Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate)
(Synonyms: GLYX-13 Trifluoroacetate) 目录号 : GC33492
A partial agonist of the NMDA receptor
Cas No.:1435786-04-1
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Animal experiment: | Male C57BL/6J mice are used in this study. Mice are group housed (five/cage) in a controlled environment held at 21±2°C with a 14:10 h light-dark period (lights on:±05:00 am). All experiments are conducted during the light phase. Food and water are available ad libitum. For acute drug treatments, Rapastinel Trifluoroacetate (1.0 mg/kg, iv) is administered 30 min prior to the acquisition trial of the novel object recognition (NOR) task to the subchronic ketamine or subchronic phencyclidine (PCP)-treated animals[1]. |
References: [1]. Rajagopal L, et al. GLYX-13 (rapastinel) ameliorates subchronic phencyclidine- and ketamine-induced declarative memory deficits in mice. Behav Brain Res. 2016 Feb 15;299:105-10. | |
GLYX 13 is a monoclonal antibody-derived tetrapeptide that acts as a partial agonist at the glycine site of the N-methyl-D-aspartate (NMDA) receptor.1,2 It is active in vivo when administered intravenously, and it readily passes through the blood-brain barrier.1,3 GLYX 13 has diverse effects in animals, as it blocks neuropathic pain, enhances learning and memory, and significantly reduces anxiety.2,3,4 GLYX 13 induces rapid antidepressant-like effects in animal models and rescued normal behavior in a rat model of autism.5,6,7
1.Moskal, J.R., Kuo, A.G., Weiss, C., et al.GLYX-13: a monoclonal antibody-derived peptide that acts as an N-methyl-D-aspartate receptor modulatorNeuropharmacology49(7)1077-1087(2005) 2.Wood, P.L., Mahmood, S.A., and Moskal, J.R.Antinociceptive action of GLYX-13: An N-methyl-D-aspartate receptor glycine site partial agonistNeuroport.19(10)1059-1061(2008) 3.Burgdorf, J., Zhang, X.-l., Weiss, C., et al.The N-methyl-D-aspartate receptor modulator GLYX-13 enhances learning and memory, in young adult and learning impaired aging ratsNeurobiol. Aging32(4)698-706(2011) 4.Jin, Z.-L., Liu, J.-X., Liu, X., et al.Anxiolytic effects of GLYX-13 in animal models of posttraumatic stress disorder-like behaviorJ. Psychopharmacol.30(9)913-921(2016) 5.Burgdorf, J., Zhang, X.-l., Nicholson, K.L., et al.GLYX-13, a NMDA receptor glycine-site functional partial agonist, induces antidepressant-like effects without ketamine-like side effectsNeuropsychopharmacology38(5)729-742(2013) 6.Santini, A.C., Pierantoni, G.M., Gerlini, R., et al.Glix 13, a new drug acting on glutamatergic pathways in children and animal models of autism spectrum disordersBiomed. Res. Int.2014234295(2014) 7.Yang, B., Zhang, J.-c., Han, M., et al.Comparison of R-ketamine and rapastinel antidepressant effects in the social defeat stress model of depressionPsychopharmacology233(19-20)3647-3657(2016)
| Cas No. | 1435786-04-1 | SDF | |
| 别名 | GLYX-13 Trifluoroacetate | ||
| Canonical SMILES | O=C([C@H]1N(C([C@H]2N(C([C@@H](N)[C@H](O)C)=O)CCC2)=O)CCC1)N[C@@H]([C@H](O)C)C(N)=O.O=C(O)C(F)(F)F | ||
| 分子式 | C20H32F3N5O8 | 分子量 | 527.49 |
| 溶解度 | DMSO : 125 mg/mL (236.97 mM) | 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 | 1.8958 mL | 9.4789 mL | 18.9577 mL |
| 5 mM | 0.3792 mL | 1.8958 mL | 3.7915 mL |
| 10 mM | 0.1896 mL | 0.9479 mL | 1.8958 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。