Home PI3K/Akt/mTOR AMPK activator MK-3903

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MK-3903 AMPK activator

Cat.No.S8803

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%.
MK-3903 AMPK activator Chemical Structure

Chemical Structure

Molecular Weight: 454.90

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Quality Control

Batch: S880301 4-Methylpyridine]23 mg/mL]true]DMSO]5.6 mg/mL]false]Water]Insoluble]false Purity: 99.28%
99.28

Chemical Information, Storage & Stability

Molecular Weight 454.90 Formula

C27H19ClN2O3

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1219737-12-8 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C=C(C=C1)OC2=NC3=C(N2)C=C(C(=C3)C4=CC=C(C=C4)C5=CC=CC=C5)Cl)C(=O)O

Solubility

In vitro
Batch:

4-Methylpyridine : 23 mg/mL

DMSO : 5.6 mg/mL (12.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
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%. This 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. It 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. This chemical 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 this compound robustly increased ACC phosphorylation in liver with more modest effects in skeletal muscle. Treatment of various mouse models with this chemical results in expected alterations in lipid metabolism and improvements in a measure of insulin sensitization[1].
References

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