MK-1064

MK-1064 serves as a specific, orally effective OX2R antagonist, with a Ki of 0.5 nM and an IC50 of 18 nM, and is observed to facilitate sleep in live models, suggesting its potential for insomnia research¹.³.

Through OX2R targeting, MK-1064 (administered orally at 30 mg/kg) selectively enhances sleep in rodent models, specifically in Wild-type mice².

With a 5-day, oral regimen at 30 mg/kg, MK-1064 counteracts the struggle behavior in rats induced by prior CNO treatment³.

Additionally, varying doses of MK-1064 (1-5 mg/kg, administered either intravenously or orally) demonstrate moderate oral bioavailability and clearance rates in species including rats, dogs, and rhesus monkeys¹.

Through OX2R targeting, MK-1064 (administered orally at 30 mg/kg) selectively enhances sleep in rodent models, specifically in Wild-type mice².

With a 5-day, oral regimen at 30 mg/kg, MK-1064 counteracts the struggle behavior in rats induced by prior CNO treatment³.

Additionally, varying doses of MK-1064 (1-5 mg/kg, administered either intravenously or orally) demonstrate moderate oral bioavailability and clearance rates in species including rats, dogs, and rhesus monkeys¹.

溶解方案(细胞实验)

DMSO 中的溶解度 : 50 mg/mL (108.25 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

溶解方案(动物实验)

"方案 一": "请依序添加每种溶剂：10% DMSO 40% PEG300 5% Tween-80 45% SalineSolubility: ≥ 2.5 mg/mL (5.41 mM); 澄清溶液 此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。"