VU0650786-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEVU0650786Cat.No.:HY-108710CASNo.:1809085-30-0分?式:C??H??ClFN?O?分?量:387.8作?靶點(diǎn):mGluR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:250mg/mL(644.66mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.5786mL12.8932mL25.7865mL5mM0.5157mL2.5786mL5.1573mL10mM0.2579mL1.2893mL2.5786mL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%salineSolubility:≥2.08mg/mL(5.36mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.36mM);ClearsolutionBIOLOGICALACTIVITY?物活性VU0650786?種有效的，能透過中樞神經(jīng)系統(tǒng)的，選擇性?氨酸受體亞型3的負(fù)變構(gòu)調(diào)節(jié)劑(mGlu3NAM)，IC50值為392nM。VU0650786在嚙齒動(dòng)物中具有抗抑郁和抗焦慮活性[1]。IC50&TargetmGluR3392nM(IC50)體內(nèi)研究VU0650786(VU786)(i.p.,30mg/kg)increasestheproportionofc-Fos-positivecellsbyapproximately4-fold,enhancessynapticstrengthinconecellsubpopulations,weakensthalamocorticallong-termdepression(LTD),andreducespassivecopinginacutemodelsofantidepressant-likeactivityininduciblecFos-EGFPmice[2].ThepharmacokineticparametersofVU0650786(compound106)inrats[1].ParametersIV(0.2mg/kg)t1/2(min)42CLplasma(mL/min/kg)37VSS(L/kg)1.6REFERENCES[1].MaxEJoffe,etal.mGlu2andmGlu3NegativeAllostericModulatorsDivergentlyEnhanceThalamocorticalTransmissionandExertRapidAntidepressant-likeEffects.Neuron.2020Jan8;105(1):46-59.e3.[2].EngersJL,etal.DiscoveryofaSelectiveandCNSPenetrantNegativeAllostericModulatorofMetabotropicGlutamateReceptorSubtype3withAntidepressantandAnxiolyticActivityinRodents.JMedChem.2015Sep24;58(18):7485-500.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonl