PF-04620110

产品说明书

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Chemical Structure| 1109276-89-2 同义名 : -
CAS号 : 1109276-89-2
货号 : A853379
分子式 : C21H24N4O4
纯度 : 99%
分子量 : 396.44
MDL号 : MFCD19443642
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(30.27 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • Transferase

    DGAT1, IC50:19 nM
描述 PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01166217 Healthy Phase 1 Completed - Singapore ... 展开 >> Pfizer Investigational Site Singapore, Singapore, 188770 收起 <<
NCT01064492 Healthy Volunteers Phase 1 Completed - Belgium ... 展开 >> Pfizer Investigational Site Bruxelles, Belgium, 1070 收起 <<
NCT01474941 Healthy Phase 1 Completed - Belgium ... 展开 >> Pfizer Investigational Site Bruxelles, Belgium, B-1070 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.61mL

2.52mL

1.26mL

25.22mL

5.04mL

2.52mL
参考文献

[1]Lee KR, Choi SH, et al. Determination of PF-04620110, a novel inhibitor of diacylglycerol acyltransferase-1, in rat plasma using liquid chromatography-tandem mass spectrometry and its application in pharmacokinetic studies. Biomed Chromatogr. 2013 Jul;27(7):846-52.

[2]Dow RL, Andrews M, et al. Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3-d] pyrimidine core. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6122-5.