A2793-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesA2793Cat.No.:HY-137563CASNo.:88349-90-0分?式:C??H??ClNO?分?量:265.69作?靶點(diǎn):PotassiumChannel作?通路:MembraneTransporter/IonChannel儲(chǔ)存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(376.38mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.7638mL18.8189mL37.6378mL5mM0.7528mL3.7638mL7.5276mL10mM0.3764mL1.8819mL3.7638mL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(9.41mM);Clearsolution此?案可獲得≥2.5mg/mL(9.41mM，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2.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:≥2.5mg/mL(9.41mM);Clearsolution此?案可獲得≥2.5mg/mL(9.41mM，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1/2實(shí)驗(yàn)。以1mL?作液為例，取100μL25.0mg/mL的澄DMSO儲(chǔ)備液加到900μL??油中，混合均勻。BIOLOGICALACTIVITY?物活性A2793有效的TWIK相關(guān)酸敏感K+通道1(TASK-1)/TRESK的抑制劑，其對(duì)mTRESK的IC50值為6.8μM。A2764對(duì)TRESK選擇性更好,對(duì)TREK-1和TALK-1相對(duì)弱?些。IC50&TargetIC50:6.8μM(mTRESK)[1].體外研究A2793(100μM)inhibitstheunstimulatedchannelby43.0±8.9%(n=5)whileafterionomycinactivationthereductionoftheTRESKcurrentis85.5±2.9%(n=5)[1].A2793inhibitsTASK-1(100μM,53.4±13,5%,n=5),whileA2764ismoreselectiveforTRESK,itonlymoderatelyinfluencesTREK-1andTALK-1[1].A2793maybeconsideredasatooltodiscriminatebetweentherestingandactivatedchannelsinheterologousexpressionsystems,andtoblockTRESKactivatedbycalcineurininthenativecellswhichdonotexpressTASK-1[1].REFERENCES[1].MiklósLengyel,etal.ChemicallyModifiedDerivativesoftheActivatorCompoundCloxyquinExertInhibitoryEffectonTRESK(K2P18.1)BackgroundPotassiumChannel.MolPharmacol.2019Jun;95(6):652-660.McePdfHeightMedChemExpress(MCE)只為有資質(zhì)的科研機(jī)構(gòu)、醫(yī)藥企業(yè)基于科學(xué)研究或