PF-04620110
Based on 7 publication(s) in Google Scholar
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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- Pureté: 99.60%
- CAS No.: 1109276-89-2
- Formule: C21H24N4O4
- Masse moléculaire:396.44
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) PF-04620110
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Activité biologique
IC50: 19 nM (DGAT-1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hep 3B2 | IC50 |
0.09 μM
Compound: PF4620110
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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
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[PMID: 23810496] |
| HT-29 | IC50 |
16 nM
Compound: 1, PF-04620110
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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
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[PMID: 21908190] |
| HT-29 | IC50 |
8 nM
Compound: 1
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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
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[PMID: 23871442] |
| HT-29 | IC50 |
8 nM
Compound: 3, PF-04620110
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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
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[PMID: 24900321] |
| Sf9 | IC50 |
19 nM
Compound: 1
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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
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[PMID: 23871442] |
| Sf9 | IC50 |
19 nM
Compound: 3, PF-04620110
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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
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[PMID: 24900321] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague−Dawley rats[2]
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Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg
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Administration:Oral administration
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Result:Produced a statistically significant reduction in plasma triglyceride excursion at 2 hours to near prelipid load levels.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1109276-89-2
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Appearance Solid
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Masse moléculaire 396.44
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Formule C21H24N4O4
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Color White to off-white
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SMILES
O=C(C[C@@H]1CC[C@H](CC1)C2=CC=C(C=C2)N3CCOC4=NC=NC(N)=C4C3=O)O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Neurosci
The mitochondrial unfolded protein response in human microglia disrupts neuronal-glial communication and promotes senescence. [Abstract]2026 Jun 26. PMID: 42362883 -
Mol Metab
Long-chain acyl-CoA synthetase-4 regulates endometrial decidualization through a fatty acid β-oxidation pathway rather than lipid droplet accumulation. [Abstract]2024 Jun:84:101953. PMID: 38710444 -
Stem Cell Reports
An efficient, non-viral arrayed CRISPR screening platform for iPSC-derived myeloid and microglia models. [Abstract]2025 Mar 11;20(3):102420. PMID: 39983727 -
Physiol Rep
Diacylglycerol acyltransferase 1/2 inhibition induces dysregulation of fatty acid metabolism and leads to intestinal barrier failure and diarrhea in mice. [Abstract]2020 Aug;8(15):e14542. PMID: 32786057 -
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Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Portuguese - PT (392 KB)
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Instruction de manipulation (2659 KB)
Références
[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
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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