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1mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
MK-8722 (MK8722) is a novel, potent allosteric pan-AMPK activator with anti-diabetic effects. AMPK is a master regulator of energy homeostasis in eukaryotes. Despite three decades of research, there is still a lack of understanding of the biological functions of AMPK and its potential as a drug target, largely due to the lack of pharmacological tools that are optimized for this purpose. Although MK-8722 causes cardiac hypertrophy, it improves glucose homeostasis. Rodents and rhesus monkeys' skeletal muscles experienced robust, long-lasting, insulin-independent glucose uptake and glycogen synthesis, which improved glycemia and left no sign of hypoglycemia. These effects were observed in diabetic rhesus monkeys as well as other species, but they were accompanied by concurrent cardiac hypertrophy and elevated cardiac glycogen without obvious functional consequences.
Targets |
AMPK; pan-AMPK
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ln Vitro |
MK-8722 activates pAMPK complexes more powerfully and significantly than AMP. MK-8722 causes the phosphorylation of a number of additional known pAMPK targets in primary mouse hepatocytes, HepG2 cells, or primary human myocytes. The most potent off-target activity seen for MK-8722 is against the serotonin 5-HT2A receptor. [1]
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ln Vivo |
In addition to reducing insulin resistance and hyperglycemia, pharmacological pan-AMPK activation by MK-8722 results in improvements in glucose homeostasis that are chronically sustainable. MK-8722 (30 mpk) acute treatment significantly reduces blood sugar and insulin levels. Chronic MK-8722 administration to mice also raises the level of Glut4 protein in the muscles. With increased cardiac and skeletal muscle glycogen, MK8722 causes cardiac hypertrophy in rhesus monkeys. [1]
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Animal Protocol |
Mice: Lean Housing Both C57BL/6 eDIO mice and C57BL/6 mice between the ages of 10 and 12 weeks are employed. 7-week-old db/db mice are employed. With free access to food and water and a constant temperature of 22°C, animals are kept on a 12/12-hour light-dark cycle. In a typical cage, four thin C57BL/6 mice are kept. eDIO mice are housed in individual cages. In a sizable rodent cage, eight db/db mice are kept. Before receiving compound treatments, C57BL/6 mice and db/db mice are kept on the regular rodent chow diet 7012 (5% dietary fat; 3.75 kcal/g). A diet high in fat (60 kcal%) is used to maintain eDIO mice. Use 10 mL/kg body weight when administering MK8722 orally in a standard vehicle or by the vehicle alone. By contrasting MK8722's effects with those of animals that had been given vehicles as treatments, various metabolic parameters are determined[1].
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References |
Molecular Formula |
C24H20CLN3O4
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Molecular Weight |
449.886304855347
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Exact Mass |
449.1142
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Elemental Analysis |
C, 64.07; H, 4.48; Cl, 7.88; N, 9.34; O, 14.22
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CAS # |
1394371-71-1
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Related CAS # |
1394371-71-1
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Appearance |
Solid powder
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SMILES |
C1[C@H]([C@@H]2[C@H](O1)[C@@H](CO2)OC3=NC4=NC(=C(C=C4N3)Cl)C5=CC=C(C=C5)C6=CC=CC=C6)O
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InChi Key |
XQMNBTZLYOOAGA-UGESXGAOSA-N
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InChi Code |
InChI=1S/C24H20ClN3O4/c25-19-16(15-8-6-14(7-9-15)13-4-2-1-3-5-13)10-26-23-20(19)27-24(28-23)32-18-12-31-21-17(29)11-30-22(18)21/h1-10,17-18,21-22,29H,11-12H2,(H,26,27,28)/t17-,18-,21-,22-/m1/s1
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Chemical Name |
(3R,3aR,6R,6aR)-6-[[6-chloro-5-(4-phenylphenyl)-1H-imidazo[4,5-b]pyridin-2-yl]oxy]-2,3,3a,5,6,6a-hexahydrofuro[3,2-b]furan-3-ol
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Synonyms |
MK8722; MK 8722; MK-8722
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: ~90 mg/mL (~115.1 mM)
Ethanol: ~2 mg/mL (~4.5 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.62 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2228 mL | 11.1138 mL | 22.2277 mL | |
5 mM | 0.4446 mL | 2.2228 mL | 4.4455 mL | |
10 mM | 0.2223 mL | 1.1114 mL | 2.2228 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.