681245-85-2

Usage

Uses

Used in Cardiovascular Applications:
Avasimibe is utilized as a therapeutic agent for the treatment of atherosclerosis and cardiovascular diseases. Its application is based on its ability to reduce cholesterol accumulation in cells, which is a critical factor in the development of atherosclerotic lesions. By inhibiting ACAT, Avasimibe helps in preventing the formation of these lesions, thereby reducing the risk of cardiovascular events.
Used in Pharmaceutical Development:
In the pharmaceutical industry, Avasimibe is considered a promising compound for the development of new medications aimed at managing lipid metabolism. Its potential to prevent atherosclerosis makes it a valuable asset in the quest for innovative treatments for cardiovascular diseases, which are among the leading causes of mortality worldwide.
Used in Research Studies:
Avasimibe is also used in scientific research as a tool to study the mechanisms of cholesterol esterification and the role of ACAT in lipid metabolism. Its application in research settings helps in advancing our understanding of the pathophysiology of atherosclerosis and the potential for targeted therapies to combat this condition.
Used in Drug Delivery Systems:
Similar to gallotannin, Avasimibe may also benefit from novel drug delivery systems to enhance its bioavailability and therapeutic efficacy. The development of such systems could improve the delivery of Avasimibe to target tissues, potentially increasing its effectiveness in treating atherosclerosis and cardiovascular diseases.

Upstream product

• 681247-91-6 methyl 2-[({2-[(1Z)-3-(diethylamino)-1-propenyl]phenyl}sulfonyl)amino]-5,6,7,8-tetrahydro-1-naphthalenecarboxylate 
• 681247-87-0 N,N-diethyl-N-((Z)-1-tributylstannanylprop-1-en-3-yl)-amine 
• 846540-87-2 2-trifluoromethanesulfonyloxy-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid methyl ester 
• 681248-34-0 methyl 2-({[2-bromophenyl]sulfonyl}amino)-5,6,7,8-tetrahydro-1-naphthalenecarboxylate 
• 900492-90-2 2-(benzhydrylidene-amino)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid methyl ester 
• 947-65-9 methyl 2-hydroxy-1-naphthoate 
• 59604-96-5 2-hydroxy-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid methyl ester 
• 681247-89-2 methyl 2-[({2-[(1E)-3-(diethylamino)-1-propenyl]phenyl}sulfonyl)amino]-5,6,7,8-tetrahydro-1-naphthalenecarboxylate 
• 681247-87-0 N,N-diethyl-N-[(2E)-3-(tributylstannyl)-2-propenyl]amine 

Relevant academic research and scientific papers

Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: A structural basis for the reduction of albumin binding

Methionine aminopeptidase-2 (MetAP2) is a novel target for cancer therapy. As part of an effort to discover orally active reversible inhibitors of MetAP2, a series of anthranilic acid sulfonamides with micromolar affinities for human MetAP2 were identified using affinity selection by mass spectrometry (ASMS) screening. These micromolar hits were rapidly improved to nanomolar leads on the basis of insights from protein crystallography; however, the compounds displayed extensive binding to human serum albumin and had limited activity in cellular assays. Modifications based on structural information on the binding of lead compounds to both MetAP2 and domain III of albumin allowed the identification of compounds with significant improvements in both parameters, which showed good cellular activity in both proliferation and methionine processing assays.

Sulfonamides having antiangiogenic and anticancer activity

Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.

Sulfonamides having antiangiogenic and anticancer activity

Compounds having methionine aminopeptidase-2 inhibitory (MetAP2) are described. Also described are pharmaceutical compositions comprising the compounds, methods of treatment using the compounds, methods of inhibiting angiogenesis, and methods of treating cancer.