MK-8722
MK-8722 is a potent pan-AMPK activator. MK-8722 improves glucose homeostasis but induces cardiac hypertrophy. In rodents and rhesus monkeys, MK-8722-mediated AMPK activation in skeletal muscle induced robust, durable, insulin-independent glucose uptake and glycogen synthesis, with resultant improvements in glycemia and no evidence of hypoglycemia. These effects translated across species, including diabetic rhesus monkeys, but manifested with concomitant cardiac hypertrophy and increased cardiac glycogen without apparent functional sequelae.
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化学信息
| 名称 | MK-8722 |
|---|---|
| Iupac 化学名称 | (3R,3aR,6R,6aR)-6-((6-([1,1'-biphenyl]-4-yl)-7-chloro-3H-imidazo[4,5-b]pyridin-2-yl)oxy)hexahydrofuro[3,2-b]furan-3-ol |
| 同义词 | MK-8722; MK 8722; MK8722. |
| 英文同义词 | MK-8722; MK 8722; MK8722. |
| 分子式 | C24H20ClN3O4 |
| 分子量 | 449.89 |
| Smile | ClC1=C2C(NC(O[C@@H]3CO[C@@]4([H])[C@]3([H])OC[C@H]4O)=N2)=NC=C1C5=CC=C(C6=CC=CC=C6)C=C5 |
| InChiKey | VEGCGBKTFKSLJB-MCEIDBOGSA-N |
| InChi | 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 |
| Cas号 | 1394371-71-1 |
| 相关CAS号 |
订购信息
| 包装 | 价格 | 库存 | 纯度 | 备货期 |
|---|---|---|---|---|
| 大货 | 询价 | 询价 | 询价 |
| 外观性状 | 固体粉末 |
|---|---|
| 纯度 | 98% Min. |
| 存储 | 短期（几天到几周）为0-4摄氏度，长期（几个月）为-20摄氏度 |
| 可溶性 | 溶于DMSO |
| 处理方式 | |
| 运输条件 | 作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周. |
| 海关编码 |
| Targets | |
|---|---|
| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Weihrauch M, Handschin C. Pharmacological targeting of exercise adaptations in
skeletal muscle: Benefits and pitfalls. Biochem Pharmacol. 2017 Oct 20. pii:
S0006-2952(17)30636-6. doi: 10.1016/j.bcp.2017.10.006. [Epub ahead of print]
Review. PubMed PMID: 29061342.
2: Myers RW, Guan HP, Ehrhart J, Petrov A, Prahalada S, Tozzo E, Yang X, Kurtz
MM, Trujillo M, Gonzalez Trotter D, Feng D, Xu S, Eiermann G, Holahan MA, Rubins
D, Conarello S, Niu X, Souza SC, Miller C, Liu J, Lu K, Feng W, Li Y, Painter RE,
Milligan JA, He H, Liu F, Ogawa A, Wisniewski D, Rohm RJ, Wang L, Bunzel M, Qian
Y, Zhu W, Wang H, Bennet B, LaFranco Scheuch L, Fernandez GE, Li C, Klimas M,
Zhou G, van Heek M, Biftu T, Weber A, Kelley DE, Thornberry N, Erion MD, Kemp DM,
Sebhat IK. Systemic pan-AMPK activator MK-8722 improves glucose homeostasis but
induces cardiac hypertrophy. Science. 2017 Aug 4;357(6350):507-511. doi:
10.1126/science.aah5582. Epub 2017 Jul 13. PubMed PMID: 28705990.
3. Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase
Danqing Feng, Tesfaye Biftu, F. Anthony Romero, Ahmet Kekec, James Dropinski, Andrew Kassick, Shiyao Xu, Marc M. Kurtz, Anantha Gollapudi, Qing Shao, Xiaodong Yang, Ku Lu, Gaochao Zhou, Daniel Kemp, Robert W. Myers, Hong-Ping Guan, Maria E. Trujillo, Cai Li, Ann Weber, and Iyassu K. Sebhat
Publication Date (Web): December 1, 2017 (Letter)
DOI: 10.1021/acsmedchemlett.7b00417
