PF-04620110

Name: PF-04620110
Brand: MedChemExpress
SKU: HY-13009
Rating: 5.0 (6 reviews)

Cat. No.: HY-13009 Pureza: 99.60%: Ficha de datos
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PF-04620110 is a potent, selective and orally bioavailable diglyceride acyltransferase-1 (DGAT-1) inhibitor with an IC₅₀ of 19 nM.

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PF-04620110 Estructura química

No. CAS : 1109276-89-2

Tamaño	Stock	Cantidad

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
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10 mg	En stock	Estimated Time of Arrival: December 31
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Revisión del cliente

Based on 6 publication(s) in Google Scholar

6 Publications Citing Use of MCE PF-04620110

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Acyltransferase:

Ver todas las isoformas

ACAT1 ACAT2 MGAT2 ACAT DGAT1 DGAT2

Actividad biológica
Pureza y Documentación
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Revisión del cliente

Descripciòn

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 3 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	8 1 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]
HT-29	IC₅₀	8 1 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	16 1 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 1 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	16 1 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	16 1 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]
Hep 3B2	IC₅₀	0.09 3 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	8 1 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]
HT-29	IC₅₀	8 1 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]
Sf9	IC₅₀	19 1 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 1 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]
HT-29	IC₅₀	8 1 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 1 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]
Sf9	IC₅₀	19 1 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]
Hep 3B2	IC₅₀	0.09 3 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]
Sf9	IC₅₀	19 1 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]
Sf9	IC₅₀	19 1 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]

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.

In Vivo

PF-04620110 (0.1-10 mg/kg; p.o.) reduces plasma triglyceride levels at doses of ≥0.1 mg/kg following a lipid challenge in rat^[2].

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

Animal Model:	Sprague−Dawley rats^[2]
Dosage:	0.1 mg/kg, 1 mg/kg, 10 mg/kg
Administration:	Oral administration
Result:	Produced a statistically significant reduction in plasma triglyceride excursion at 2 hours to near prelipid load levels.

Ensayo clínico

Peso molecular

396.44

Fòrmula

C₂₁H₂₄N₄O₄

No. CAS

1109276-89-2

Appearance

Solid

Color

White to off-white

SMILES

O=C(C[C@@H]1CC[C@H](CC1)C2=CC=C(C=C2)N3CCOC4=NC=NC(N)=C4C3=O)O

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvente y solubilidad

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.

Calculadora de molaridad
Calculadora de dilución

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Pureza y Documentación

Purity: 99.60%

Select Batch:

Ficha de datos (278 KB) SDS (392 KB)

COA (254 KB) LCMS (95 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5225 mL	12.6123 mL	25.2245 mL	63.0613 mL
	5 mM	0.5045 mL	2.5225 mL	5.0449 mL	12.6123 mL
	10 mM	0.2522 mL	1.2612 mL	2.5225 mL	6.3061 mL
	15 mM	0.1682 mL	0.8408 mL	1.6816 mL	4.2041 mL
	20 mM	0.1261 mL	0.6306 mL	1.2612 mL	3.1531 mL
	25 mM	0.1009 mL	0.5045 mL	1.0090 mL	2.5225 mL
	30 mM	0.0841 mL	0.4204 mL	0.8408 mL	2.1020 mL

PF-04620110 Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-046201101109276-89-2PF04620110PF 04620110AcyltransferaseDiacylglycerol acyltransferaseDiglyceride acyltransferaseacyl-CoA:cholesterol acyltransferasemono- acylglycerol acyltransferaseInhibitorinhibitorinhibit

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PF-04620110

Revisión del cliente

PF-04620110 Related Antibodies

6 Publications Citing Use of MCE PF-04620110

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Acyltransferase:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

PF-04620110 Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

PF-04620110 Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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