Valiglurax-VU0652957-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEValigluraxCat.No.:HY-122647CASNo.:1976050-09-5Synonyms:VU0652957;VU2957分?式:C??H??F?N?分?量:329.28作?靶點(diǎn):mGluR作?通路:GPCR/GProtein;NeuronalSignaling儲(chǔ)存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:125mg/mL(379.62mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.0369mL15.1846mL30.3693mL5mM0.6074mL3.0369mL6.0739mL10mM0.3037mL1.5185mL3.0369mL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(protectfromlight)。-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(7.59mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性Valiglurax(VU0652957)?種?服有效的選擇性mGlu4正變構(gòu)調(diào)節(jié)劑，對(duì)hmGlu4和rmGlu4GIRK的EC50值分別為64.6nM和197nM。Valiglurax?種中樞神經(jīng)系統(tǒng)(CNS)滲透劑。Valiglurax可?于帕?森病的研究。體內(nèi)研究Valiglurax(VU0652957;0.3-30mg/kg;po)reverseshaloperidol(HY-14538)-inducedcatalepsy(HIC)inratsinadose-dependentmanner[1].AnimalModel:haloperidol-inducedcatalepsy(HIC)inrats[1]Dosage:0.3-30mg/kgAdministration:OraladministrationResult:Reversedhaloperidol(HY-14538)-inducedcatalepsy(HIC)inratsinadose-dependentmanner.REFERENCES[1].PanareseJD,et,al.DiscoveryofVU2957(Valiglurax):AnmGlu4PositiveAllostericModulatorEvaluatedasaPreclinicalCandidatefortheTreatmentofParkinson'sDisease.ACSMedChemLett.2018Oct16;10(3):255-260.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-37