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Purity: ≥98%
PF-04620110 (PF04620110; PF 04620110) is a novel, potent, orally bioactive, and selective diglyceride acyltransferase-1 (DGAT1) inhibitor with the potential to treat type 2 diabetes mellitus. It inhibits DGAT1 with an IC50 of 19 nM. PF-04620110 has been advanced to clinical trials on the basis of the excellent pharmacologic and pharmacokinetic profiles. F-04620110 shows high selectivity versus a broad panel of off-target pharmacologic end points. In vivo DGAT-1 inhibition has been demonstrated through reduction of plasma triglyceride levels in rodents at doses of ≥0.1 mg/kg following a lipid challenge.
| ln Vitro |
Orally bioavailable, PF-04620110 exhibits passive permeability (1x10-6 cm/s)[1]. PF-04620110 inhibits triglyceride production in HT-29 cells with an IC50 of 8 nM and DGAT-1 with an IC50 of 19 nM[2]. With >100-fold selectivity against a panel of lipid processing enzymes (human DGAT-2, multiple human acyl-CoA: cholesterol acyltransferase-1, wax alcohol acyltransferase -1/-2 and monacylglycerol acyltransferase-2/-3, and mouse MGAT-1), PF-04620110 is a highly selective inhibitor of DGAT-1[2].
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| ln Vivo |
After a lipid challenge in rats, PF-04620110 (0.1–10 mg/kg; po) lowers plasma triglyceride levels at dosages of ≥0.1 mg/kg[2].
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| Animal Protocol |
Animal/Disease Models: Sprague−Dawley rats[2]
Doses: 0.1 mg/ kg, 1 mg/kg, 10 mg/kg Route of Administration: Oral administration Experimental Results: Produced a statistically significant reduction in plasma triglyceride excursion at 2 hrs (hours) to near prelipid load levels. |
| References |
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| Additional Infomation |
PF-04620110 is under investigation in clinical trial NCT01146327 (A Multiple Dose Study Of PF-04620110 In Healthy Overweight Or Obese Subjects).
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| Molecular Formula |
C21H24N4O4
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| Molecular Weight |
396.44
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| Exact Mass |
396.179
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| CAS # |
1109276-89-2
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| Related CAS # |
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| PubChem CID |
46926360
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
701.9±60.0 °C at 760 mmHg
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| Flash Point |
378.3±32.9 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.623
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| LogP |
2.08
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
587
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
GEVVQZHMFVFGLN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)
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| Chemical Name |
2-[4-[4-(4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6-yl)phenyl]cyclohexyl]acetic acid
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (3.15 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.15 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00959426 | Completed | Drug: PF-04620110 Drug: Placebo |
Obesity Overweight |
Pfizer | August 2009 | Phase 1 |
| NCT01146327 | Completed | Drug: PF-04620110 Drug: Placebo |
Healthy | Pfizer | June 2010 | Phase 1 |
| NCT00799006 | Completed | Drug: Placebo Drug: PF-04620110 |
Overweight | Pfizer | November 2008 | Phase 1 |
| NCT01298518 | Completed Has Results | Drug: PF-04620110 Drug: Placebo |
Type 2 Diabetes Patients | Pfizer | February 2011 | Phase 1 |
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