1. Metabolic Enzyme/Protease
  2. Acetyl-CoA Carboxylase
  3. MK-4074

MK-4074 

Cat. No.: HY-107709 Purity: 99.71%
Handling Instructions

MK-4074 is a liver-specific inhibitor of acetyl-CoA carboxylase ACC1 and ACC2 with IC50 values of approximately 3 nM.

For research use only. We do not sell to patients.

MK-4074 Chemical Structure

MK-4074 Chemical Structure

CAS No. : 1039758-22-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 311 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 311 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 400 In-stock
Estimated Time of Arrival: December 31
25 mg USD 800 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

MK-4074 is a liver-specific inhibitor of acetyl-CoA carboxylase ACC1 and ACC2 with IC50 values of approximately 3 nM.

IC50 & Target

IC50: 3 nM (Acetyl-CoA Carboxylase)[1]

In Vitro

MK-4074 strongly inhibits both ACC1 and ACC2 with IC50 values of approximately 3 nM. MK-4074 is highly liver specific because it is a substrate of organic anion transport protein (OATP) transporters that are present only in hepatocytes, and excretion of MK-4074 from hepatocytes into bile is dependent on the MRP2 efflux transporter[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

In male KKAy mice, a mouse model of obesity, type 2 diabetes, and fatty liver, a single oral dose of MK-4074 (0.3-3 mg/kg) significantly decreases DNL in a dose-dependent manner with an ID50 value of 0.9 mg/kg 1 hr post-administration. In a time course study, MK-4074 orally at 30 mg/kg reduces hepatic DNL by 83%, 70%, and 51% at 4, 8, and 12 hr post-dose, respectively. Single oral doses of MK-4074 at 30 and 100 mg/kg significantly increases plasma total ketones, a surrogate biomarker for hepatic FAO, by 1.5-fold to 3-fold for up to 8 hr[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

565.62

Formula

C₃₃H₃₁N₃O₆

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 : 50 mg/mL (88.40 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7680 mL 8.8399 mL 17.6797 mL
5 mM 0.3536 mL 1.7680 mL 3.5359 mL
10 mM 0.1768 mL 0.8840 mL 1.7680 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: ≥ 2.5 mg/mL (4.42 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Recombinant ACC protein is purified from FM3A or Sf9 cells expressing recombinant ACC by chelating chromatography or from liver by Softlink avidin resin chromatography. Purified ACC protein is incubated with MK-4074 in assay buffer containing 5 mM ATP, 250 mM acetyl-CoA, 4.1 mM NaHCO3, 0.086 mM NaH14CO3, 20 mM potassium citrate, 20 mM MgCl2, 2 mM DTT, 0.5 mg/mL BSA and 50 mM HEPES-Na (pH 7.5) for 40 min at 37°C[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

For cellular assays of DNL and FAO, cells are pre-incubated with MK-4074 for 1 hr. Then the cells are incubated for additional 1-3 hr with either 65-260 mM 14C-labeled acetate or 0.018 mM 3H-labeled palmitate for DNL or FAO assay, respectively. After incubation, intracellular 14C-labeled lipids and released 3H-labeled fatty acids are extracted and measured for DNL and FAO, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice[1]

Studies are performed in male KKAy mice or C57BL/6J mice. KKAy mice are fed a chow diet while C57BL/6J mice are fed a high-fat diet (45% fat) for 3 weeks prior to study. Mice are treated for 7 days with vehicle (distilled water, 0.2 mL/mouse) before MK-4074 administration to acclimate mice to oral dosing. Animals are drug naive at the time of study. Mice are housed individually. Male KKAy mice (n=10-11/group) are administered a single oral dose of MK-4074 (0.3 to 3 mg/kg) prior to liver slice studies. Male KKAy mice (n=5/group) are administered a single oral dose of MK-4074 (3 to 30 mg/kg) prior to measurement of liver DNL rates. Male KKAy mice (n=8/group) are administered a single oral dose of MK-4074 (10 to 100 mg/kg) and plasma ketone bodies are measured at the indicated times. Male C57BL/6J mice (n=5, veh; n=10, MK-4074) are fed chow or a high-fat/high-sucrose (HF/HS) diet for 7 weeks and vehicle or MK-4074 is administered orally (10 or 30 mg/kg/day) for 4 weeks prior to study[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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Product Name:
MK-4074
Cat. No.:
HY-107709
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