MK8722

SKU: orb1308031

Description

MK8722 is a potent small molecule activator of all AMP-activated protein kinase (AMPK) isoforms. It is used in research to study AMPK's systemic effects in metabolic disorders, with applications in both cellular assays and animal models of diabetes and obesity.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1394371-71-1
• MW: 449.89
• Purity: 98.08% (May vary between batches)
• Formula: C₂₄H₂₀ClN₃O₄
• SMILES: [H][C@]12OC[C@@H](Oc3nc4nc(c(Cl)cc4[nH]3)-c3ccc(cc3)-c3ccccc3)[C@@]1([H])OC[C@H]2O
• Target: AMPK
• Solubility: DMSO:50 mg/mL (111.14 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.45 mM)

Bioactivity

• In Vivo:
  MK8722(once-daily)administration, causes dose-dependent lowering of ambient blood glucose. Chronic MK8722 dosing in mice also increases muscle Glut4 protein levels, possibly contributing to efficacy. Chronic antihyperglycemic efficacy of MK8722 is evaluated in db/db mice (a leptin receptor-deficient T2DM model). Glucose reductions after MK8722 treatment (30 mpk/day) are comparable to those observed with the PPARγ agonist BRL49653 (3 mpk/day), on treatment day 12. Dose-dependent enhances in tissue pACC are maintained throughout the dosing period. Chronic efficacy, without tachyphylaxis, is also observed in additional dysmetabolic and diabetic rodent models. In all cases, efficacy is associated with trough MK8722 plasma levels comparable to the concentrations required to acutely stimulate skeletal muscle glucose uptake. The glucose-lowering action of MK8722 manifests without significant effects on body weight .
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• In Vitro:
  MK8722 is an effective, direct, allosteric activator of all 12 mammalian AMPK complexes. pAMPK activation by maximal AMP plus MK8722 is synergistic, demonstrating that the agents act at distinct sites. MK8722 activates pAMPK complexes with increased potency and magnitude versus AMP (EC50: ~1 to 60 nM) and increased activation by factors of ~4 to 24. Although MK8722 exhibits a higher affinity for β1-containing (~1 to 6 nM) versus β2-containing (~15 to 63 nM) pAMPK complexes, it is the most potent activator of β2 complexes reported to date .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, MK8722, MK-8722, MK 8722, inhibit, AMP-activated protein kinase, AMPK

Compound Identifiers

PubChem CID

89558344