PF-04620110

Catalog No.S7192

PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.

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PF-04620110 Chemical Structure

PF-04620110 Chemical Structure
Molecular Weight: 396.44

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Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description PF-04620110 is an orally active, selective and potent diglyceride acyltransferase-1 (DGAT1) inhibitor with IC50 of 19 nM.
Targets DGAT1 [1]
IC50 19 nM
In vitro
In vivo In Rats, PF-04620110 reduces plasma triglyceride levels t doses of ≥0.1 mg/kg following a lipid challenge. [1] DGAT1 inhibition by PF-04620110 causes an enrichment of polyunsaturated fatty acids within the TG class of lipids in rodents. [2]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

In Vitro Assay for DGAT-1 Enzyme Inhibition Human full-length diacylglycerol:acylCoA acyltransferase 1 (DGAT-1) is expressed in Sf9 insect cells which are then lysed and a crude membrane fraction is prepared. DGAT-1 activity was measured in 384-well format in a total assay volume of 25 μL that contained, Hepes buffer (50 mM, pH7.5), MgCl2 (10 mM), bovine serum albumin (0.6 mg/ml), [14C]decanoylCoA (20 μM, 58 Ci/mol) and membranes (25 μg/ml) into which 1,2 dioleoyl-sn-glycerol (75 μM) in acetone has already been incorporated. The inhibitors are present at a range of eight concentrations to generate an apparent IC50 for each compound. The reactions are allowed to proceed for 1.5 h at room temperature and then terminated by the addition of 10 μl of HCl (0.5 M). Reaction mixtures are neutralized by the addition of 15μl of tris(hydroxy-methyl)aminomethane (1M, pH 8.0) and then mixed by trituration with 37.5 μl of Microscint™-E. Plates contents are allowed to partition for 15 to 30 min before 14C was measured in a scintillation spectrometer.

Animal Study: [1]

Animal Models Male Sprague Dawley rats
Formulation water
Dosages ~10 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Dow RL, et al. ACS Med Chem Lett. 2011, 2(5), 407-412.

[2] Maciejewski BS, et al. Am J Physiol Gastrointest Liver Physiol. 2013, 304(11), G958-969.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01474941 Completed Healthy Pfizer June 2011 Phase 1
NCT01298518 Completed Type 2 Diabetes Patients Pfizer February 2011 Phase 1
NCT01166217 Completed Healthy Pfizer|Bristol-Myers Squibb July 2010 Phase 1
NCT01146327 Completed Healthy Pfizer|Bristol-Myers Squibb June 2010 Phase 1
NCT01064492 Completed Healthy Volunteers Pfizer February 2010 Phase 1

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Chemical Information

Download PF-04620110 SDF
Molecular Weight (MW) 396.44
Formula

C21H24N4O4

CAS No. 1109276-89-2
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 49 mg/mL warming (123.6 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Cyclohexaneacetic acid, 4-[4-(4-amino-7,8-dihydro-5-oxopyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl]-, trans-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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