A reversible inhibitor of Lp-PLA2 (IC50 = 0.25 nM) that produces sustained inhibition of plasma Lp-PLA2 activity in humans

Darapladib – 5 mg

Brand:
Cayman
CAS:
356057-34-6
Storage:
-20
UN-No:
Non-Hazardous - /

Lipoprotein-associated phospholipase A2 (Lp-PLA2), also known as platelet activating factor acetylhydrolase (PAF-AH) or phospholipase A2 group 7 (PLA2G7), hydrolyzes glycerophospholipids to produce lyso-PAF/lyso-phosphatidylcholine and short and/or oxidized fatty acids, many of which have pro-inflammatory or pro-oxidative activities.{26682,26483} Darapladib is a reversible inhibitor of Lp-PLA2 (IC50 = 0.25 nM).{27391} It produces sustained inhibition of plasma Lp-PLA2 activity in humans receiving intensive atorvastatin therapy.{27387} Lp-PLA2 inhibition with darapladib also reduces the development of coronary atherosclerotic plaques.{27388,27390}  

 

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Description

A reversible inhibitor of Lp-PLA2 (IC50 = 0.25 nM) that produces sustained inhibition of plasma Lp-PLA2 activity in humans

Formal name: N-[2-(diethylamino)ethyl]-2-[[(4-fluorophenyl)methyl]thio]-4,5,6,7-tetrahydro-4-oxo-N-[[4′-(trifluoromethyl)[1,1′-biphenyl]-4-yl]methyl]-1H-cyclopentapyrimidine-1-acetamide

Synonyms:  SB-480848

Molecular weight: 666.8

CAS: 356057-34-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Phospholipases||Research Area|Cardiovascular System|Cardiovascular Diseases|Atherosclerosis||Research Area|Cardiovascular System|Lipids & Lipoproteins||Research Area|Lipid Biochemistry|Glycerophospholipids|Phospholipases

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