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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); shows high selectivity versus a broad panel of off-target pharmacologic end points; inhibits triglyceride synthesis of 3 in the intestinal-derived HT-29 cell line with IC50 of 8 nM; 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.

Diabetes

Phase 1 Discontinued

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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