ProductDescription
LY-2484595(Evacetrapib)isabenzazepine-based,selectiveinhibitorofcholesterylestertransferprotein(CETP)atanIC50valueof5.5nMforhumanrecombinantCETP.Inhibitioninhumanplasmawas3.6nMIC50.[1]InH295Rcellsatconcentrationsupto10uM,LY-2484595hasbeenshowntoelevateHDLcholesterolwithoutinducingaldosterone,cortisolsynthesis,orincreasingbloodpressure.
Inarandomizedcontrolledtrialof398patientswithelevatedLDLandlowHDL,LY-2484595wasshowntobeeffectiveinloweringLDLandraisingHDL.Incombinationwithstatins,LY-2484595showedgreaterefficacyinloweringLDLwithnoadverseeffects.[2]
Technicalinformation:
| ChemicalFormula: | C31H36F6N6O2 | |
| CAS#: | 1186486-62-3 | |
| MolecularWeight: | 638.65 | |
| Purity: | >98% | |
| Appearance: | WhiteCrystalline | |
| ChemicalName: | Trans-4-({(5S)-5-[{[3,5-bis(trifluoromethyl)phenyl]methyl}(2-methyl-2H-tetrazol-5-yl)amino]-7,9-dimethyl-2,3,4,5-tetrahydro-1H-benzazepin-1-yl}methyl)cyclohexanecarboxylicacid | |
| Solubility: | Upto22mMinDMSO | |
| Synonyms: | LY-2484595,LY2484595,LY2484595,Evacetrapib |
ShippingCondition:Theproductisshippedinaglassvialatambienttemperature.
Storagecondition:Forlongershelflife,storesolidpowderat4oCdesiccated,orstoreDMSOsolutionat-20oC.
Reference:
| 1. | Caoetal.,Evacetrapibisanovel,potent,andselectiveinhibitorofcholesterylestertransferproteinthatelevatesHDLcholesterolwithoutinducingaldosteroneorincreasingbloodpressure.J.LipidRes.2011,52,2169-2176.PubmedID:21957197 |
| 2. | Nichollsetal.,EffectsoftheCETPinhibitorevacetrapibadmiNISTeredasmonotherapyorincombinationwithstatinsonHDLandLDLcholesterol:arandomizedcontrolledtrial.JAMA2011,306(19),2099-2109.PubmedID:22089718 |
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