MK-3903

Catalog No.S8803

MK-3903 Chemical Structure

Molecular Weight(MW): 454.90

MK-3903 is a potent and selective AMPK activator with an EC50 of 8 nM for α1 β1 γ1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%.

Size Price Stock Quantity  
USD 147 In stock
USD 447 In stock
Bulk Discount

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

Purity & Quality Control

Choose Selective AMPK Inhibitors

Biological Activity

Description MK-3903 is a potent and selective AMPK activator with an EC50 of 8 nM for α1 β1 γ1 subunit. It activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%.
Targets
AMPK [1]
()
8 nM(EC50)
In vitro

MK-3903 activates 10 of the 12 pAMPK complexes with EC50 values in the range of 8-40 nM and maximal activation >50%. The compound partially activates pAMPK5 (36% max), which is only a minor component of human and mouse liver, and it does not activate pAMPK6, which is not detected in liver. MK-3903 is a weak reversible inhibitor of CYP3A4 and 2D6 in human liver microsomes (apparent IC50 > 50 μM) and does not exhibit time-dependent inhibition of CYP3A4 activity. MK-3903 is not a potent PXR agonist[1].

In vivo

The pharmacokinetics of MK-3903 in C57BL/6 mice, Sprague–Dawley rats, and beagle dogs were characterized by moderate systemic plasma clearance (5.0–13 mL/min/kg), a volume of distribution at steady state of 0.6–1.1 L/kg, and a terminal half-life of ∼2 h. It has low oral bioavailability (8.4%) in C57BL/6 mice, but the oral exposure is later improved using other vehicles. Oral bioavailabilities in rats and dogs are improved (27-78%). Chronic oral administration of compound MK-3903 robustly increased ACC phosphorylation in liver with more modest effects in skeletal muscle. Treatment of various mouse models with MK-3903 results in expected alterations in lipid metabolism and improvements in a measure of insulin sensitization[1].

Protocol

Animal Research:

[1]

- Collapse
  • Animal Models: lean C57BL/6 mice, Sprague-Dawley rats and beagle dogs
  • Formulation: for mice, sulfobutyl ether-β-cyclodextrin/50 mM NaHCO3 (IV) and PEG400:water (P.O.); for rats, PEG200:water (1:1) + 2M equiv. NaHCO3(IV) and Tween 80:0.25% Methylcellulose/0.02% SDS (5:95) + 2M equiv NaHCO3 (P.O.); for dogs, PEG200:water(1:1) + 2M equiv. NaHCO3 (IV) and Tween 80:0.25% Methylcellulose/0.02% SDS (5:95) + 2M equiv NaHCO3 (P.O.)
  • Dosages: for I.V., 2 mg/kg in mouse, 1 mg/kg in rat and 0.5 mg/kg in dog; for P.O., 10 mg/kg in mouse, 4 mg/kg in rat and 1 mg/kg in dog
  • Administration: P.O. and I.V.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 91 mg/mL (200.04 mM)
Water Insoluble
Ethanol 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 Information

Molecular Weight 454.90
Formula

C27H19ClN2O3

CAS No. 1219737-12-8
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

AMPK Signaling Pathway Map

Related AMPK Products

Tags: buy MK-3903 | MK-3903 supplier | purchase MK-3903 | MK-3903 cost | MK-3903 manufacturer | order MK-3903 | MK-3903 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID