AM-6538-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAM-6538Cat.No.:HY-120423CASNo.:1245626-00-9分?式:C??H??Cl?N?O?分?量:542.41作?靶點(diǎn):CannabinoidReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(92.18mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.8436mL9.2181mL18.4362mL5mM0.3687mL1.8436mL3.6872mL10mM0.1844mL0.9218mL1.8436mL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(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:4.5mg/mL(8.30mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(4.61mM);ClearsolutionBIOLOGICALACTIVITY?物活性AM6538?種長(zhǎng)效、?親和?、偽不可逆的cannabinoid(CB)拮抗劑。AM6538利那班的結(jié)構(gòu)類似物。AM6538可有效評(píng)價(jià)??素完全和部分激動(dòng)劑的表觀療效。AM6538可能在未來(lái)需暫時(shí)減少??素受體可?性的研究中有?[1]。IC50&Targetcannabinoid[1]體外研究AM6538isacannabinoidantagonistthatbindsCB1receptorsexpressedinHEK-293cellsinawash-resistantmanner[1].體內(nèi)研究AM6538(1~10mg/kg)antagonizestheantinociceptiveeffectsofcannabinoidagonistsinmice[1].AM6538(10mg/kg)showsthattherearesomerecoveryintheeffectsofAM4054.AM6538dosedependentlydecreasesthetauvaluesforallcannabinoidagonists,reflectingreductionsintheavailablereceptors.AM6538producesenduringantagonism,withrobusteffectsonthetetrahydrocannabinoldose-effectfunctionevidentupto7daysaftertreatment[1].REFERENCES[1].ParonisCA,etal.Long-LastingInVivoEffectsoftheCannabinoidCB1AntagonistAM6538.JPharmacolExpTher.2018;364(3):485-493.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: