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SB-435495

Cat. No. M42574
SB-435495 Structure
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Biological Activity

SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM.

Chemical Information
Molecular Weight 720.82
Formula C38H40F4N6O2S
CAS Number 304694-39-1
Form Solid
Solubility (25°C) DMSO 100 mg/mL (Need ultrasonic)
Storage 4°C, dry, sealed
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] Paul Canning et al. Proc Natl Acad Sci U S A. Lipoprotein-associated phospholipase A2 (Lp-PLA2) as a therapeutic target to prevent retinal vasopermeability during diabetes

[2] G L Crawford et al. PLoS One. The role of lipoprotein-associated phospholipase A2 in a murine model of experimental autoimmune uveoretinitis

[3] M L Booker. IDrugs. Lp-PLA2 inhibitors (GlaxoSmithKline)

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

[5] Josie A Blackie et al. Bioorg Med Chem Lett. The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man

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Keywords: SB-435495 supplier, Phospholipase, inhibitors, activators

 
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