RO5166017-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERO5166017Cat.No.:HY-12699CASNo.:1048346-74-2分?式:C??H??N?O分?量:219.28作?靶點:Others作?通路:Others儲存?式:-20°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實驗DMSO:100mg/mL(456.04mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.5604mL22.8019mL45.6038mL5mM0.9121mL4.5604mL9.1208mL10mM0.4560mL2.2802mL4.5604mL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)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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%salineSolubility:≥2.5mg/mL(11.40mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(11.40mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(11.40mM);ClearsolutionBIOLOGICALACTIVITY?物活性RO5166017具有?服活性的、跨物種的TAAR1的激動劑，其對??、??、?和?蟹猴的Ki值分別為1.9nM、2.7nM、31nM和24nM。體外研究RO5166017showedhighaffinityandpotentfunctionalactivityatmouse,rat,cynomolgusmonkey,andhumanTAAR1stablyexpressedinHEK293cellsaswellashighselectivityvs.othertargets[1].體內(nèi)研究RO5166017preventsstress-inducedhyperthermiaandblockeddopamine-dependenthyperlocomotionincocaine-treatedanddopaminetransporterknockoutmiceaswellashyperactivityinducedbyanNMDAantagonist[1].RO5166017(0.01-1mg/kg,orally)dose-dependentlypreventstheSIHinNMRImice.RO5166017exhibitsTAAR1-mediatedanxiolytic-likepropertiesatdoses0.1-0.3mg/kg.[1].RO5166017preventsthecocaine-inducedhyperlocomotion.RO5166017alsoinhibitsstereotypiesinducedbycocaineinWTmicesimilartoolanzapine,andthiseffectislostinTaar1?/?mice[1].TAAR1activationbyRO5166017increasesglucose-dependentinsulinsecretioninINS1EcellsandhumanisletsandelevatedplasmaandpeptideYY(PYY)andglucagonlikepeptide1(GLP-1)levelsinmice[2].Subchronictreatmentofdiet-inducedobese(DIO)micewithRO5166017resultsinreducedfoodintakeandbodyweight[2].REFERENCES[1].FlorentGRevel,etal.TAAR1activationmodulatesmonoaminergicneurotransmission,preventinghyperdopaminergicandhypoglutamatergicactivity.ProcNatlAcadSciUSA[2].JustinNSiemian,etal.Traceamine-associatedreceptor1agonistsRO5263397andRO5166017attenuatequinpirole-inducedyawningbutnothypothermiainrats.BehavPharmacol.2017Oct;28(7):590-593.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedica