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PF-04620110

Chemical Structure : PF-04620110

CAS No.: 1109276-89-2

PF-04620110 (PF 04620110, PF04620110)

Catalog No.: PC-43318Not For Human Use, Lab Use Only.

PF-04620110 is a potent, selective, orally bioavailable DGAT-1 inhibitor with IC50 of 19 nM, shows no acitivity for DGAT-2 (IC50>30 uM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

PF-04620110 is a potent, selective, orally bioavailable DGAT-1 inhibitor with IC50 of 19 nM, shows no acitivity for DGAT-2 (IC50>30 uM).
PF-04620110 shows high selectivity versus a broad panel of off-target pharmacologic end points.
PF-04620110 inhibits triglyceride synthesis of 3 in the intestinal-derived HT-29 cell line with IC50 of 8 nM.
PF-04620110 demonstrates in vivo DGAT-1 inhibitionthrough reduction of plasma triglyceride levels in rodent, alters the temporal and spatial pattern of dietary lipid absorption in vivo.

Physicochemical Properties

M.Wt 396.4397
Formula C21H24N4O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

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

References

1. Dow RL, et al. ACS Med Chem Lett. 2011 Mar 18;2(5):407-12.

2. Maciejewski BS, et al. Am J Physiol Gastrointest Liver Physiol. 2013 Jun 1;304(11):G958-69.

3. Maciejewski BS, et al. World J Gastrointest Pathophysiol. 2017 Nov 15;8(4):161-175.

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