PF 04620110

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Cat.No. 5863 - PF 04620110 | C21H24N4O4 | CAS No. 1109276-89-2
Description: Potent and selective DGAT-1 inhibitor; orally bioavailable
Chemical Name: trans-4-[4-(4-Amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]cyclohexaneacetic acid
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective DGAT-1 inhibitor (IC50 = 19 nM). Exhibits >1000-fold selectivity for DGAT-1 over DGAT-2, and no significant activity against a range of other enzymes, ion channels and receptors. Reduces plasma triglyceride levels in a rat lipid challenge model. Orally bioavailable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M. Wt 396.44
Formula C21H24N4O4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 1109276-89-2
PubChem ID 46926360
InChI Key GEVVQZHMFVFGLN-UHFFFAOYSA-N
Smiles O=C1N(C2=CC=C([C@@H]3CC[C@@H](CC(O)=O)CC3)C=C2)CCOC4=NC=NC(N)=C41

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 7.93 20

Preparing Stock Solutions

The following data is based on the product molecular weight 396.44. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.2 mM 12.61 mL 63.06 mL 126.12 mL
1 mM 2.52 mL 12.61 mL 25.22 mL
2 mM 1.26 mL 6.31 mL 12.61 mL
10 mM 0.25 mL 1.26 mL 2.52 mL

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References

References are publications that support the biological activity of the product.

Dow et al (2011) Discovery of PF-04620110, a potent, selective, and orally bioavailable inhibitor of DGAT-1. ACS Med.Chem.Lett. 2 407 PMID: 24900321


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