产品名称
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
Biochem/physiol Actions
PF-06424439 是一种强效选择性 DGAT2 抑制剂。
PF-06424439 是一种强效选择性甘油二酯酰基转移酶 2 (DGAT2) 抑制剂。
PF-06424439 具有降低血脂异常大鼠肝脂质水平的作用。
Application
使用 PF-06424439 作为二酰基甘油酰基转移酶 2(DGAT2)的抑制剂:
- 研究其对结肠上皮细胞和结肠癌干细胞中细胞死亡率和脂质合成的影响
- 研究其对 HeLa 细胞的影响
- 研究其对 HT-1080 细胞中性脂类合成的抑制作用
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
Veijo T Salo et al.
Developmental cell, 50(4), 478-493 (2019-06-11)
Seipin is an oligomeric integral endoplasmic reticulum (ER) protein involved in lipid droplet (LD) biogenesis. To study the role of seipin in LD formation, we relocalized it to the nuclear envelope and found that LDs formed at these new seipin-defined
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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