2. Metabolic Enzyme/Protease
  3. Ser/Thr Protease
  4. 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.

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (PF-06446846 hydrochloride) that retains the same biological activity.

For research use only. We do not sell to patients.

PF-06446846 Chemical Structure

PF-06446846 Chemical Structure

CAS No. : 1632250-49-7

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PF-06446846 Related Antibodies

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Description

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].

In Vitro

PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM[1]. PF-06446846 inhibits PCSK9(1–35)-luciferase expression with an IC50 of 2 μM[1]. PF-06446846 (Compound 7f) shows rat bone marrow and human CD34+ toxicity[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

PF-06446846 Related Antibodies

Cell Cytotoxicity Assay[2]

Cell Line: Rat bone marrow lineage (−) cell and CD34+ cell
Concentration: 0-20 µM
Incubation Time: 72 h
Result: Showed cytotoxicity with IC50 values of 2.9 µM and 2.7 µM against rat Lin(−) and human CD34+, respectively.
In Vivo

PF-06446846 reduces circulating PCSK9 and total plasma cholesterol levels in vivo without obvious toxicity[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague-Dawley (Crl:CD [SD] rats, five per group; 6–8 wk old at initiation of dosing)[1]
Dosage: 5, 15, and 50 mg/kg
Administration: Oral administration, daily, 14 days
Result: Reduced plasma PCSK9, total plasma cholesterol, and LDL-C (low-density lipoprotein cholesterol) in a dose-dependent manner without obvious toxicity.
Molecular Weight

433.89

Formula

C22H20ClN7O
CAS No.
SMILES

O=C(C1=CC=C(C=C1)N2N=NC3=CC=CN=C32)N([C@H]4CNCCC4)C5=NC=CC=C5Cl
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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PF-06446846 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-064468461632250-49-7PF06446846PF 06446846Ser/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasesSelective80S ribosomeHuh7Rat bone marrowInhibitorinhibitorinhibit

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