1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
  3. PF-06446846 hydrochloride

PF-06446846 hydrochloride 

Cat. No.: HY-120088A
Handling Instructions

PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9 (PCSK9). PF-06446846 hydrochloride inhibits PCSK9 by inducing the ribosome to stall around codon 34.

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

PF-06446846 hydrochloride Chemical Structure

PF-06446846 hydrochloride Chemical Structure

CAS No. : 1632250-50-0

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100 mg USD 2100 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9 (PCSK9). PF-06446846 hydrochloride inhibits PCSK9 by inducing the ribosome to stall around codon 34[1].

IC50 & Target

PCSK9[1]

In Vitro

PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC50 of 0.3 μM[1].

In Vivo

PF-06446846 (oral gavage; 5-50 mg/kg/day for 14 days) lowers plasma PCSK9 in a dose-dependent manner and lowers total cholesterol levels[1].

Animal Model: Male Sprague-Dawley (Crl:CD [SD] rats, 6-8 wk old at initiation of dosing)[1]
Dosage: 5, 15, and 50 mg/kg
Administration: Oral gavage; daily for 14 days
Result: Lowered plasma PCSK9 in a dose-dependent manner and lowered total cholesterol levels.
Molecular Weight

470.35

Formula

C₂₂H₂₁Cl₂N₇O

CAS No.

1632250-50-0

SMILES

O=C(N(C1=NC=CC=C1Cl)[[email protected]]2CNCCC2)C3=CC=C(N4N=NC5=CC=CN=C54)C=C3.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (531.52 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1261 mL 10.6304 mL 21.2608 mL
5 mM 0.4252 mL 2.1261 mL 4.2522 mL
10 mM 0.2126 mL 1.0630 mL 2.1261 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.42 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.42 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

PF-06446846PF06446846PF 06446846Ser/Thr ProteaseSerine proteasesSerine endopeptidasesThreonine proteasesInhibitorinhibitorinhibit

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Product name:
PF-06446846 hydrochloride
Cat. No.:
HY-120088A
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