MK8722
(Synonyms: (3S,3AS,6S,6AS)-6-((5-([1,1'-联苯]-4-基)-6-氯-1H-咪唑并[4,5-B]吡啶-2-基)氧基)六氢呋喃[3,2-B]呋喃-3-醇) 目录号 : GC31470
MK-8722 is a potent, direct, allosteric activator of all 12 mammalian pan-AMPK complexes.
Cas No.:1394371-71-1
Sample solution is provided at 25 µL, 10mM.
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MK-8722 is a potent, direct, allosteric activator of all 12 mammalian pan-AMPK complexes.
MK-8722 activates pAMPK complexes with increased potency and magnitude versus AMP. In primary mouse hepatocytes, HepG2 cells, or primary human myocytes, MK-8722 results in the phosphorylation of a number of additional known targets of pAMPK, and the most potent off-target activity observed for MK8722 is against the serotonin 5-HT2A receptor.[1]
Pharmacological pan-AMPK activation by MK-8722 leads to chronically sustainable improvements in glucose homeostasis, including the amelioration of insulin resistance and hyperglycemia. Acute treatment with MK-8722 (30 mpk) significantly suppress blood glucose and insulin levels. In mice, chronic MK-8722 dose also increases muscle Glut4 protein levels. In rhesus monkeys, MK8722 results in cardiac hypertrophy associated with increased cardiac and skeletal muscle glycogen.[1]
[1] Robert W Myers, et al. Science . 2017 Aug 4;357(6350):507-511.
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Animal experiment: |
Mice[1]Housing Lean C57BL/6 mice at 10-12 weeks of age and C57BL/6 eDIO mice at 16 weeks of age are used. db/db mice at 7 weeks of age are used. Animals are maintained on a 12 hr/12 hr light-dark cycle with free access to food and water with the temperature maintained at 22ºC. Four lean C57BL/6 mice are housed in a standard cage. eDIO mice are individually caged. Eight db/db mice are housed in a large rodent cage. C57BL/6 mice and db/db mice are maintained on regular rodent chow diet 7012 (5% dietary fat; 3.75 kcal/g) for 1-2 weeks before receiving compound treatments. eDIO mice are maintained on 60% kcal% fat diet. Oral dosing of MK8722 in standard vehicle, or vehicle alone, is performed using 10 mL/kg body weight. The effect of MK8722 on various metabolic parameters is established by comparison to vehicle treated animals[1]. |
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References: [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. |
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| Cas No. | 1394371-71-1 | SDF | |
| 别名 | (3S,3AS,6S,6AS)-6-((5-([1,1'-联苯]-4-基)-6-氯-1H-咪唑并[4,5-B]吡啶-2-基)氧基)六氢呋喃[3,2-B]呋喃-3-醇 | ||
| Canonical SMILES | O[C@H]1[C@@]([C@]2([H])OC1)([H])OC[C@H]2OC3=NC4=NC(C(C=C5)=CC=C5C6=CC=CC=C6)=C(Cl)C=C4N3 | ||
| 分子式 | C24H20ClN3O4 | 分子量 | 449.89 |
| 溶解度 | DMSO : ≥ 62.5 mg/mL (138.92 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet