MK-1064 是一种选择性的、具有口服活性的OX2R拮抗剂 (Ki: 0.5 nM,IC50: 18 nM)。MK-1064 可促进睡眠 (in vivo)。MK-1064 可用于神经相关的研究。
| 生物活性 | MK-1064 is a selective and orally activeOX2Rantagonist (Ki: 0.5 nM,IC50: 18 nM). MK-1064 promotes sleepin vivo. MK-1064 can be used in the research of insomnia[1][3]. |
| IC50& Target[1] | OX2Receptor 18 nM (IC50) | OX1Receptor 1789 nM (IC50) | OX2Receptor 0.5 nM (Ki) | OX1Receptor 1584 nM (Ki) |
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体内研究
(In Vivo) | MK-1064 (30 mg/kg, oral administration) promotes sleep in rodents selectively through OX2R in Wild-type mice[2].
MK-1064 (30 mg/kg, oral administration, 5 days) reverses the struggle behavior induced by CNO pre-treatment in rats[3].
MK-1064 (1-5 mg/kg, intravenous injection/oral administration) shows moderate oral bioavailability and clearance in rat, dog, and rhesus monkey[1].
| Animal Model: | Wild-type and OX2R knockout mice[2] | | 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)[1] | | Dosage: | 1, 2, 3, 5 mg/kg | | Administration: | Oral administration (P.O.), intravenous injection (I.V.) | | Result: | Pharmacokinetics profile of MK-1064.
| Species | Dose (mg/kg) | CL (mL/min/kg) | t1/2(h) | Dose (mg/kg) | Cmax(μM) | F (%) | | Rat | 2 (I.V.) | 39 | 0.3 | 5 (P.O.) | 1.5 | 54 | |
| Dog | 1 (I.V.) | 16 | 1.0 | 3 (P.O.) | 1.0 | 48 | |
| Rhesus | 2 (I.V.) | 12 | 0.8 | 5 (P.O.) | 0.9 | 16 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 50 mg/mL(108.25 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.1650 mL | 10.8249 mL | 21.6497 mL | | 5 mM | 0.4330 mL | 2.1650 mL | 4.3299 mL | | 10 mM | 0.2165 mL | 1.0825 mL | 2.1650 mL |
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以下溶剂前显示的百
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此方案可获得 ≥ 2.5 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 *以上所有助溶剂都可在本网站选购。
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