PF-04620110 (Synonyms: PF 04620110,PF04620110) |
| Katalog-Nr.GC15274 |
PF-04620110 is an orally active, selective diacylglycerol acyltransferase-1 (DGAT1) inhibitor (IC50 = 19nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1109276-89-2
Sample solution is provided at 25 µL, 10mM.
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PF-04620110 is an orally active, selective diacylglycerol acyltransferase-1 (DGAT1) inhibitor (IC50 = 19nM) [1]. PF-04620110 blocks triglyceride synthesis by inhibiting DGAT-1, thereby lowering plasma triglyceride levels in vivo [2]. PF-04620110 is commonly used to treat diabetes [3-4].
In MDA-MB-231 cells, PF-04620110 (5µM; 24h) blocks the conversion of diacylglycerol to triacylglycerol to inhibit lipid droplet formation [5]. In MCF10CA1a cells, PF-04620110 (50µM; 24h) reduces triacylglycerol storage and restricts cell migration [6].
In high-fat diet mice model, PF-04620110 (3mg/kg; po; 4 weeks) suppressed fatty acid induced NLRP3 inflammasome activation [7]. In high-fat diet cynomolgus monkeys model, PF-04620110 (0.1-1mg/kg; po; 4d) treatment induced diarrhea [8].
References:
[1]. Dow R L, Li J C, Pence M P, et al. Discovery of PF-04620110, a potent, selective, and orally bioavailable inhibitor of DGAT-1[J]. ACS medicinal chemistry letters, 2011, 2(5): 407-412.
[2]. Dow R L, Andrews M, Aspnes G E, et al. Design and synthesis of potent, orally-active DGAT-1 inhibitors containing a dioxino [2, 3-d] pyrimidine core[J]. Bioorganic & medicinal chemistry letters, 2011, 21(20): 6122-6125.
[3]. Dow R L, Andrews M P, Li J C, et al. Defining the key pharmacophore elements of PF-04620110: discovery of a potent, orally-active, neutral DGAT-1 inhibitor[J]. Bioorganic & Medicinal Chemistry, 2013, 21(17): 5081-5097.
[4]. Enayetallah A E, Ziemek D, Leininger M T, et al. Modeling the mechanism of action of a DGAT1 inhibitor using a causal reasoning platform[J]. PloS one, 2011, 6(11): e27009.
[5]. Almanza A, Mnich K, Blomme A, et al. Regulated IRE1α-dependent decay (RIDD)-mediated reprograming of lipid metabolism in cancer[J]. Nature communications, 2022, 13(1): 2493.
[6]. Andolino C, Cotul E K, Xianyu Z, et al. Fatty acid synthase-derived lipid stores support breast cancer metastasis[J]. Cancer & metabolism, 2025, 13(1): 35.
[7]. Jo S I, Bae J H, Kim S J, et al. PF-04620110, a potent antidiabetic agent, suppresses fatty acid-induced NLRP3 inflammasome activation in macrophages[J]. Diabetes & Metabolism Journal, 2019, 43(5): 683.
[8]. Cheng D, Zinker B A, Luo Y, et al. MGAT2 inhibitor decreases liver fibrosis and inflammation in murine NASH models and reduces body weight in human adults with obesity[J]. Cell Metabolism, 2022, 34(11): 1732-1748. e5.
| Cell experiment [1]: | |
Cell lines | MDA-MB-231 cells |
Preparation Method | MDA-MB-231 cells were cultured in DMEM high-glucose medium supplemented with 10% fetal bovine serum (FBS) and 2mM L-glutamine in a humidified incubator at 37℃ and 5% CO2. Cells were seeded at appropriate density and treated with 20µM MKC8866, 5µM PF-04620110, or an equal volume of DMSO 24 hours later. |
Reaction Conditions | 5µM; 24h |
Applications | PF-04620110 blocks the conversion of diacylglycerol to triacylglycerol to inhibit lipid droplet formation. |
| Animal experiment [2]: | |
Animal models | High-fat diet (HFD) mice model |
Preparation Method | C57BL/6J mice (male, 6 weeks old) with similar plasma glucose levels and body weights were used. For generation of HFD‐induced diabetic mice, C57BL/6J mice were fed HFD with 0.15% cholesterol (HFD, 21% crude fat, 0.15% cholesterol, and 19.5% casein) or regular diet (RD), for 12 weeks. For treatment of PF-04620110, PF-04620110 or vehicle control (dimethyl sulfoxide [DMSO]) were fed once a day at the dose of 3mg/kg for another 4 weeks. |
Dosage form | 3mg/kg; po; 4 weeks |
Applications | PF-04620110 suppressed fatty acid induced NLRP3 inflammasome activation. |
References: | |
| Cas No. | 1109276-89-2 | SDF | |
| Überlieferungen | PF 04620110,PF04620110 | ||
| Chemical Name | 2-[4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6-yl)phenyl]cyclohexyl]acetic acid | ||
| Canonical SMILES | C1CC(CCC1CC(=O)O)C2=CC=C(C=C2)N3CCOC4=NC=NC(=C4C3=O)N | ||
| Formula | C21H24N4O4 | M.Wt | 396.44 |
| Löslichkeit | ≥ 16.9mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5224 mL | 12.6122 mL | 25.2245 mL |
| 5 mM | 504.5 μL | 2.5224 mL | 5.0449 mL |
| 10 mM | 252.2 μL | 1.2612 mL | 2.5224 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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