product name Darapladib (SB-480848)
Description: Darapladib, also known as SB-480848, is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM, which is in Phase 3 trials. Recent studies showed that risk of major coronary events not reduced by darapladib therapy. In patients with stable coronary heart disease, darapladib did not significantly reduce the risk of the primary composite end point of cardiovascular death, myocardial infarction, or stroke.
References: Bioorg Med Chem Lett. 2003;13(6):1067-70; Nat Med. 2008;14(10):1059-66; J Alzheimers Dis. 2013;35(1):179-98.
666.77
Formula
C36H38F4N4O2S
CAS No.
356057-34-6
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (150.0 mM)
Water: <1 mg/mL
Ethanol: 100 mg/mL (150.0 mM)
Solubility (In vivo)
Synonyms
SB-480848
other peoduct :
| In Vitro |
In vitro activity: During the copper catalysed oxidation of human LDL, Darapladib prevents the production of lyso-PtdCho with IC50 of 4 nM and subsequent monocyte chemotaxis with IC50 of 4 nM. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | In the WHHL rabbits, Darapladib (30 mg/kg p.o.) exhibits excellent inhibition of Lp-PLA2 within the atherosclerotic plaque by 95%. Darapladib, as an inhibitor of Lp-PLA2, reduces development of advanced coronary atherosclerosis in diabetic and hypercholesterolemic (DMHC) pigs. In DMHC pigs, darapladib reduces the amount of IgG-immunopositive material that leaked into the brain and also the density of Aβ42-containing neurons. |
| Animal model | WHHL rabbits |
| Formulation & Dosage | Dissolved in 1% aq methylcellulose; 30 mg/kg; p.o. |
| References | Bioorg Med Chem Lett. 2003 Mar 24;13(6):1067-70; Nat Med. 2008 Oct;14(10):1059-66; J Alzheimers Dis. 2013;35(1):179-98. |
