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Merck

PZ0233

PF-06424439

≥98% (HPLC), DGAT2 inhibitor, powder

Sinónimos:

[(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinyl-methanone methanesulfonate

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Acerca de este artículo

Fórmula empírica (notación de Hill):
C22H26ClN7O · CH3SO3H
Número CAS:
Peso molecular:
536.05
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.28
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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Nombre del producto

PF-06424439, ≥98% (HPLC)

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

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

Quality Level

Categorías relacionadas

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.

Clase de almacenamiento

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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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
Leslie Magtanong et al.
Cell chemical biology, 26(3), 420-432 (2019-01-29)
The initiation and execution of cell death can be regulated by various lipids. How the levels of environmental (exogenous) lipids impact cell death sensitivity is not well understood. We find that exogenous monounsaturated fatty acids (MUFAs) potently inhibit the non-apoptotic
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)
Micah B Schott et al.
The Journal of cell biology, 218(10), 3320-3335 (2019-08-09)
Lipid droplet (LD) catabolism in hepatocytes is mediated by a combination of lipolysis and a selective autophagic mechanism called lipophagy, but the relative contributions of these seemingly distinct pathways remain unclear. We find that inhibition of lipolysis, lipophagy, or both

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