Darapladib - 356057-34-6
Darapladib
Catalog Number: BT-264452
CAS Number: 356057-34-6
Molecular Formula: C36H38F4N4O2S
Molecular Weight: 666.8 g/mol
The product is for non-human research only. Not for therapeutic or veterinary use.
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Product Introduction
Description
Darapladib is a small molecule inhibitor that has been developed as a potential therapeutic agent for the treatment of cardiovascular diseases. It is a potent inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme that is involved in the formation of atherosclerotic plaques in the arteries. Darapladib has been extensively studied in preclinical and clinical trials, and its potential therapeutic benefits and safety profile have been evaluated.
Properties
CAS Number
356057-34-6
Product Name
Darapladib
IUPAC Name
N-[2-(diethylamino)ethyl]-2-[2-[(4-fluorophenyl)methylsulfanyl]-4-oxo-6,7-dihydro-5H-cyclopenta[d]pyrimidin-1-yl]-N-[[4-[4-(trifluoromethyl)phenyl]phenyl]methyl]acetamide
Molecular Formula
C36H38F4N4O2S
Molecular Weight
666.8 g/mol
InChI
InChI=1S/C36H38F4N4O2S/c1-3-42(4-2)20-21-43(22-25-8-12-27(13-9-25)28-14-16-29(17-15-28)36(38,39)40)33(45)23-44-32-7-5-6-31(32)34(46)41-35(44)47-24-26-10-18-30(37)19-11-26/h8-19H,3-7,20-24H2,1-2H3
InChI Key
WDPFJWLDPVQCAJ-UHFFFAOYSA-N
SMILES
CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C4=C(CCC4)C(=O)N=C3SCC5=CC=C(C=C5)F
Solubility
Soluble in DMSO, not in water
Synonyms
SB-480848; SB 480848; SB480848; Darapladib.
Canonical SMILES
CCN(CC)CCN(CC1=CC=C(C=C1)C2=CC=C(C=C2)C(F)(F)F)C(=O)CN3C4=C(CCC4)C(=O)N=C3SCC5=CC=C(C=C5)F
Method of Synthesis or Extraction
Darapladib is a synthetic compound that is typically prepared using a multi-step chemical synthesis process. The most commonly used method involves the reaction of a substituted pyridine with a substituted benzene to form an intermediate compound, which is then further modified to produce darapladib. The efficiency and yield of this method can vary depending on the specific reaction conditions and the quality of the starting materials. Environmental and safety considerations are also important factors to consider during the synthesis process, as some of the reagents and solvents used can be hazardous to human health and the environment.
Chemical Structure and Biological Activity
Darapladib is a small molecule inhibitor that has a molecular weight of 394.4 g/mol and a chemical formula of C23H28N2O4S. It is a potent inhibitor of Darapladib, an enzyme that is involved in the formation of atherosclerotic plaques in the arteries. By inhibiting Darapladib, darapladib can reduce the levels of oxidized phospholipids in the blood, which are known to contribute to the development of cardiovascular disease. Darapladib has been shown to have a high degree of selectivity for Darapladib, with minimal effects on other enzymes or biological targets.
Biological Effects
Darapladib has been shown to have a number of biological effects on cell function and signal transduction. In preclinical studies, darapladib has been shown to reduce the formation of atherosclerotic plaques in animal models of cardiovascular disease. It has also been shown to have anti-inflammatory effects, which may contribute to its therapeutic benefits. However, darapladib has also been associated with potential toxic effects, including liver toxicity and gastrointestinal side effects.
Applications
Darapladib has been studied extensively in medical research, particularly in the context of its potential role in drug development for the treatment of cardiovascular disease. Clinical trials have shown that darapladib can reduce the risk of major cardiovascular events, such as heart attack and stroke, in patients with stable coronary heart disease. However, the benefits of darapladib may be limited to certain patient populations, and further research is needed to fully understand its potential therapeutic benefits and side effects.
In environmental research, darapladib has been studied for its effects on ecosystems and its potential role in pollution management. However, there is currently limited research on the environmental impact of darapladib, and further studies are needed to fully understand its potential effects on the environment.
In industrial research, darapladib has been studied for its use in manufacturing processes and its potential to improve product quality and efficiency. Health and safety considerations are important factors to consider in the industrial use of darapladib, as it can be hazardous to human health and the environment if not handled properly.
Future Perspectives and Challenges
Despite its potential therapeutic benefits, there are currently limitations in the use and study of darapladib. One of the main challenges is the high cost of the drug, which may limit its accessibility to patients. Additionally, further research is needed to fully understand the potential side effects of darapladib and to identify patient populations that may benefit most from its use. Future trends and prospects in the application of darapladib in scientific research will likely focus on identifying new therapeutic targets and developing more effective and affordable treatment options for cardiovascular disease.
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