所有图片(1)
别名:
[(3R)-1-[2-[1-（4-氯-1H-吡唑-1-基）环丙基]-3H-咪唑并 [4,5-b] 吡啶-5-基]-3-哌啶基]-1-吡咯烷甲酮甲磺酸盐
经验公式（希尔记法）:
C22H26ClN7O · CH3SO3H
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质量水平
检测方案
≥98% (HPLC)
形式
powder
旋光性
[α]/D +7 to +11°, c = 1.0 in methanol
颜色
white to light brown
溶解性
H2O: 10 mg/mL, clear
储存温度
room temp
SMILES字符串
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
应用
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
生化/生理作用
PF-06424439 具有降低血脂异常大鼠肝脂质水平的作用。
PF-06424439 是一种强效选择性甘油二酯酰基转移酶 2 (DGAT2) 抑制剂。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°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
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
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)
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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