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Merck
CN

PZ0374

PF-06446846 hydrochloride

≥98% (HPLC)

Synonym(s):

N-(3-Chloropyridin-2-yl)-N-((3R)-piperidin-3-yl)-4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)benzamide hydrochloride

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About This Item

Empirical Formula (Hill Notation):
C22H20ClN7O · xHCl
CAS Number:
1632250-50-0
Molecular Weight:
433.89 (free base basis)
UNSPSC Code:
41121800
NACRES:
NA.77

Key Documents

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Assay

≥98% (HPLC)

form

powder

optical activity

[α]/D -60 to -50°, c = 1 in methanol

storage condition

desiccated

color

white to beige

solubility

H2O: 2 mg/mL, clear

storage temp.

room temp

SMILES string

O=C(C1=CC=C(N2C(N=CC=C3)=C3N=N2)C=C1)N([C@H]4CNCCC4)C5=C(Cl)C=CC=N5

InChI

1S/C22H20ClN7O/c23-18-5-2-12-25-20(18)29(17-4-1-11-24-14-17)22(31)15-7-9-16(10-8-15)30-21-19(27-28-30)6-3-13-26-21/h2-3,5-10,12-13,17,24H,1,4,11,14H2/t17-/m1/s1

InChI key

FDTXHWQFIXYHCL-QGZVFWFLSA-N

Biochem/physiol Actions

PF-06446846 is a selective orally active PCSK9 inhibitor that appears to act by causing the ribosome to stall when synthesizing PCSK9. PCSK9 binds to the LDL receptor, preventing it from removing LDL cholesterol from the blood. PF-06446846 was found to reduce plasma PCSK9 and total cholesterol levels in rats.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

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Certificates of Analysis (COA)

Lot/Batch Number
0000386284
0000386284
0000290070
0000290070
0000157666

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Nathanael G Lintner et al.
PLoS biology, 15(3), e2001882-e2001882 (2017-03-23)
Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a key role in regulating the levels of plasma low-density lipoprotein cholesterol (LDL-C). Here, we demonstrate that the compound PF-06446846 inhibits translation of PCSK9 by inducing the ribosome to stall around codon 34

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