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Darapladib

Catalog No.
A3349
Lp-PLA2 inhibitor, selective and orally active
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$143.00
In stock
5mg
$113.00
In stock
25mg
$451.00
In stock
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

Darapladib (CAS 356057-34-6) is a selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme strongly implicated in the progression and instability of atherosclerotic plaques. In vitro, Darapladib shows high potency toward Lp-PLA2 (IC50 approximately 270 pM) with minimal inhibition of other secretory PLA2 isoforms (e.g., III, V, X). Preclinical studies in ApoE-deficient mouse models demonstrate that inhibition of Lp-PLA2 attenuates vascular inflammatory processes and markedly reduces atherosclerotic lesion formation. Clinically, Darapladib administration in statin-treated patients significantly decreases plasma Lp-PLA2 activity and inflammatory markers, indicating potential applications in cardiovascular research related to atherosclerosis and associated inflammation.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt666.77
Cas No.356057-34-6
FormulaC36H38F4N4O2S
SynonymsSB-480848;SB480848;SB 480848
Solubility≥32.95 mg/mL in DMSO; insoluble in H2O; ≥891 mg/mL in EtOH
Chemical NameN-[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
SDFDownload SDF
Canonical SMILESCCN(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
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Biological Activity

Description Darapladib (SB-480848) is a reversible inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2) with IC50 of 0.25 nM.
Targets Lp-PLA2          
IC50 0.25 nM          

Quality Control

Chemical structure

Darapladib