MK8722

Additional information:
MK8722 is a potent and systemic pan-AMPK activator.|Product information|CAS Number: 1394371-71-1|Molecular Weight: 449.89|Formula: C24H20ClN3O4|Chemical Name: (3R,3aR,6R,6aR)-6-[(5-[1,1′-biphenyl]-4-yl-6-chloro-1H-imidazo[4,5-b]pyridin-2-yl)oxy]-hexahydrofuro[3,2-b]furan-3-ol|Smiles: O[C@@H]1CO[C@H]2[C@@H]1OC[C@H]2OC1NC2=CC(Cl)=C(N=C2N=1)C1C=CC(=CC=1)C1=CC=CC=C1|InChiKey: XQMNBTZLYOOAGA-UGESXGAOSA-N|InChi: InChI=1S/C24H20ClN3O4/c25-16-10-17-23(28-24(26-17)32-19-12-31-21-18(29)11-30-22(19)21)27-20(16)15-8-6-14(7-9-15)13-4-2-1-3-5-13/h1-10,18-19,21-22,29H,11-12H2,(H,26,27,28)/t18-,19-,21-,22-/m1/s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : 31.25 mg/mL (69.Dihydromyricetin supplier 46 mM; Need ultrasonic).Cefditoren Pivoxil custom synthesis |Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:32649469 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|MK8722 (MK-8722) is a potent, direct, allosteric activator of all 12 mammalian AMPK complexes. MK8722 activates pAMPK complexes with increased potency and magnitude versus AMP, with EC50 values of ~1 to 60 nM and increased activation by factors of ~4 to 24. Although MK8722 exhibits 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. pAMPK activation by maximal AMP plus MK8722 is synergistic, demonstrating that the agents act at distinct sites.|In Vivo:|Chronic antihyperglycemic efficacy of MK8722 (MK-8722) is evaluated in db/db mice, a leptin receptor-deficient T2DM model. Once-daily administration of MK8722 results in dose-dependent lowering of ambient blood glucose. On treatment day 12, glucose reductions after MK8722 treatment (30 mpk/day) are comparable to those observed with the PPARγ agonist BRL49653 (3 mpk/day). Unlike BRL49653, the glucose-lowering action of MK8722 manifests without significant effects on body weight, which is a consistent finding. Dose-dependent increases 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. Chronic MK8722 dosing in mice also increases muscle Glut4 protein levels, possibly contributing to efficacy.|Products are for research use only. Not for human use.|