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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-;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;2-(trans-4-(4-(4-Amino-5-oxo-7,8-dihydropyrimido[5,4-f]-[1,4]oxazepin-6(5H)-yl)phenyl)cyclohex;PF-04620110 | | CAS: | 1109276-89-2 | | MF: | C21H24N4O4 | | MW: | 396.44 | | EINECS: | | | Product Categories: | Inhibitors | | Mol File: | 1109276-89-2.mol |  |
| | 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 |
| Hazard Codes | Xn | | Risk Statements | 22 | | WGK Germany | 3 |
| | 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-04620110 Preparation Products And Raw materials |
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