Fig. 1 · Structure

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PF-04620110

Cat. No. A11526 CAS 1109276-89-2

DGAT1 Inhibitor

PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

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Biological Activity

Target & Activity

Target Activity Value
DGAT1 19 nM

Cellular Effect

Cell Line Activity Value Description Reference
Hep 3B2 IC50 0.09 μM Inhibition of recombinant human DGAT-1 expressed in Hep3B cell lysate using didecanoyl glycerol and [14C]decanoyl-CoA as substrate after 60 mins by liquid scintillation counting analysis [PMID: 23810496]
HT-29 IC50 16 nM Inhibition of human DGAT-1-mediated triglyceride synthesis in the HT-29 cells by whole cell assay [PMID: 21908190]
HT-29 IC50 8 nM Inhibition of DGAT-1-mediated triglyceride synthesis in human HT-29 cells using [3H]-glycerol as substrate incubated for 1 hr prior to substrate addition measured after 5 hrs by scintillation counting analysis [PMID: 23871442]
HT-29 IC50 8 nM Inhibition of DGAT1-mediated triglyceride synthesis in human HT-29 cells using [3H]glycerol as substrate after 6 hrs by beta counting [PMID: 24900321]
Sf9 IC50 19 nM Inhibition of full length human microsomal DGAT-1 expressed in baculovirus infected insect Sf9 cells using [14C]decanoylCoA as substrate after 1.5 hrs by scintillation counting [PMID: 24900321]
Sf9 IC50 19 nM Inhibition of human full length DGAT-1 expressed in insect sf9 cells using [14C]decanoylCoA as substrate after 1.5 hrs by scintillation spectrometry [PMID: 23871442]

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 1109276-89-2
Applications DGAT1 Inhibitor
Formula C21H24N4O4
Molecular Weight 396.44
SMILES
Nc1ncnc2c1C(=O)N(c1ccc([C@H]3CC[C@H](CC(=O)O)CC3)cc1)CCO2

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO Warmed: 46 mg/mL (116.03 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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