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
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
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
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.
저장 등급
11 - Combustible Solids
wgk
WGK 3
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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