| 产品描述： | MK-1064 is a selective and orally active OX2R antagonist (Ki: 0.5 nM, IC50: 18 nM). MK-1064 promotes sleep in vivo. MK-1064 can be used in the research of insomnia |
| 靶点： |
OX2 Receptor:18 nM (IC50);OX1 Receptor:1789 nM (IC50);OX2 Receptor:0.5 nM (Ki);OX1 Receptor;1584 nM (Ki);OXReceptor |
| 体内研究： |
MK-1064 (30 mg/kg, oral administration) promotes sleep in rodents selectively through OX2R in Wild-type mice. MK-1064 (30 mg/kg, oral administration, 5 days) reverses the struggle behavior induced by CNO pre-treatment in rats. MK-1064 (1-5 mg/kg, intravenous injection/oral administration) shows moderate oral bioavailability and clearance in rat, dog, and rhesus monkey. Animal Model: Wild-type and OX2R knockout mice Dosage: 30 mg/kg Administration: Oral administration Result: Displayed active wake reduction accompanied by significant increases in SWS (slow-wave sleep) and REM (rapid eye movement) at time points up to 3.5 hours following treatment. Animal Model: Rat, dog, and rhesus monkey (Pharmacokinetics assay) Dosage: 1, 2, 3, 5 mg/kg Administration: Oral administration (P.O.), intravenous injection (I.V.) Result: Pharmacokinetics profile of MK-1064. |
| 参考文献： |
1. Roecker AJ et al. Discovery of 5''-chloro-N-[(5,6-dimethoxypyridin-2-yl)methyl]-2,2':5',3''-terpyridine-3'-carboxamide (MK-1064): a selective orexin 2 receptor antagonist (2-SORA) for the treatment of insomnia. ChemMedChem. 2014 Feb;9(2):311-22. 2. Gotter AL et al. Orexin 2 Receptor Antagonism is Sufficient to Promote NREM and REM Sleep from Mouse to Man. Sci Rep. 2016 Jun 3;6:27147. 3. Laura A Grafe, et al. Orexin 2 receptor regulation of the hypothalamic-pituitary-adrenal (HPA) response to acute and repeated stress. Neuroscience. 2017 Apr 21;348:313-323. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.165 ml |
10.825 ml |
21.65 ml |
| 5 mM |
0.433 ml |
2.165 ml |
4.33 ml |
| 10 mM |
0.216 ml |
1.082 ml |
2.165 ml |
| 50 mM |
0.043 ml |
0.216 ml |
0.433 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京