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PF-06446846 

Cat. No. M28735
PF-06446846  Structure
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Biological Activity

PF-06446846 is an orally active proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PF-06446846 directly and selectively inhibits translation of PCSK9 by stalling the 80S ribosome in the proximity of codon region.

Chemical Information
Molecular Weight 433.89
Formula C22H20ClN7O
CAS Number 1632250-49-7
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] Di Zhang, et al. Small. An Injectable Hydrogel to Modulate T Cells for Cancer Immunotherapy

[2] Dafne Jacome Sanz, et al. Cancers (Basel). Evaluating Targeted Therapies in Ovarian Cancer Metabolism: Novel Role for PCSK9 and Second Generation mTOR Inhibitors

[3] Wenfei Li, et al. Nat Commun. Selective inhibition of human translation termination by a drug-like compound

[4] Wenfei Li, et al. Nat Struct Mol Biol. Structural basis for selective stalling of human ribosome nascent chain complexes by a drug-like molecule

[5] Nathanael G Lintner, et al. PLoS Biol. Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain

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  Catalog
Abmole Inhibitor Catalog




Keywords: PF-06446846  supplier, PCSK9, inhibitors, activators


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