Rapastinel Trifluoroacetate
Based on 1 publication(s) in Google Scholar
Rapastinel (GLYX-13) Trifluoroacetate is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel Trifluoroacetate enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel Trifluoroacetate moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel Trifluoroacetate is applicable to the research of major depressive disorder and hepatocellular carcinoma.
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 1435786-04-1
- Formula: C20H32F3N5O8
- Molecular Weight:527.49
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Rapastinel Trifluoroacetate
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Biological Activity
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NMDA Receptor |
Rapastinel Trifluoroacetate (20 μM; 4 h) reverses the propofol-induced reductions in CaMKII phosphorylation, AKT phosphorylation, HIF-1α expression, intracellular Ca2+ concentration, glycolysis protein levels, adhesion molecule levels, and tumor cell-endothelial cell adhesion in Huh7 tumor conditioned medium-treated HUVECs[2].
Rapastinel Trifluoroacetate (tested concentrations; 15 min preincubation, 15 min with [3H] MK-801) partially enhances [3H] MK-801 binding to recombinant human NR2A-, NR2B-, NR2C-, and NR2D-containing NMDARs with EC50 values of 9.8 pM, 9.9 nM, 2.2 pM, and 1.7 pM, respectively[5].
Rapastinel Trifluoroacetate (100 nM-1 μM) has its modulatory effects on NMDAR-mediated calcium mobilization completely abolished by mutations of critical amino acids in the NR2A(R392E) or NR2B(R393E) NMDAR amino terminal domain, confirming this domain is required for rapastinel's activity[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
A single intravenous administration of Rapastinel (3 mg/kg) Trifluoroacetate produces sustained antidepressant-like and anxiolytic-like effects in male Sprague-Dawley rats for at least 1 week, as evidenced by significant changes in ultrasonic vocalizations, time spent in the central zone of the open field test, and immobility time in the Porsolt forced swim test. It also induces sustained cognitive-enhancing effects, as reflected by improved behavioral performance of rats in spontaneous alternation, positive affective learning, Morris water maze, and contextual fear extinction tests[3].
Rapastinel (1 mg/kg; subcutaneous injection; twice daily; administered for 3 or 5 days) Trifluoroacetate reverses subchronic Phencyclidine-induced novel object recognition (NOR) impairment for at least 9 or 10 weeks, respectively, whereas Rapastinel (1 mg/kg; subcutaneous injection; 30 minutes in advance; single dose) Trifluoroacetate only transiently reverses NOR function when the test interval is 24 hours[4].
Rapastinel (10-30 mg/kg; subcutaneous injection; single administration) Trifluoroacetate produces rapid and sustained antidepressant-like effects in rats, corresponding to concentrations of approximately 30 nM and ~100 nM in the medial prefrontal cortex (mPFC), respectively[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1435786-04-1
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Appearance Solid
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Molecular Weight 527.49
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Formula C20H32F3N5O8
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Color White to off-white
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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
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Synonyms
GLYX-13 Trifluoroacetate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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J Cell Mol Med
Calpain-2 plays a pivotal role in the inhibitory effects of propofol against TNF-α-induced autophagy in mouse hippocampal neurons. [Abstract]2020 Aug;24(16):9287-9299. PMID: 32627970
Rapastinel Trifluoroacetate purchased from MedChemExpress. Usage Cited in: J Cell Mol Med. 2020 Aug;24(16):9287-9299. [Abstract]
Neurons are pre-treated with 25 μM propofol plus 20 μM Rapastinel, followed by TNF-α treatment (40 ng/mL, 2 h). The effect of propofol on TNF-α- induced intracellular calcium accumulation, phosphorylation of CaMK II and calpain-2, calpain activation, cathepsin B release and TrkB truncation is counteracted by Rapastinel.
Solvent & Solubility
DMSO : 125 mg/mL (236.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Shen M, et al. ERK/mTOR signaling may underlying the antidepressant actions of rapastinel in mice. Transl Psychiatry. 2022;12(1):522. Published 2022 Dec 22. [Content Brief]
[2]. Qi J, et al. Propofol attenuates the adhesion of tumor and endothelial cells through inhibiting glycolysis in human umbilical vein endothelial cells. Acta Biochim Biophys Sin (Shanghai). 2019;51(11):1114-1122. [Content Brief]
[3]. Burgdorf J, et al. The long-lasting antidepressant effects of rapastinel (GLYX-13) are associated with a metaplasticity process in the medial prefrontal cortex and hippocampus. Neuroscience. 2015;308:202-211. [Content Brief]
[4]. Rajagopal L, et al. Repeated administration of rapastinel produces exceptionally prolonged rescue of memory deficits in phencyclidine-treated mice. Behav Brain Res. 2022;432:113964. [Content Brief]
[5]. Donello JE, et al. Positive N-Methyl-D-Aspartate Receptor Modulation by Rapastinel Promotes Rapid and Sustained Antidepressant-Like Effects. Int J Neuropsychopharmacol. 2019;22(3):247-259. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8958 mL | 9.4789 mL | 18.9577 mL | 47.3943 mL |
| 5 mM | 0.3792 mL | 1.8958 mL | 3.7915 mL | 9.4789 mL | |
| 10 mM | 0.1896 mL | 0.9479 mL | 1.8958 mL | 4.7394 mL | |
| 15 mM | 0.1264 mL | 0.6319 mL | 1.2638 mL | 3.1596 mL | |
| 20 mM | 0.0948 mL | 0.4739 mL | 0.9479 mL | 2.3697 mL | |
| 25 mM | 0.0758 mL | 0.3792 mL | 0.7583 mL | 1.8958 mL | |
| 30 mM | 0.0632 mL | 0.3160 mL | 0.6319 mL | 1.5798 mL | |
| 40 mM | 0.0474 mL | 0.2370 mL | 0.4739 mL | 1.1849 mL | |
| 50 mM | 0.0379 mL | 0.1896 mL | 0.3792 mL | 0.9479 mL | |
| 60 mM | 0.0316 mL | 0.1580 mL | 0.3160 mL | 0.7899 mL | |
| 80 mM | 0.0237 mL | 0.1185 mL | 0.2370 mL | 0.5924 mL | |
| 100 mM | 0.0190 mL | 0.0948 mL | 0.1896 mL | 0.4739 mL |
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