Home PI3K/Akt/mTOR AMPK activator MK-3903 For research use only.

MK-3903

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 Chemical Structure

MK-3903 Chemical Structure

CAS: 1219737-12-8

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

Purity & Quality Control

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

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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
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
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].
Animal Research 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.

Chemical Information & Solubility

Molecular Weight 454.90 Formula

C27H19ClN2O3
CAS No. 1219737-12-8 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

4-Methylpyridine : 23 mg/mL

DMSO : 5.6 mg/mL ( (12.31 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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

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