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Submit ReviewPF 04620110
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)
Biological Activity for PF 04620110
PF 04620110 is a 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.
Compound Libraries for PF 04620110
PF 04620110 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for PF 04620110
| 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 for PF 04620110
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 7.93 | 20 |
Preparing Stock Solutions for PF 04620110
The following data is based on the product molecular weight 396.44. Batch specific molecular weights may vary from batch to batch due to the degree 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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Product Datasheets for PF 04620110
References for PF 04620110
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
If you know of a relevant reference for PF 04620110, please let us know.
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Keywords: PF 04620110, PF 04620110 supplier, PF04620110, potent, selective, orally, bioavailable, inhibitors, inhibits, DGAT-1, Diacylglycerol, acyltransferase, O-Acyltransferase, 5863, Tocris Bioscience
1 Citation for PF 04620110
Citations are publications that use Tocris products. Selected citations for PF 04620110 include:
Jian et al (2020) ABHD5 suppresses cancer cell anabolism through lipolysis-dependent activation of the AMPK/mTORC1 pathway. J Biol Chem 296 100104 PMID: 33219129
Do you know of a great paper that uses PF 04620110 from Tocris? Please let us know.
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