澄DMSO儲(chǔ)備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性Ivermectin(MK-933)?種?譜的抗寄??藥物。Ivermectin(MK-933)?種特異性的Impα/β1介導(dǎo)的核導(dǎo)?抑制劑，對(duì)HIV-1和登?熱病毒都具有很強(qiáng)的抗病毒活性。Ivermectin(MK-933)也P2X4和α7nAChRs的正異構(gòu)效應(yīng)物。Ivermectin還可抑制?疹病毒1(BoHV-1)復(fù)制并抑制BoHV-1DNA聚合酶的核輸?。Ivermectin應(yīng)?于抗SARS-CoV-2/COVID-19的候選藥物。IC50&TargetParasiteHSV-1BoHV-1SARS-CoV-2體外研究Inthesubmicromolarrange(EC50=250nM)theactionofIvermectin(MK-933)israpidandreversible,resultinginincreasedamplitudeandsloweddeactivationofP2X4channelcurrentsevokedbyATP[1].Ivermectin(MK-933)markedlyincreasesthepotencyofATPandthatofthenormallylow-potencyagonista,b-methylene-ATPinause-andvoltage-independentmannerwithoutchangingtheionselectivityofP2X4channels[1].Ivermectin(MK-933)activatesglutamate-gatedchloridechannelsinthenervesandmusclesoftheparasite,leadingtomembranehyperpolarizationandmuscleparalysis[2].Ivermectin(MK-933)stronglyinhibitsthebindingofImpα/β1toNS5(IC50=17μM),butnotofImpβ1alonetoNS5[3].Ivermectin(MK-933)haspotentantiviralactivitytowardsbothHIV-1anddenguevirus,bothofwhicharestronglyreliantonimportinα/βnuclearimport,withrespecttotheHIV-1integraseandNS5(non-structuralprotein5)polymeraseproteinsrespectively[3].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NucleicAcidsRes.2021Jan8;49(D1):D1113-D1121.?PLoSNeglTropDis.2019Aug20;13(8):e0007681.?NeurosciLett.2021Feb24;135773.?JAnimPhysiolAnimNutr(Berl).2020Jul;104(4):1024-1033.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KhakhBS,etal.AllostericcontrolofgatingandkineticsatP2X(4)receptorchannels.JNeurosci.1999Sep1;19(17):7289-99.[2].PrielA,etal.MechanismofivermectinfacilitationofhumanP2X4receptorchannels.JGenPhysiol.2004Mar;123(3):281-93.[3].WagstaffKM,etal.Ivermectinisaspecificinhibitorofimportinα/β-mediatednuclearimportabletoinhibitreplicationofHIV-1and2/3www.MedChemEwww.MedChemEdenguevirus.BiochemJ.2012May1;443(3):851-6.[4].RazaS,etal.IvermectinInhibitsBovineHerpesvirus1DNAPolymeraseNuclearImportandInterfereswithViralReplication.Microorganisms.2020Mar13;8(3).pii:E409.[5].KhanSharun,etal.Ivermectin,aNewCandidateTherapeuticAgainstSARS-CoV-2/COVID-19.AnnClinMicrobiolAntimicrob.2020May30;19(1):23.McePdfHeight關(guān)注MCE中國(guó)公眾號(hào)，

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