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Merck
CN

PZ0233

PF-06424439

≥98% (HPLC), DGAT2 inhibitor, powder

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

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关于此项目

经验公式(希尔记法):
C22H26ClN7O · CH3SO3H
化学文摘社编号:
分子量:
536.05
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.28
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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产品名称

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

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

Biochem/physiol Actions

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 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。


存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



历史批次信息供参考:

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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)



全球贸易项目编号

货号GTIN
PZ0233-25MG04061833058152
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