2. Metabolic Enzyme/Protease
  3. Acyltransferase
  4. PF-04620110

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

For research use only. We do not sell to patients.

PF-04620110 Chemical Structure

PF-04620110 Chemical Structure

CAS No. : 1109276-89-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Solution
10 mM * 1 mL in DMSO USD 79 In-stock
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10 mg USD 131 In-stock
50 mg USD 432 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

PF-04620110 Related Antibodies

Top Publications Citing Use of Products

View All Acyltransferase Isoform Specific Products:

View All Isoforms
ACAT1 ACAT2 MGAT2 ACAT

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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]
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.

PF-04620110 Related Antibodies
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.
Clinical Trial
Molecular Weight

396.44

Formula

C21H24N4O4
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
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
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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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.
Purity & Documentation

Purity: 98.86%

COA (254 KB) LCMS (275 KB)

Handling Instructions (2659 KB)
References

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.

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
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PF-04620110 Related Classifications

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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