Rilmenidine-phosphate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrarieswww.MedChemERilmenidinephosphateCat.No.:HY-100490BCASNo.:85409-38-7分⼦式:C₁₀H₁₉N₂O₅P分⼦量:278.24作⽤靶点:ImidazolineReceptor;AdrenergicReceptor;Apoptosis;Autophagy作⽤通路:GPCR/GProtein;NeuronalSignaling;Apoptosis;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:62.5mg/mL(224.63mM;Needultrasonic)DMSO:5mg/mL(17.97mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.5940mL17.9701mL35.9402mL5mM0.7188mL3.5940mL7.1880mL10mM0.3594mL1.7970mL3.5940mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存⽅式和期限。BIOLOGICALACTIVITY⽣物活性Rilmenidinephosphate⼀种新型的抗⾼⾎压药物和⼝服活性选择性I1咪唑啉受体(I1imidazolinereceptor)激动剂。Rilmenidinephosphate也⼀种α2肾上腺素受体激动剂。Rilmenidinephosphate诱导⾃噬(autophagy)。Rilmenidinephosphate可通过减少交感神经过度活跃⽽发挥中枢作⽤，并通过抑制Na+/H+反向转运⽽在肾脏中发挥作⽤。Rilmenidinephosphate可调节⽩⾎病细胞增殖，刺激促凋亡蛋⽩Bax，从⽽诱导⼈⽩⾎病K562细胞线粒体通路的紊乱和凋亡。1/2MasterofSmallMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究Rilmenidinephosphate(25-100μM;24hours)inhibitsK562cellproliferation[2].Rilmenidineprovidesantihypertensiveefficacycomparablewiththatofdiuretics,beta-blockers,calciumchannelblockers,andangiotensin-convertingenzyme(ACE)inhibitors[3].CellProliferationAssay[2]CellLine:K562cellsConcentration:25,50,100μMIncubationTime:24hoursResult:Dose-dependentlyinhibitedK562colonyformation.体内研究Rilmenidinephosphate-treatedN171-82Qmice(i.p.;4-timesaweek)displayssignificantimprovedforelimbgripstrengthandalllimbsgripstrengthfrom12to22weeksofage[4].Rilmenidinephosphatedecreaseslevelsofmutanthuntingtin[4].REFERENCES[1].ReidJL.Rilmenidine:aclinicaloverview.AmJHypertens.2000;13(6Pt2):106S-111S.[2].Srdic-RajicT,etal.RilmenidinesuppressesproliferationandpromotesapoptosisviathemitochondrialpathwayinhumanleukemicK562cells.EurJPharmSci.2016;81:172-180.[3].RoseC,etal.RilmenidineattenuatestoxicityofpolyglutamineexpansionsinamousemodelofHuntington'sdisease.HumMolGenet.2010;19(11):2144-2153.[4].ReidJL.Rilmenidine:aclinicaloverview.AmJHypertens.2000;13(6Pt2):106S-111S.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearc