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PF-04620110

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PF-04620110 Basic information

Product Name:
PF-04620110
Synonyms:
  • Cyclohexaneacetic acid, 4-[4-(4-amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]-, trans-
  • PF 04620110; PF04620110
  • CS-1117
  • 2-((1r,4r)-4-(4-(4-aMino-5-oxo-7,8-dihydropyriMido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl)cyclohexyl)acetic acid
  • 2-(4-(4-(4-aMiNA-5-oxo-7,8-dihydropyriMido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl)cyclohexyl)acetic acid
  • 2-(trans-4-(4-(4-Amino-5-oxo-7,8-dihydropyrimido[5,4-f]-[1,4]oxazepin-6(5H)-yl)phenyl)cyclohexyl)
  • 2-(trans-4-(4-(4-Amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl)cyclohexyl)acetic acid
  • 2-[4-[4-(4-Amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6-yl)phenyl]cyclohexyl]acetic acid
CAS:
1109276-89-2
MF:
C21H24N4O4
MW:
396.44
Product Categories:
  • Inhibitors
Mol File:
1109276-89-2.mol
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PF-04620110 Chemical Properties

Boiling point:
701.9±60.0 °C(Predicted)
Density 
1.326
storage temp. 
room temp
solubility 
DMSO: soluble10mg/mL (clear solution)
pka
4.72±0.10(Predicted)
form 
powder
color 
white to beige
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Safety Information

Hazard Codes 
Xn
Risk Statements 
22
WGK Germany 
3
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PF-04620110 Usage And Synthesis

Uses

PF 04620110 is an orally-active, inhibitor that has selectivity towards neutral-diglyceride acyltransferase-1 (DGAT-1).

Biological Activity

pf-04620110 is a potent, selective and orally-bioavailable inhibitor of diacylglycerol acyltransferase 1 (dgat-1), an enzyme catalyzing the final committed step in the biosynthesis of triglycerides, that inhibits dgat-1 with values of 50% inhibition concentration ic50 of 19 nm and 8 nm in human and ht-29 cells respectively. pf-04620110 displays a highly selective, more than 100 fold, inhibition against dgat-1 rather than a range of lipid processing enzymes, including human dgat-2, human acyl-coa:cholesterol acyltransferase 1, human acyl-coa:wax alcohol acyltransferase 1, human acyl-coa:wax alcohol acyltransferase 2, human acyl-coa:monacylglycerol acyltransferase 2, human acyl-coa:monacylglycerol acyltransferase 3 and mouse mgat 1.lee kr, choi sh, song js, seo h, chae yj, cho he, ahn jh, ahn sh, bae ma. 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; 27(7):846-852.robert l. dow *, jian-cheng li , michael p. pence , e. michael gibbs , jennifer l. laperle , john litchfield , david w. piotrowski , michael j. munchhof , tara b. manion , william j. zavadoski , gregory s. walker , r. kirk mcpherson , susan tapley , eliot sugarman , angel guzman-perez , and paul dasilva-jardine discovery of pf-04620110, a potent, selective, and orally bioavailable inhibitor of dgat-1. acs med. chem. lett., 2011, 2 (5), pp 407–412

Biochem/physiol Actions

PF-04620110 is known to regulate gut hormones. Inhibition of DGAT1 might serve as a good approach for the treatment of obesity and type 2 diabetes. DGAT1 inhibition might increase the oxidation of fatty acids, thus it is found to be protective against hepatic steatosis.

target

DGAT-1

storage

Store at +4°C

PF-04620110Supplier

Shanghai Boyle Chemical Co., Ltd.
Tel
Email
sales@boylechem.com
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Email
sales@BioChemBest.com
Accendatech Co., LTD.
Tel
13132578992
Email
sales@accendatech.com
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Email
info@chemexpress.com
Shanghai Aladdin Bio-Chem Technology Co.,LTD
Tel
400-400-6206333 18521732826
Email
market@aladdin-e.com
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PF-04620110(1109276-89-2)Related Product Information