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PZ0207

Sigma-Aldrich

PF-04620110

≥98% (HPLC)

别名:

trans-4-[4-(4-Amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]-cyclohexaneacetic acid

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About This Item

经验公式（希尔记法）:
C21H24N4O4
CAS号:
1109276-89-2
分子量:
396.44
UNSPSC代码:
12352202
PubChem化学物质编号:
329823775
NACRES:
NA.77
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质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 10 mg/mL (clear solution)

储存温度

room temp

SMILES字符串

Nc1ncnc2OCCN(C(=O)c12)c3ccc(cc3)[C@@H]4CC[C@H](CC4)CC(O)=O

InChI

1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)/t13-,14-

InChI key

GEVVQZHMFVFGLN-HDJSIYSDSA-N

生化/生理作用

PF-04620110 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that inhibits triacylglycerol synthesis in cells and in rodents.
PF-04620110 is an orally active, selective and potent DGAT1 inhibitor.
PF-04620110 is known to regulate gut hormones.[1] Inhibition of DGAT1 might serve as a good approach for the treatment of obesity and type 2 diabetes.[2] DGAT1 inhibition might increase the oxidation of fatty acids, thus it is found to be protective against hepatic steatosis.[3]

象形图

Exclamation mark
GHS07

警示用语：

Warning

危险声明

H302

危险分类

Acute Tox. 4 Oral

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000376148
0000376148
082M4721V
0000187925

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Specific role for acyl CoA: Diacylglycerol acyltransferase 1 (Dgat1) in hepatic steatosis due to exogenous fatty acids
Villanueva CJ, et al.
Hepatology, 50(2), 434-442 (2009)
Targeting Acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases
Cao J, et al.
The Journal of biological chemistry, jbc-M111 (2011)
Targeting Acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases
Cao J, et al.
The Journal of Biological Chemistry, jbc-M111 (2011)
Targeting Acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) with small molecule inhibitors for the treatment of metabolic diseases
Cao J, et al.
Test, jbc-M111 (2011)
New Therapeutic Strategies for Type 2 Diabetes: Small Molecule Approaches, 237-237 (2012)
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Questions

  1. I need pharmacokinetics and pharmacodynamics study sheet for PF-0420110 product please, what is the half life of this DGAT1 inhibitor?

    1 answer

    1. Unfortunately, pharmacokinetic, pharmacodynamic, and half-like information on this product are not available. The compound was developed by Pfizer, however, this product is intended for research use only. Some publications may be of interest.

      See the link below for one such article.
      https://pubs.acs.org/doi/10.1021/ml200051p

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