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

PF-04620110 

Cat. No.: HY-13009 Purity: 99.30%
Handling Instructions

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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 79 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 131 In-stock
Estimated Time of Arrival: December 31
50 mg USD 432 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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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].

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].

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (31.53 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5224 mL 12.6122 mL 25.2245 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 mL
10 mM 0.2522 mL 1.2612 mL 2.5224 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (3.15 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
PF-04620110
Cat. No.:
HY-13009
Quantity:
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