Avasimibe


Catalog No. size PriceQuantity
M7116-2 2mg solid $126
M7116-10 10mg solid $535

Description

Cas:166518-60-1

Product Information

Avasimibe is an acyl coenzyme A: cholesterol acyltransferase (ACAT) inhibitor. Avasimibe can also reduce the synthesis and secretion of Apo B 100 in HepG2 cells. Avasimibe encapsulated in human serum albumin blocks cholesterol esterification for selective cancer treatment. Avasimibe could be an efficient therapy in the treatment of glioblastoma.

 

Chemical Formula: C29H43NO4S

 

Exact Mass: 501.29128

 

Molecular Weight: 501.72

 

Elemental Analysis: C, 69.42; H, 8.64; N, 2.79; O, 12.76; S, 6.39

 

Synonym: 

 

CI-1011

CI 1011

CI1011

Avasimibe sodium

 

Chemical Name: 

((2,4,6-Tris(1-methylethyl)phenyl)acetyl)sulfamic acid 2,6-bis(1-methylethyl)phenyl ester

 

InChi Key: 

PTQXTEKSNBVPQJ-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C29H43NO4S/c1-17(2)22-14-25(20(7)8)27(26(15-22)21(9)10)16-28(31)30-35(32,33)34-29-23(18(3)4)12-11-13-24(29)19(5)6/h11-15,17-21H,16H2,1-10H3,(H,30,31)

 

Smiles Code:

c1(C(C)C)cc(cc(c1CC(NS(Oc1c(cccc1C(C)C)C(C)C)(=O)=O)=O)C(C)C)C(C)C

 

 

Technical Data:

 

Appearance: White to off-white 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, not in water

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

 

 

References

 

  1. Tardif JC, Grégoire J, L'Allier PL, Anderson TJ, Bertrand O, Reeves F, Title LM, Alfonso F, Schampaert E, Hassan A, McLain R, Pressler ML, Ibrahim R, Lespérance J, Blue J, Heinonen T, Rodés-Cabau J; Avasimibe and Progression of Lesions on UltraSound (A-PLUS) Investigators. Effects of the acyl coenzyme A:cholesterol acyltransferase inhibitor avasimibe on human atherosclerotic lesions. Circulation. 2004 Nov 23;110(21):3372-7. Epub 2004 Nov 8. PubMed PMID: 15533865.

 

  1. Burnett JR, Telford DE, Barrett PH, Huff MW. The ACAT inhibitor avasimibe increases the fractional clearance rate of postprandial triglyceride-rich lipoproteins in miniature pigs. Biochim Biophys Acta. 2005 Dec 30;1738(1-3):10-8. Epub 2005 Dec 22. PubMed PMID: 16427354.

 

  1. Lee SS, Li J, Tai JN, Ratliff TL, Park K, Cheng JX. Avasimibe encapsulated in human serum albumin blocks cholesterol esterification for selective cancer treatment. ACS Nano. 2015 Mar 24;9(3):2420-32. doi: 10.1021/nn504025a. Epub 2015 Feb 16. PubMed PMID: 25662106.

 

  1. Bemlih S, Poirier MD, El Andaloussi A. Acyl-coenzyme A: cholesterol acyltransferase inhibitor Avasimibe affect survival and proliferation of glioma tumor cell lines. Cancer Biol Ther. 2010 Jun 15;9(12):1025-32. Epub 2010 Jun 24. PubMed PMID: 20404512.

 

  1. Raal FJ, Marais AD, Klepack E, Lovalvo J, McLain R, Heinonen T. Avasimibe, an ACAT inhibitor, enhances the lipid lowering effect of atorvastatin in subjects with homozygous familial hypercholesterolemia. Atherosclerosis. 2003 Dec;171(2):273-9. PubMed PMID: 14644397.

 

Products are for research use only. Not for human use.

 

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