Carbetocin-acetate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemECarbetocinacetateCat.No.:HY-17573ACASNo.:1631754-28-3分?式:C??H??N??O??S分?量:1048.21作?靶點(diǎn):OxytocinReceptor作?通路:GPCR/GProtein儲存?式:Sealedstorage,awayfrommoisturePowder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(119.25mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM0.9540mL4.7700mL9.5401mL5mM0.1908mL0.9540mL1.9080mL10mM0.0954mL0.4770mL0.9540mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，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:≥2.08mg/mL(1.98mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(1.98mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(1.98mM);ClearsolutionBIOLOGICALACTIVITY?物活性Carbetocinacetate?種催產(chǎn)素(OT)類似物，催產(chǎn)素受體(oxytocinreceptor)激動劑，Ki7.1nM。Carbetocinacetate對催產(chǎn)素受體的嵌合N末端(E1)具有?親和?(Ki=1.17μM)。Carbetocinacetate具有?于產(chǎn)后出?研究的潛?。Carbetocinacetate能透過?腦屏障，可以通過激活CNS中的催產(chǎn)素受體?具有類抗抑郁活性。體外研究Carbetocinacetateisanagonistwithabout10-foldloweraffinityfortheoxytocinreceptorbutwithsignificantlyhigherstabilityandalongerdurationofaction.CarbetocinacetatehashigheraffinitytothechimericE1receptorandespeciallytoeachofthecombinationsofE1withtheotherextracellulardomains,i.e.chimericreceptorsE13(Ki=13nM),E123(Ki=56nM),andE1234(Ki=37nM)[2].體內(nèi)研究Carbetocin(2-20mg/kg;i.p.)acetatehasasignificanteffectoftreatmentonthepercenttimespentclimbing,swimmingandimmobile[1].Carbetocin(1,10,100μg/rat,i.c.v.)acetaterevealsadose-dependentincreaseinthepercenttimespentswimmingandacorrespondingreductioninimmobilityfollowingacuteadministrationof100μg/rat[1].AnimalModel:MaleSprague-Dawleyratsweighingbetween300and500g[1]Dosage:2,6.4,20mg/kgAdministration:IP;singledoseResult:Increasedclimbingwith6.4mg/kgandresultedinasignificantlygreaterproportionoftimespentswimmingwith20mg/kg.REFERENCES[1].StellaChaviaras,etal.Assessingtheantidepressant-likeeffectsofcarbetocin,anoxytocinagonist,usingamodificationoftheforcedswimmingtest.Psychopharmacology(Berl).2010May;210(1):35-43.[2].GeraldGimpl,etal.Bindingdomainsoftheoxytocinreceptorfortheselectiveoxytocinreceptorantagonistbarusibanincomparisontotheagonistsoxytocinandcarbetocin.EurJPharmacol.2005Mar7;510(1-2):9-16.[3].DavidFeifel,etal.Theeffectsofoxytocinanditsanalog,carbetocin,ongeneticdeficitsinsensorimotorgating.EurNeuropsychopharmacol.2012May;22(5):374-8.McePdfHeightCaution:Producthasnotbeenfullyvalida