WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H584375
CAS#: 141799-76-0
Description: E 5324, an acyl-CoA cholesterol acyltransferase inhibitor, has been found to inhibit cholesterol esterification and CE mass in atherosclerotic foam cells, derived from either macrophages or arterial smooth muscle cells.
Hodoodo Cat#: H584375
Name: E 5324
CAS#: 141799-76-0
Chemical Formula: C26H34N4O2
Exact Mass: 434.27
Molecular Weight: 434.584
Elemental Analysis: C, 71.86; H, 7.89; N, 12.89; O, 7.36
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Synonym: E-5324; E5324; E 5324
IUPAC/Chemical Name: Urea, N-butyl-N'-(2-(3-(5-ethyl-4-phenyl-1H-imidazol-1-yl)propoxy)-6-methylphenyl)-
InChi Key: NQZTZGNLFLQHKG-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H34N4O2/c1-4-6-16-27-26(31)29-24-20(3)12-10-15-23(24)32-18-11-17-30-19-28-25(22(30)5-2)21-13-8-7-9-14-21/h7-10,12-15,19H,4-6,11,16-18H2,1-3H3,(H2,27,29,31)
SMILES Code: O=C(NC1=C(C)C=CC=C1OCCCN2C(CC)=C(C3=CC=CC=C3)N=C2)NCCCC
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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 434.58 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.
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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Azuma Y, Kawasaki T, Ohno K, Seto J, Yamada T, Yamasaki M, Nobuhara Y. Effects of NTE-122, a novel acyl-CoA:cholesterol acyltransferase inhibitor, on cholesterol esterification and secretions of apolipoprotein B-containing lipoprotein and bile acids in HepG2. Jpn J Pharmacol. 1999 Feb;79(2):151-8. PubMed PMID: 10202850.
2: Kawasaki T, Miyazaki A, Hakamata H, Matsuda H, Horiuchi S. Biochemical evidence for oligomerization of rat adrenal acyl-coenzyme A:cholesterol acyltransferase. Biochem Biophys Res Commun. 1998 Mar 17;244(2):347-52. PubMed PMID: 9514926.
3: Kogushi M, Tanaka H, Ohtsuka I, Yamada T, Kobayashi H, Saeki T, Takada M, Hiyoshi H, Yanagimachi M, Kimura T, Yoshitake S, Saito I. Anti-atherosclerotic effect of E5324, an inhibitor of acyl-CoA:cholesterol acyltransferase, in Watanabe heritable hyperlipidemic rabbits. Atherosclerosis. 1996 Aug 2;124(2):203-10. PubMed PMID: 8830933.
4: Nicholson AC, Pomerantz KB, Fujimori T, Hajjar DP. Inhibition of cholesterol esterification in macrophages and vascular smooth muscle foam cells: evaluation of E5324, an acyl-CoA cholesterol acyltransferase inhibitor. Lipids. 1995 Aug;30(8):771-4. PubMed PMID: 7475994.
5: Kogushi M, Tanaka H, Kobayashi H, Yamada T, Ohtsuka I, Kimura T, Saito I. Effect of E5324, a novel inhibitor of acyl-CoA:cholesterol acyltransferase, on cholesteryl ester synthesis and accumulation in macrophages. Jpn J Pharmacol. 1995 Jun;68(2):191-9. PubMed PMID: 7563976.
6: Nagata Y, Yonemoto M, Iwasawa Y, Shimizu-Nagumo A, Hattori H, Sawazaki Y, Kamei T. N-[2-[N'-pentyl-(6,6-dimethyl-2,4-heptadiynyl)amino]ethyl]- (2-methyl-1-naphthylthio)acetamide (FY-087). A new acyl coenzyme a:cholesterol acyltransferase (ACAT) inhibitor of diet-induced atherosclerosis formation in mice. Biochem Pharmacol. 1995 Mar 1;49(5):643-51. PubMed PMID: 7887979.
7: Tanaka H, Ohtsuka I, Kogushi M, Kimura T, Fujimori T, Saeki T, Hayashi K, Kobayashi H, Yamada T, Hiyoshi H, et al. Effect of the acyl-CoA:cholesterol acyltransferase inhibitor, E5324, on experimental atherosclerosis in rabbits. Atherosclerosis. 1994 Jun;107(2):187-201. PubMed PMID: 7980693.