Alniditan-dihydrochloride-Alnitidan-dihydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAlniditandihydrochlorideCat.No.:HY-101698BCASNo.:155428-00-5Synonyms:Alnitidandihydrochloride分?式:C??H??Cl?N?O分?量:375.34作?靶點(diǎn):5-HTReceptor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:62.5mg/mL(166.52mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.6643mL13.3213mL26.6425mL5mM0.5329mL2.6643mL5.3285mL10mM0.2664mL1.3321mL2.6643mL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%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(5.54mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(5.54mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.54mM);ClearsolutionBIOLOGICALACTIVITY?物活性Alniditan(Alnitidan)dihydrochloride?種有效的5-HT1B和5-HT1D受體激動(dòng)劑，在HEK293細(xì)胞中，對(duì)?5-HT1B和?5-HT1D受體的IC50分別為1.7nM和1.3nM。Alniditandihydrochloride具有預(yù)防偏頭痛的作?。IC50&Targethuman5-HT1Bhuman5-HT1D5-HT1BReceptor5-HT1DReceptorReceptorReceptor0.9nM(Kd)1.2nM(Kd)1.7nM(IC50)1.3nM(IC50)體外研究Invitro,Alniditanexhibitslittlevasoconstrictiveeffectsontheratbasilarartery,althoughataveryhighconcentration1mM,Alniditancausesintensiveconstriction,mostlikelythroughamechanismindependentfrom5-HTreceptoractivation[1].體內(nèi)研究TheintraperitonealadministrationofAlniditanED50=9μg/kgdosedependlyreduces[125I]-BSAextravasationintheratmeningeswhendone30minbeforestimulation.Alniditandosedependentlyattenuatedstheneurogenicinflammationinvivomodelofneurogenicinflammation[1].REFERENCES[1].LimmrothV,etal.Effectsofalniditanonneurogenicoedemaintheratduramaterandoncontractionofratbasilarartery.EurJPharmacol.1999Oct8;382(2):103-9.[2].LesageAS,etal.Agonisticpropertiesofalniditan,sumatriptananddihydroergotamineonhuman5-HT1Band5-HT1Dreceptorsexpressedinvariousmammaliancelllines.BrJPharmacol.1998Apr;123(8):1655-65.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For