VU-6008667-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVU6008667Cat.No.:HY-101281CASNo.:2092923-21-0分?式:C??H??ClF?N?O?分?量:438.85作?靶點(diǎn):mAChR作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:4°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(227.87mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.2787mL11.3934mL22.7868mL5mM0.4557mL2.2787mL4.5574mL10mM0.2279mL1.1393mL2.2787mL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(storedundernitrogen)。-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%salineSolubility:≥2.5mg/mL(5.70mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.70mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性VU6008667M5NAM毒蕈堿型?酰膽堿受體亞型5的選擇性負(fù)變構(gòu)調(diào)節(jié)劑，對(duì)?M5和??M5的IC50值分別為1.2μM和1.6μM。VU6008667具有?CNS滲透性。IC50&TargetIC50:1.2μM(HumanM5);1.6μM(RatM5)[1]體內(nèi)研究VU6008667(1mg/kg)/PO(3mg/kg,solutiondose)displaysadiminishedeliminationhalf-life(t1/2=2.3hr)drivenbyasmallervolume(Vss=7.4L/kg)andhigherclearance(CLp=82mL/min/kg),withmoderateoralbioavailability(17%F)[1].AnimalModel:RAT(PKstudy)[1]Dosage:1mg/kg;3mg/kgAdministration:oraladminstrationResult:Hadadesiredshorthalf-lifeinrat(t1/2=2.3hr),withmoderateoralbioavailability(17%F).REFERENCES[1].McGowanKMetal,ContinuedoptimizationoftheM5NAMML375:DiscoveryofVU6008667,anM5NAMwithhighCNSpenetrationandadesiredshorthalf-lifeinratforaddictionstudies.BioorgMedChemLett.2017Mar15;27(6):1356-1359.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:4