Rilmenidine-phosphate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemERilmenidinephosphateCat.No.:HY-100490BCASNo.:85409-38-7分?式:C??H??N?O?P分?量:278.24作?靶點(diǎn):ImidazolineReceptor;AdrenergicReceptor;Apoptosis;Autophagy作?通路:GPCR/GProtein;NeuronalSignaling;Apoptosis;Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:62.5mg/mL(224.63mM;Needultrasonic)DMSO:5mg/mL(17.97mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.5940mL17.9701mL35.9402mL5mM0.7188mL3.5940mL7.1880mL10mM0.3594mL1.7970mL3.5940mL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，并請注意儲備液的保存?式和期限。BIOLOGICALACTIVITY?物活性Rilmenidinephosphate?種新型的抗??壓藥物和?服活性選擇性I1咪唑啉受體(I1imidazolinereceptor)激動劑。Rilmenidinephosphate也?種α2腎上腺素受體激動劑。Rilmenidinephosphate誘導(dǎo)?噬(autophagy)。Rilmenidinephosphate可通過減少交感神經(jīng)過度活躍?發(fā)揮中樞作?，并通過抑制Na+/H+反向轉(zhuǎn)運(yùn)?在腎臟中發(fā)揮作?。Rilmenidinephosphate可調(diào)節(jié)??病細(xì)胞增殖，刺激促凋亡蛋?Bax，從?誘導(dǎo)???病K562細(xì)胞線粒體通路的紊亂和凋亡。1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE體外研究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.體內(nèi)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