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PPI-2458 

Cat. No. M30084
PPI-2458  Structure
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Biological Activity

PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research.

Chemical Information
Molecular Weight 424.53
Formula C22H36N2O6
CAS Number 431077-35-9
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] Christopher C Arico-Muendel, et al. Drug Metab Dispos. Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity

[2] D D Lazarus, et al. Inflamm Res. An inhibitor of methionine aminopeptidase type-2, PPI-2458, ameliorates the pathophysiological disease processes of rheumatoid arthritis

[3] Gerhard Hannig, et al. Arthritis Rheum. Suppression of inflammation and structural damage in experimental arthritis through molecular targeted therapy with PPI-2458

[4] Andrew C Cooper, et al. Clin Cancer Res. A novel methionine aminopeptidase-2 inhibitor, PPI-2458, inhibits non-Hodgkin's lymphoma cell proliferation in vitro and in vivo

[5] Sylvie G Bernier, et al. Proc Natl Acad Sci U S A. A methionine aminopeptidase-2 inhibitor, PPI-2458, for the treatment of rheumatoid arthritis

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Keywords: PPI-2458  supplier, inhibitors, activators


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