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About This Item
Empirical Formula (Hill Notation):
C22H26ClN7O · CH3SO3H
CAS Number:
Molecular Weight:
536.05
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.28
Product Name
PF-06424439, ≥98% (HPLC)
Quality Level
assay
≥98% (HPLC)
form
powder
optical activity
[α]/D +7 to +11°, c = 1.0 in methanol
color
white to light brown
solubility
H2O: 10 mg/mL, clear
storage temp.
room temp
SMILES string
O=C([C@@H]1CCCN(C2=NC(NC(C3(CC3)N4N=CC(Cl)=C4)=N5)=C5C=C2)C1)N6CCCC6.CS(=O)(O)=O
InChI
1S/C22H26ClN7O.CH4O3S/c23-16-12-24-30(14-16)22(7-8-22)21-25-17-5-6-18(26-19(17)27-21)29-11-3-4-15(13-29)20(31)28-9-1-2-10-28;1-5(2,3)4/h5-6,12,14-15H,1-4,7-11,13H2,(H,25,26,27);1H3,(H,2,3,4)/t15-;/m1./s1
InChI key
ZSTFDNQQOJUJFL-XFULWGLBSA-N
Application
PF-06424439 has been used as a diacylglycerol acyltransferase 2 (DGAT2) inhibitor:
- to study its effects on cell mortality and lipid synthesis in epithelial colon cells and colorectal cancer stem cells
- to study its effects on HeLa cells
- to study its inhibitory effects on neutral lipid synthesis in HT-1080 cells
Biochem/physiol Actions
PF-06424439 functions in reducing the hepatic lipid levels in dyslipidemic rats.
PF-06424439 is a potent and selective inhibitor of diacylglycerol acyltransferase 2 (DGAT2).
PF-06424439 is a potent, selective DGAT2 inhibitor.
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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Articles
Discover Bioactive Small Molecules for Lipid Signaling Research
Kentaro Futatsugi et al.
Journal of medicinal chemistry, 58(18), 7173-7185 (2015-09-09)
The medicinal chemistry and preclinical biology of imidazopyridine-based inhibitors of diacylglycerol acyltransferase 2 (DGAT2) is described. A screening hit 1 with low lipophilic efficiency (LipE) was optimized through two key structural modifications: (1) identification of the pyrrolidine amide group for
Masaaki Uematsu et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 34(8), 10357-10372 (2020-06-28)
Visualizing intracellular fatty acids (including free and esterified form) is very useful for understanding how and where such molecules are incorporated, stored, and metabolized within cells. However, techniques of imaging multiple intracellular fatty acids have been limited by their small
Alexandre Santinho et al.
Current biology : CB, 30(13), 2481-2494 (2020-05-23)
Lipid droplet (LD) biogenesis begins in the endoplasmic reticulum (ER) bilayer, but how the ER topology impacts this process is unclear. An early step in LD formation is nucleation, wherein free neutral lipids, mainly triacylglycerols (TGs) and sterol esters (SEs)
Global Trade Item Number
| SKU | GTIN |
|---|---|
| PZ0233-25MG | 04061833058152 |
| PZ0233-5MG | 04061833058169 |