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Key Documents

PZ0233

Sigma-Aldrich

PF-06424439

≥98% (HPLC)

Synonyme(s) :

[(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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About This Item

Formule empirique (notation de Hill):
C22H26ClN7O · CH3SO3H
Numéro CAS:
Poids moléculaire :
536.05
Code UNSPSC :
12352200
ID de substance PubChem :

Niveau de qualité

Pureté

≥98% (HPLC)

Forme

powder

Activité optique

[α]/D +7 to +11°, c = 1.0 in methanol

Couleur

white to light brown

Solubilité

H2O: 10 mg/mL, clear

Température de stockage

room temp

Chaîne SMILES 

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

Clé InChI

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

Actions biochimiques/physiologiques

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).

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable


Certificats d'analyse (COA)

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Les clients ont également consulté

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
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
Nimesha Tadepalle et al.
Life science alliance, 3(6) (2020-04-24)
Lipid droplets (LDs) are metabolic organelles that store neutral lipids and dynamically respond to changes in energy availability by accumulating or mobilizing triacylglycerols (TAGs). How the plastic behavior of LDs is regulated is poorly understood. Hereditary spastic paraplegia is a

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