| Identification | Back Directory | [Name]
PF-06446846 HYDROCHLORIDE | [CAS]
1632250-50-0 | [Synonyms]
PF 6446846 hydrochloride
PF-06446846 HYDROCHLORIDE
PF-06446846 hydrochloride >=98% (HPLC)
N-(3-chloropyridin-2-yl)-N-[(3R)-piperidin-3-yl]-4-(3H-[1,2,3]triazolo[4,5-b]pyridin-3-yl)benzamide hydrochloride | [Molecular Formula]
C22H21Cl2N7O | [MOL File]
1632250-50-0.mol | [Molecular Weight]
470.36 |
| Chemical Properties | Back Directory | [storage temp. ]
room temp | [solubility ]
DMSO : 250 mg/mL (531.52 mM) | [form ]
powder | [color ]
white to beige | [Optical Rotation]
[α]/D -60 to -50°, c = 1 in methanol | [Water Solubility ]
H2O: 2mg/mL, clear | [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 | [InChIKey]
FDTXHWQFIXYHCL-QGZVFWFLSA-N | [SMILES]
O=C(C1=CC=C(N2C(N=CC=C3)=C3N=N2)C=C1)N([C@H]4CNCCC4)C5=C(Cl)C=CC=N5 |
| Hazard Information | Back Directory | [Uses]
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]. | [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]
| [References]
[1] Lintner NG, et al. Selective stalling of human translation through small-molecule engagement of the ribosome nascent chain. PLoS Biol. 2017 Mar 21;15(3):e2001882. DOI:10.1371/journal.pbio.2001882 |
|
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|