MK 6096
(Synonyms: MK-6096) 目录号 : GC12242
A dual orexin receptor antagonist
Cas No.:1088991-73-4
Sample solution is provided at 25 µL, 10mM.
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Filorexant (MK-6096) is an orally bioavailable potent and selective reversible antagonist of OX1 and OX2 receptor(<3 nM in binding).
In radioligand binding and functional cell based assays Filorexant (MK-6096) demonstrated potent binding and antagonism of both human OX(1)R and OX(2)R (170 receptors and enzymes. Filorexant (MK-6096) occupies 90% of human OX(2)Rs expressed in transgenic rats at a plasma concentration of 142 nM.
Filorexant (MK-6096) dose-dependently reduced locomotor activity and significantly increased sleep in rats (3-30 mg/kg) and dogs (0.25 and 0.5 mg/kg).
References:
[1]. Winrow CJ, et al. Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia. Neuropharmacology. 2012 Feb;62(2):978-87.
[2]. Coleman PJ, et al. Discovery of [(2R,5R)-5-{[(5-fluoropyridin-2-yl)oxy]methyl}-2-methylpiperidin-1-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanone (MK-6096): a dual orexin receptor antagonist with potent sleep-promoting properties. ChemMedChem. 2012 Mar 5;7(3):415-24, 337.
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Animal experiment: |
Animal administration[1]The male Sprague Dawley rats (n = 8/study; age: 3-6 months; weight: 450-600 g) were singly housed with water and food ad libitum and a 12 h light: 12 h dark cycle with lights on at 04:00 and off at 16:00. Sleep studies were conducted to evaluate Filorexant (3 and 10 mg/kg, p.o.), DORA-22 (10 mg/kg, p.o.) and almorexant (3 and 30 mg/kg, p.o.), employing a counterbalanced crossover design in which all animals were alternatively treated with drug and vehicle daily for either 3 or 7 consecutive days (for DORA-22 and Filorexant, respectively): 2 baseline days (no dosing), a 2 day vehicle-only run-in, a 3 or 7-day arm of drug or vehicle followed by 3 or 7 days of conditional crossover. Effects of compound treatments relative to vehicle (20% Vitamin E TPGS, p.o.) were evaluated following administration in the active phase). |
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References: [1]. Winrow CJ, et al. Pharmacological characterization of MK-6096 - a dual orexin receptor antagonist for insomnia. Neuropharmacology. 2012 Feb;62(2):978-87. |
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| Cas No. | 1088991-73-4 | SDF | |
| 别名 | MK-6096 | ||
| 化学名 | ((2S,5S)-5-(((5-fluoropyridin-2-yl)oxy)methyl)-2-methylpiperidin-1-yl)(5-methyl-2-(pyrimidin-2-yl)phenyl)methanone | ||
| Canonical SMILES | CC1=CC=C(C2=NC=CC=N2)C(C(N3C[C@@H](COC4=NC=C(F)C=C4)CC[C@@H]3C)=O)=C1 | ||
| 分子式 | C24H25FN4O2 | 分子量 | 420.48 |
| 溶解度 | DMF: 10mg/mL,DMF:PBS (pH 7.2) (1:4): 0.2mg/mL,DMSO: 2mg/mL,Ethanol: 5mg/mL | 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 | 2.3782 mL | 11.8912 mL | 23.7823 mL |
| 5 mM | 0.4756 mL | 2.3782 mL | 4.7565 mL |
| 10 mM | 0.2378 mL | 1.1891 mL | 2.3782 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet