Basic information Safety Supplier Related

PF-06446846 HYDROCHLORIDE

Basic information Safety Supplier Related

PF-06446846 HYDROCHLORIDE Basic information

Product Name:
PF-06446846 HYDROCHLORIDE
Synonyms:
  • PF-06446846 HYDROCHLORIDE
  • N-(3-chloropyridin-2-yl)-N-[(3R)-piperidin-3-yl]-4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)benzamide hydrochloride
  • PF 6446846 hydrochloride
  • PF-06446846 hydrochloride >=98% (HPLC)
  • PF06446846 hydrochloride,PF 06446846 hydrochloride
  • (R)-4-(3H-[1,2,3]Triazolo[4,5-b]pyridin-3-yl)-N-(3-chloropyridin-2-yl)-N-(piperidin-3-yl)benzamide xhydrochloride
CAS:
1632250-50-0
MF:
C22H21Cl2N7O
MW:
470.36
Mol File:
1632250-50-0.mol
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PF-06446846 HYDROCHLORIDE Chemical Properties

storage temp. 
room temp
solubility 
DMSO : 250 mg/mL (531.52 mM)
form 
powder
color 
white to beige
optical activity
[α]/D -60 to -50°, c = 1 in methanol
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PF-06446846 HYDROCHLORIDE Usage And Synthesis

Biological Activity

PF-06446846 hydrochloride is an orally active, highly selective translation inhibitor of the proprotein convertase subtilisin/kexin type 9 (PCSK9). It inhibits PCSK9 by inducing ribosome parking around codon 34.

in vitro

PF-06446846 inhibits the secretion of PCSK9 by Huh7 cells with an IC 50 of 0.3 μM.

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.

Animal Model: Male Sprague-Dawley (Crl:CD [SD] rats, 6-8 wk old at initiation of dosing)
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.

target

PCSK9

PF-06446846 HYDROCHLORIDESupplier

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