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MedKoo Cat#: 530202 | Name: Eflucimibe

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Eflucimibe, 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).

Chemical Structure

Eflucimibe
Eflucimibe
CAS#202340-45-2

Theoretical Analysis

MedKoo Cat#: 530202

Name: Eflucimibe

CAS#: 202340-45-2

Chemical Formula: C29H43NO2S

Exact Mass: 469.3015

Molecular Weight: 469.73

Elemental Analysis: C, 74.15; H, 9.23; N, 2.98; O, 6.81; S, 6.83

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
Eflucimibe; F-12511; L-0081; F12511; L0081.
IUPAC/Chemical Name
(S)-2-(dodecylthio)-N-(4-hydroxy-2,3,5-trimethylphenyl)-2-phenylacetamide
InChi Key
ZXEIEKDGPVTZLD-NDEPHWFRSA-N
InChi Code
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
SMILES Code
O=C(NC1=CC(C)=C(O)C(C)=C1C)[C@@H](SCCCCCCCCCCCC)C2=CC=CC=C2
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 469.73 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
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. 11: Rival Y, Junquéro D, Bruniquel F, N'Guyen X, Fauré P, Pomiès JP, Degryse AD, Delhon A. Anti-atherosclerotic properties of the acyl-coenzyme A:cholesterol acyltransferase inhibitor F 12511 in casein-fed New Zealand rabbits. J Cardiovasc Pharmacol. 2002 Feb;39(2):181-91. PubMed PMID: 11791003. 12: Milliat F, Férézou J, Delhon A, Lutton C. Overexpression of SR-BI in hamsters treated with a novel ACAT inhibitor (F12511). C R Acad Sci III. 2001 Mar;324(3):229-34. PubMed PMID: 11291309. 13: Junquero D, Pilon A, Carilla-Durand E, Patoiseau JF, Tarayre JP, Torpier G, Staels B, Fruchart JC, Colpaert FC, Clavey V, Delhon A. Lack of toxic effects of F 12511, a novel potent inhibitor of acyl-coenzyme A: cholesterol O-acyltransferase, on human adrenocortical cells in culture. Biochem Pharmacol. 2001 Feb 15;61(4):387-98. PubMed PMID: 11226372. 14: Junquero D, Bruniquel F, N'Guyen X, Autin JM, Patoiseau JF, Degryse AD, Colpaert FC, Delhon A. F 12511, a novel ACAT inhibitor, and atorvastatin regulate endogenous hypercholesterolemia in a synergistic manner in New Zealand rabbits fed a casein-enriched diet. Atherosclerosis. 2001 Mar;155(1):131-42. PubMed PMID: 11223434. 15: Junquero D, Oms P, Carilla-Durand E, Autin J, Tarayre J, Degryse A, Patoiseau J, Colpaert FC, Delhon A. Pharmacological profile of F 12511, (S)-2',3', 5'-trimethyl-4'-hydroxy-alpha-dodecylthioacetanilide a powerful and systemic acylcoenzyme A: cholesterol acyltransferase inhibitor. Biochem Pharmacol. 2001 Jan 1;61(1):97-108. PubMed PMID: 11137714.

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