PF-04620110


CAS No. : 1109276-89-2

PF-04620110,1109276-89-2
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000443
Synonyms:2-[4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6-yl)phenyl]cyclohexyl]acetic acid
Molecular Formula:C21H24N4O4
Molecular Weight:396.4
Target:Transferase
IC50:19 nM
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Appearance:Solid powder
Purity: > 98%
Cat No:I000443
Cas No:1109276-89-2
Product-Name:PF-04620110
InChIKey:GEVVQZHMFVFGLN-HDJSIYSDSA-N
SMILES:OC(C[C@@H]1CC[C@@H](C2=CC=C(N3CCOC(N=CN=C4N)=C4C3=O)C=C2)CC1)=O

PF-04620110(cas 1109276-89-2) is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
 It has high oral bioavailability (100%) in rats, with a moderate half-life of 6.8 hours. PF-04620110 significantly blocks an increase in plasma triglyceride levels following a corn oil bolus in rats.

1:Defining the key pharmacophore elements of PF-04620110: discovery of a potent, orally-active, neutral DGAT-1 inhibitor. Dow RL, Andrews MP, Li JC, Michael Gibbs E, Guzman-Perez A, Laperle JL, Li Q, Mather D, Munchhof MJ, Niosi M, Patel L, Perreault C, Tapley S, Zavadoski WJ.Bioorg Med Chem. 2013 Sep 1;21(17):5081-97. doi: 10.1016/j.bmc.2013.06.045. Epub 2013 Jul 1. PMID: 23871442
2: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. Lee KR, Choi SH, Song JS, Seo H, Chae YJ, Cho HE, Ahn JH, Ahn SH, Bae MA.Biomed Chromatogr. 2013 Jul;27(7):846-52. doi: 10.1002/bmc.2869. Epub 2013 Feb 19. PMID: 23420715
3:Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1. Dow RL, Li JC, Pence MP, Gibbs EM, LaPerle JL, Litchfield J, Piotrowski DW, Munchhof MJ, Manion TB, Zavadoski WJ, Walker GS, McPherson RK, Tapley S, Sugarman E, Guzman-Perez A, DaSilva-Jardine P.ACS Med Chem Lett. 2011 Mar 18;2(5):407-12. doi: 10.1021/ml200051p. eCollection 2011 May 12. PMID: 24900321 Free PMC Article
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