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MK8722

Catalog No. T16099 CAS 1394371-71-1

MK8722 is an effective and systemic activator of pan-AMPK.

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MK8722, CAS 1394371-71-1

Pack Size	Availability	Price/USD
1 mg	In stock	$ 31.00
2 mg	In stock	$ 44.00
5 mg	In stock	$ 72.00
10 mg	In stock	$ 122.00
25 mg	In stock	$ 238.00
50 mg	In stock	$ 441.00
100 mg	In stock	$ 649.00
1 mL * 10 mM (in DMSO)	In stock	$ 79.00

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Purity: 99.72%

Biological Description

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Description	MK8722 is an effective and systemic activator of pan-AMPK.
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 .
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 .

Molecular Weight	449.89
Formula	C24H20ClN3O4
CAS No.	1394371-71-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 62.5 mg/mL (138.92 mM)

References and Literature

1. Myers RW, et al. Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but induces cardiachypertrophy. Science. 2017 Aug 4;357(6350):507-511.

Related compound libraries

This product is contained In the following compound libraries：

Kinase Inhibitor Library Anti-Metabolism Disease Compound Library PI3K-AKT-mTOR Compound Library Anti-Lung Cancer Compound Library Anti-Colorectal Cancer Compound Library Anti-Cancer Compound Library Glycolysis Compound Library Metabolism Compound Library Glycometabolism Compound Library Reprogramming Compound Library

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Related compounds with same targets

HTH-01-015 AMPK-α1β1γ1 activator 1 HL271 Adenosine monophosphate A-769662 XMD-17-51 Epiberberine PF-06409577

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Keywords

MK8722 1394371-71-1 Chromatin/Epigenetic PI3K/Akt/mTOR signaling AMPK AMP-activated protein kinase inhibit Inhibitor MK-8722 MK 8722 inhibitor

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