PF-06446846

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[1].

Product Specifications

CAS Number

[1632250-49-7]

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

PCSK9

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/pf-06446846.html

Solubility

10 mM in DMSO

Smiles

O=C(C1=CC=C(C=C1)N2N=NC3=CC=CN=C32)N([C@H]4CNCCC4)C5=NC=CC=C5Cl

Molecular Formula

C22H20ClN7O

Molecular Weight

433.89

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[1]Nathanael G Lintner, et al. Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain. PLoS Biol. 2018 Apr 17;16 (4) :e1002628.|[2]Allyn T. Londregan, et al. Small Molecule Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9) Inhibitors: Hit to Lead Optimization of Systemic Agents. J Med Chem. 2018 Jul 12;61 (13) :5704-5718.