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Darapladib

Cat. No. M2759
Darapladib Structure
Synonym:

SB-480848

Size Price Availability Quantity
5mg USD 140  USD140 In stock
10mg USD 250  USD250 In stock
25mg USD 540  USD540 In stock
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Quality Control & Documentation
Biological Activity

Darapladib is a novel inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme that may link lipid metabolism with inflammation, leading to the increased stability of atherosclerotic plaques present in the major arteries. 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. Darapladib is being studied as a possible add-on treatment for atherosclerosis.

Chemical Information
Molecular Weight 666.77
Formula C36H38F4N4O2S
CAS Number 356057-34-6
Solubility (25°C) DMSO 70 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Acharya NK, et al. J Alzheimers Dis. Diabetes and hypercholesterolemia increase blood-brain barrier permeability and brain amyloid deposition: beneficial effects of the LpPLA2 inhibitor darapladib.

[2] Wilensky RL, et al. Nat Med. Inhibition of lipoprotein-associated phospholipase A2 reduces complex coronary atherosclerotic plaque development.

[3] Blackie JA, et al. Bioorg Med Chem Lett. The identification of clinical candidate SB-480848: a potent inhibitor of lipoprotein-associated phospholipase A2.

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