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Eflucimibe_202340-45-2_产品详情
202340-45-2
  • names:

    (S)-2-(dodecylthio)-N-(4-hydroxy-2,3,5-trimethylphenyl)-2-phenylacetamide

  • CAS号:

    202340-45-2

    MDL Number:
  • MF(分子式): C29H43NO2S MW(分子量): 469.728
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
Eflucimibe
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中文别名 Eflucimibe
英文别名 Eflucimibe; F-12511; L-0081; F12511; L0081.
CAS号 202340-45-2
Inchi InChI=1S/C29H43NO2S/c1-5-6-7-8-9-10-11-12-13-17-20-33-28(25-18-15-14-16-19-25)29(32)30-26-21-22(2)27(31)24(4)23(26)3/h14-16,18-19,21,28,31H,5-13,17,20H2,1-4H3,(H,30,32)/t28-/m0/s1
InchiKey ZXEIEKDGPVTZLD-NDEPHWFRSA-N
分子式 Formula C29H43NO2S
分子量 Molecular Weight 469.728
溶解度Solubility
性状 Solid powder
储藏条件 Storage conditions Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).
产品说明 Eflucimibe(CAS:202340-45-2):仅限应用于工业或者科学研究过程中非医疗目的,不应用于人类或动物的临床诊断以及治过程疗,该产品非药用,非食用。
IntroductionEflucimibe, also known as F-12511; L-0081, is an ACAT inhibitor potentially for the treatment of atherosclerosis and hyperlipidemia. F 12511 regulates endogenous hypercholesterolemia in a synergistic manner in New Zealand rabbits fed a casein-enriched diet. F 12511 inhibited ACAT activity with IC(50) values of 3, 7, and 71 nM, respectively. In vivo, orally administered F 12511 displayed high potency and efficacy as an antihypercholesterolemic compound in different cholesterol-fed animals (rat, guinea-pig, rabbit).
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[1]Zhang XF, O'Shea H, Kehoe S, Boyd D. Time-dependent evaluation of mechanical properties and in vitro cytocompatibility of experimental composite-based nerve guidance conduits. J Mech Behav Biomed Mater. 2011 Oct;4(7):1266-74. doi: 10.1016/j.jmbbm.2011.04.013. PubMed PMID: 21783135.
[2]López-Farré AJ, Sacristán D, Zamorano-León JJ, San-Martín N, Macaya C. Inhibition of acyl-CoA cholesterol acyltransferase by F12511 (Eflucimibe): could it be a new antiatherosclerotic therapeutic? Cardiovasc Ther. 2008 Spring;26(1):65-74. doi: 10.1111/j.1527-3466.2007.00030.x. Review. PubMed PMID: 18466422.
[3] Zamorano-León JJ, Fernández-Sánchez R, López Farré AJ, Lapuente-Tiana L, Alonso-Orgaz S, Sacristán D, Junquera D, Delhon A, Conesa A, Mateos-Cáceres PJ, Macaya C. Direct effect of F12511, a systemic inhibitor of Acyl-CoA cholesterol acyltransferase on bovine aortic endothelial cells. J Cardiovasc Pharmacol. 2006 Sep;48(3):128-34. PubMed PMID: 17031267.
[4] Teychene S, Autret JM, Biscans B. Determination of solubility profiles of eflucimibe polymorphs: experimental and modeling. J Pharm Sci. 2006 Apr;95(4):871-82. PubMed PMID: 16489606.
[5] Rodier E, Lochard H, Sauceau M, Letourneau JJ, Freiss B, Fages J. A three step supercritical process to improve the dissolution rate of eflucimibe. Eur J Pharm Sci. 2005 Oct;26(2):184-93. PubMed PMID: 16081259.
6: Mesplet N, Morin P, Ribet JP. Spectrofluorimetric study of eflucimibe-gamma-cyclodextrin inclusion complex. Eur J Pharm Biopharm. 2005 Apr;59(3):523-6. PubMed PMID: 15760733.7: Mesplet N, Morin P, Ribet JP. Development of a method for simultaneous determination of eflucimibe and its three major metabolites in rat plasma by liquid chromatography/electrospray tandem mass spectrometry: a preliminary study. Rapid Commun Mass Spectrom. 2005;19(3):297-302. PubMed PMID: 15645487.8: Gil A, Chamayou A, Leverd E, Bougaret J, Baron M, Couarraze G. Evolution of the interaction of a new chemical entity, eflucimibe, with gamma-cyclodextrin during kneading process. Eur J Pharm Sci. 2004 Oct;23(2):123-9. PubMed PMID: 15451000.9: Burnett JR. Eflucimibe. Pierre Fabre/Eli Lilly. Curr Opin Investig Drugs. 2003 Mar;4(3):347-51. Review. PubMed PMID: 12735237.10: Ribet JP, Pena R, Chauvet A, Patoiseau JF, Autin JM, Segonds R, Basquin M, Autret JM. [Crystalline polymorphism of eflucimibe]. Ann Pharm Fr. 2002 May;60(3):177-86. French. PubMed PMID: 12050596.1
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