MK-3903

Catalog No.S8803 Batch:S880301

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Technical Data

Formula

C27H19ClN2O3
Molecular Weight 454.90 CAS No. 1219737-12-8
Solubility (25°C)* In vitro 4-Methylpyridine 23 mg/mL warmed with 50ºC water bath (50.56 mM)
DMSO 5.6 mg/mL (12.31 mM)
Water Insoluble
* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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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 (from reference)

Animal Study:

[1]
  • Animal Models

    lean C57BL/6 mice, Sprague-Dawley rats and beagle dogs

  • 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.

Selleck's MK-3903 has been cited by 1 publication

MK8722, an AMPK activator, inhibiting carcinoma proliferation, invasion and migration in human pancreatic cancer cells [ Biomed Pharmacother, 2021, 144:112325] PubMed: 34656065

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.