de en

Reagents and instruments for immunology, cell biology and molecular biology.

PF-04620110 [1109276-89-2]

Print

Cat# HY-13009-5mg

Size : 5mg

Contact local distributor :

Phone : +1 850 650 7790

Brand : MedChemExpress

Request more information

Contact local distributor :

Phone : +1 850 650 7790

Description

PF-04620110 is a potent, selective and orally bioavailable diglyceride acyltransferase-1 (DGAT-1) inhibitor with an IC₅₀ of 19 nM^[1].

IC₅₀ & Target

IC50: 19 nM (DGAT-1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Hep 3B2	IC₅₀	0.09 μM Compound: PF4620110	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 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 Compound: 1, PF-04620110	Inhibition of human DGAT-1-mediated triglyceride synthesis in the HT-29 cells by whole cell assay Inhibition of human DGAT-1-mediated triglyceride synthesis in the HT-29 cells by whole cell assay	[PMID: 21908190]
HT-29	IC₅₀	8 nM Compound: 1	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 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 Compound: 3, PF-04620110	Inhibition of DGAT1-mediated triglyceride synthesis in human HT-29 cells using [3H]glycerol as substrate after 6 hrs by beta counting 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 Compound: 3, PF-04620110	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 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 Compound: 1	Inhibition of human full length DGAT-1 expressed in insect sf9 cells using [14C]decanoylCoA as substrate after 1.5 hrs by scintillation spectrometry 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]

In Vitro

PF-04620110 is orally bioavailable, has passive permeability(1x10^-6 cm/s)^[1].
PF-04620110 inhibits DGAT-1 with an IC₅₀ of 19 nM, and inhibits triglyceride synthesis with an IC₅₀ of 8 nM in HT-29 cells^[2].
PF-04620110 is a highly selective inhibitor of DGAT-1 with >100-fold selectivity against a panel of lipid processing enzymes (human DGAT-2, several human acyl-CoA: cholesterol acyltransferase-1, wax alcohol acyltransferase-1/-2 and monacylglycerol acyltransferase-2/-3, and mouse MGAT-1)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (31.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5225 mL	12.6123 mL	25.2245 mL
5 mM	0.5045 mL	2.5225 mL	5.0449 mL
10 mM	0.2522 mL	1.2612 mL	2.5225 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1.25 mg/mL (3.15 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (3.15 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (3.15 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation

Purity: 99.60%

Data Sheet (278 KB) SDS (392 KB)

COA (254 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

References

[1]. Dow RL, et al. Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino[2,3-d]pyrimidine core. Bioorg Med Chem Lett. 2011 Oct 15;21(20):6122-5. [Content Brief]

[2]. Dow RL, et al. Discovery of PF-04620110, a Potent, Selective, and Orally Bioavailable Inhibitor of DGAT-1. ACS Med Chem Lett. 2011 Mar 18;2(5):407-12. [Content Brief]

You might also be interested by the following products:

Cat#

Description

Cond.

Price Bef. VAT

HY-10038-5mg

A 922500 [959122-11-3]

5mg

HY-13009-10mg

PF-04620110 [1109276-89-2]

10mg

HY-13009-50mg

PF-04620110 [1109276-89-2]

50mg

PF-04620110 [1109276-89-2]

Cat# HY-13009-5mg

Contact local distributor :

Brand : MedChemExpress

Contact local distributor :

PF-04620110 Related Antibodies

You might also be interested by the following products: