Heptamidine-dimethanesulfonate-SBi4211-dimethanesulfonate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEHeptamidinedimethanesulfonateCat.No.:HY-16918ACASNo.:161374-55-6Synonyms:SBi4211dimethanesulfonate分?式:C??H??N?O?S?分?量:560.68作?靶點(diǎn):Others作?通路:Others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:62.5mg/mL(111.47mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7835mL8.9177mL17.8355mL5mM0.3567mL1.7835mL3.5671mL10mM0.1784mL0.8918mL1.7835mL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(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%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(3.71mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(3.71mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(3.71mM);ClearsolutionBIOLOGICALACTIVITY?物活性Heptamidinedimethanesulfonate(SBi4211dimethanesulfonate)?種強(qiáng)效的，與噴他脒(HY-B0537)有關(guān)的鈣結(jié)合蛋?S100B的抑制劑(Kd=6.9μM)，選擇性地殺死表達(dá)S100B的?素瘤細(xì)胞。Heptamidinedimethanesulfonate研究強(qiáng)直性肌營(yíng)養(yǎng)不良(DM)的有效?具。IC50&TargetKd:6.9μM(calcium-bindingproteinS100B)[1]體外研究HeptamidineisaPentamidine-S100Bcomplex,twomoleculesofpentamidinebindpermonomerofS100B,whichperformstobeaninhibitorforS100B[1].Heptamidine(20μM)doesnotdecreaseCUGlevelssignificantlywhencomparestoPropamidineandPentamidine,andexhibitscytotoxicatconcentrationsabove17.5μMinHeLacellsexpressing960CUGrepeats[2].Heptamidinerescuesmis-splicingofminigenereportersinaHeLacellDM1modelwithanEC50valueof15μM[2].體內(nèi)研究Heptamidine(intraperitonealinjection;20or30mg/kg;7days)causesadose-dependentreductionofexon7ainclusioninHSALRmice,returningtowildtypelevels(6±1%)whenat20mg/kgdose,themyotoniaisreducedfromgrade3tograde1(occasionalmyotonicdischarge)orgrade0atboth20or30mg/kg[2].AnimalModel:HomozygousHSALRtransgenicmiceinline20b(FVBinbredbackground)withaMyotonicdystrophy(DM)mousemodel[2]Dosage:20or30mg/kgAdministration:Intraperitonealinjection;7days;oncedailyResult:ReversedsplicingdefectsandrescuesmyotoniainaDMmousemodel.REFERENCES[1].McKnightLE,etal.Structure-BasedDiscoveryofaNovelPentamidine-RelatedInhibitoroftheCalcium-BindingProteinS100B.ACSMedChemLett.2012Dec13;3(12):975-979.Epub2012Sep25.[2].CoonrodLA,etal.ReducinglevelsoftoxicRNAwithsmallmolecules.ACSChemBiol.2013Nov15;8(11):2528-37.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform