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Rapastinel Trifluoroacetate

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Catalog No. T5819Cas No. 1435786-04-1
Alias Thr-Pro-Pro-Thr-NH2 Trifluoroacetate, GLYX-13 Trifluoroacetate

Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with partial agonist properties at the glycine site.

Rapastinel Trifluoroacetate

Rapastinel Trifluoroacetate

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Purity: 99.77%
Catalog No. T5819Alias Thr-Pro-Pro-Thr-NH2 Trifluoroacetate, GLYX-13 TrifluoroacetateCas No. 1435786-04-1
Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with partial agonist properties at the glycine site.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$33In StockIn Stock
5 mg$77In StockIn Stock
10 mg$123In StockIn Stock
25 mg$198In StockIn Stock
50 mg$372In StockIn Stock
100 mg$587In StockIn Stock
1 mL x 10 mM (in DMSO)$89In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.77%
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Product Introduction

Bioactivity
Description
Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with partial agonist properties at the glycine site.
In vivo
Rapastinel Trifluoroacetate, a tetrapeptide (Thr-Pro-Pro-Thr-amide), has been reported to have fast acting antidepressant properties in man based upon its N-methyl-D-aspartate receptor (NMDAR) glycine site functional partial agonism.
Animal Research
C57BL/6J mice given a single dose or subchronic ketamine (30 mg/kg.i.p.) showed acute or persistent deficits in NOR, respectively.?Acute i.v. rapastinel (1.0 mg/kg), did not induce NOR deficit.?Pre-treatment with Rapastinel Trifluoroacetate?significantly prevented acute ketamine-induced NOR deficit.?Rapastinel Trifluoroacetate?(1.0 mg/kg, but not 0.3 mg/kg, iv) significantly reversed both subchronic ketamine- and subchronic PCP-induced NOR deficits.?Rapastinel Trifluoroacetate?also potentiated the atypical antipsychotic drug with antidepressant properties, lurasidone, to restore NOR in subchronic ketamine-treated mice.?Unlike ketamine,Rapastinel Trifluoroacetate?does not induce a declarative memory deficit in mice, and can prevent or reverse the ketamine-induced NOR deficit.?Further study is required to determine if these differences translate during clinical use of ketamine and rapastinel as fast acting antidepressant drugs and if rapastinel could have non-ionotropic effects as an add-on therapy with antipsychotic/antidepressant medications.
SynonymsThr-Pro-Pro-Thr-NH2 Trifluoroacetate, GLYX-13 Trifluoroacetate
Chemical Properties
Molecular Weight527.49
FormulaC20H32F3N5O8
Cas No.1435786-04-1
SmilesOC(=O)C(F)(F)F.C[C@@H](O)[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(N)=O
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 125 mg/mL (236.97 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (7.58 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8958 mL9.4789 mL18.9577 mL94.7885 mL
5 mM0.3792 mL1.8958 mL3.7915 mL18.9577 mL
10 mM0.1896 mL0.9479 mL1.8958 mL9.4789 mL
20 mM0.0948 mL0.4739 mL0.9479 mL4.7394 mL
50 mM0.0379 mL0.1896 mL0.3792 mL1.8958 mL
100 mM0.0190 mL0.0948 mL0.1896 mL0.9479 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Dose Conversion

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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