CP-601932-1S-5R-CP-601927-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECP-601932Cat.No.:HY-138879BCASNo.:357425-68-4Synonyms:(1S,5R)-CP-601927分?式:C??H??F?N分?量:227.23作?靶點(diǎn):nAChR作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲(chǔ)存?式:Pureform-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:200mg/mL(880.17mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM4.4008mL22.0041mL44.0083mL5mM0.8802mL4.4008mL8.8017mL10mM0.4401mL2.2004mL4.4008mL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。-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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥5mg/mL(22.00mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(22.00mM);ClearsolutionBIOLOGICALACTIVITY?物活性CP-601932α3β4nAChR的?親和?部分激動(dòng)劑(Ki=21;EC50=~3μM)。CP-601932對(duì)α3β4和α4β2nAChR具有相同的?結(jié)合親和?，對(duì)α6和α7nAChR亞型親和?降低?個(gè)數(shù)量級(jí)。CP-601932在長(zhǎng)期露后選擇性地減少?醇消耗，但不減少蔗糖消耗和操作性?我給藥。CP-601932可透過?腦屏障。體內(nèi)研究CP-601932(10?mg/kg;s.c;adultmaleSprague-Dawleyrats)decreasesactiveleverpressesfor10%ethanol,butnot5%sucroseintheoperantself-administrationparadigm[1].CP-601932(adultmaleSprague-Dawleyrats)readilypenetratestheCNSandat30?minreachesmaximalCb,uvaluesof340?nMafter5?mg/kgand710?nMafter10?mg/kg.BrainconcentrationsofCP-601932declineveryslowlyandlevelsstayrelativelyhigh,eg,530?nMat5?hand85?nMat24?hafter10?mg/kg[1].REFERENCES[1].ChatterjeeS,etal.Partialagonistsoftheα3β4*neuronalnicotinicacetylcholinereceptorreduceethanolconsumptionandseekinginrats.Neuropsychopharmacology.2011;36(3):603-615.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: