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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
SMILES O=C(NC1=CC(C)=C(O)C(C)=C1C)[C@@H](SCCCCCCCCCCCC)C2=CC=CC=C2
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
闪点 FP
熔点 Melting point
沸点 Boiling point
Polarizability极化度
密度 Density
蒸汽压 Vapor Pressure
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).
Application1
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危险性警示
安全声明
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备注
[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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