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GNF6702 

Cat. No. M28866
GNF6702  Structure
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Biological Activity

GNF6702 is a selective inhibitor of the kinetoplastid proteasome. GNF6702 clears parasites in murine models of leishmaniasis, Chagas disease, and human African trypanosomiasis.

Chemical Information
Molecular Weight 429.41
Formula C22H16FN7O2
CAS Number 1799329-72-8
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] Advait Nagle, et al. J Med Chem. Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases

[2] Srinivasa P S Rao, et al. Trop Med Infect Dis. Anti-Trypanosomal Proteasome Inhibitors Cure Hemolymphatic and Meningoencephalic Murine Infection Models of African Trypanosomiasis

[3] Alane Beatriz Vermelho, et al. Expert Opin Drug Discov. Why hasn't there been more progress in new Chagas disease drug discovery?

[4] Patrícia de Almeida Machado, et al. Life Sci. Leishmanicidal therapy targeted to parasite proteases

[5] Shilpi Khare, et al. Nature. Proteasome inhibition for treatment of leishmaniasis, Chagas disease and sleeping sickness

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Keywords: GNF6702  supplier, Parasite, inhibitors, activators


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