TMPyP4-tosylate-TMP-1363-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETMPyP4tosylateCat.No.:HY-108477CASNo.:36951-72-1Synonyms:TMP1363分?式:C??H??N?O??S?分?量:1363.6作?靶點(diǎn):G-quadruplex;Telomerase;Cholinesterase(ChE);SARS-CoV作?通路:CellCycle/DNADamage;NeuronalSignaling;Anti-infection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)H2O:25mg/mL(18.33mM;Needultrasonic)DMSO:10mg/mL(7.33mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM0.7334mL3.6668mL7.3335mL5mM0.1467mL0.7334mL1.4667mL10mM0.0733mL0.3667mL0.7334mL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%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥1mg/mL(0.73mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1mg/mL(0.73mM);Clearsolution3.請(qǐng)依序添加每種溶劑：PBSSolubility:7.14mg/mL(5.24mM);Clearsolution;Needultrasonicandwarmingandheatto60°CBIOLOGICALACTIVITY?物活性TMPyP4tosylate(TMP1363)?種四鏈體(G-quadruplex)特異性配體，可抑制G-四鏈體和IGF-1之間的相互作?。TMPyP4tosylate?種端粒酶(telomerase)抑制劑，且抑制腫瘤細(xì)胞增殖。TMPyP4tosylate也是核酸?級(jí)結(jié)構(gòu)的穩(wěn)定劑和?酰膽堿酯酶抑制劑。除此之外，TMPyP4tosylate對(duì)SARS-CoV-2有抗病毒活性。IC50&TargetAChEG-quadruplexTelomeraseSARS-CoV-2體外研究TMPyP4tosylate(50?μM,96h)inhibitstelomeraseactivityintelomerasepositiveHOScells[2].TMPyP4tosylate(50?μM,48or96h)inhibitsthegrowthofHOScells[2].TMPyP4tosylate(50?μM,96h)inducescellapoptosisinHOS,Saos-2,MG-63,andU2OScelllines[2].TMPyP4tosylate(100?μM,24or48h)increasescellcycleregulatoryproteinsandMAPKsinK562cells[4].CellViabilityAssay[2]CellLine:HOScellsConcentration:50?μMIncubationTime:48or96hResult:Time-dependentlyinhibitedcellviability.WesternBlotAnalysis[4]CellLine:K562cellsConcentration:100?μMIncubationTime:24or48hResult:Increasedtheexpressionofp21CIP1proteinandp57KIP2protein.體內(nèi)研究TMPyP4tosylate(10and20mg/kg,i.p.,twotimesweekly)inhibitstumorgrowthinMX-1tumormodel[5].TMPyP4tosylate(15?mg/kgor30?mg/kg,i.n.)decreasesthemeanviralloadsinSARS-CoV-2-infectedhamster[6].TMPyP4tosylate(30?mg/kg,i.n.,hamsters)showsaCmaxof17.88?μg/mLat1h,andahalf-life(T1/2)of6.36?h[6].2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEAnimalModel:MX-1mammarychemoadjuvantmodel[5]Dosage:10and20mg/kgAdministration:Intraperitonealinjection(i.p.),twiceweekly.Result:Inhibitedtumorgrowthandprolongedmicesurvival.AnimalModel:SARS-CoV-2-infectedhamster[6]Dosage:15?mg/kgor30?mg/kgAdministration:i.n.,startingat1?hpriortovirusinoculationandcontinuinguntil3dayspostinfectionResult:Decreasedthemeanviralloadsinthenasalwash,nasalturbinateandlungtissues.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?MicrobiolSpectr.2022Apr21;e0046022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].FujiwaraN,etal.aStabilizerofNucleicAcidSecondaryStructure,IsaNovelAcetylcholinesteraseInhibitor.PLoSOne.2015Sep24;10(9):e0139167.[2].Mikami-TeraoY,etal.AntitumoractivityofG-quadruplex-interactiveagentTMPyP4inK562leukemiccells.CancerLett.2008Mar18;261(2):226-34.[3].GrandCL,etal.ThecationicporphyrinTMPyP4down-regulatesc-MYCandhumantelomerasereversetranscriptaseexpressionandinhibitstumorgrowthinvivo.MolCancerTher.2002Jun;1(8):565-73.Erratumin:MolCancerTher.2003Feb;2(2):208.[4].QinG,etal.RNAG-quadruplexformedinSARS-CoV-2usedforCOVID-19treatmentinanimalmodels.CellDiscov.2022Sep6;8(1):86.[5].ChenH,etal.Insuline-likegrowthfactortypeIselectivelybindstoG-quadruplexstructures.BiochimBiophysActaGenSubj.2019Jan;1863(1):31-38.[6].FujimoriJ,etal.AntitumoreffectsoftelomeraseinhibitorTMPyP4inosteosarcomacelllines.JOrthopRes.2011Nov;29(11):1