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CP-195543 

Cat. No. M29132
CP-195543  Structure
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Quality Control & Documentation
Biological Activity

CP-195543 is a potent, selective and orally active leukotriene B4 (LTB4) receptor antagonist with IC50s of 6.8, 37.0 nM for human neutrophils and murine spleen membranes, respectively. CP-195543 blocks CD11b up-regulation. CP-195543 inhibits LTB4-mediated neutrophil infiltration.

Chemical Information
Molecular Weight 428.4
Formula C24H19F3O4
CAS Number 204981-48-6
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] S Caron. Curr Opin Drug Discov Devel. The synthesis of CP-195543, an LTB4 antagonist for the treatment of inflammatory diseases

[2] Lisa Fischer, et al. Biochim Biophys Acta. Leukotriene and purinergic receptors are involved in the hyperpolarizing effect of glucagon in liver cells

[3] T Yokomizo, et al. J Biol Chem. Hydroxyeicosanoids bind to and activate the low affinity leukotriene B4 receptor, BLT2

[4] L A Reiter, et al. Bioorg Med Chem Lett. trans-3-Benzyl-4-hydroxy-7-chromanylbenzoic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor

[5] H J Showell, et al. J Pharmacol Exp Ther. The preclinical pharmacological profile of the potent and selective leukotriene B4 antagonist CP-195543

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Keywords: CP-195543  supplier, Leukotriene Receptor, inhibitors, activators


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