2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. Rapastinel Trifluoroacetate

Rapastinel Trifluoroacetate  (Synonyms: GLYX-13 Trifluoroacetate)

Cat. No.: HY-16728B Purity: ≥98.0%
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Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.

For research use only. We do not sell to patients.

Rapastinel Trifluoroacetate Chemical Structure

Rapastinel Trifluoroacetate Chemical Structure

CAS No. : 1435786-04-1

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 244 In-stock
Solution
10 mM * 1 mL in DMSO USD 244 In-stock
Solid
1 mg USD 70 In-stock
5 mg USD 210 In-stock
10 mg USD 350 In-stock
25 mg USD 650 In-stock
50 mg USD 890 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Rapastinel Trifluoroacetate:

Rapastinel Trifluoroacetate Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Rapastinel Trifluoroacetate

WB

    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.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Rapastinel Trifluoroacetate (GLYX-13 Trifluoroacetate) is an NMDA receptor modulator with glycine-site partial agonist properties. Rapastinel Trifluoroacetate has the potential for major depressive disorder treatment.

    IC50 & Target

    NMDA receptor[1]
    In Vivo

    Rapastinel Trifluoroacetate is an NMDA receptor modulator with glycine-site partial agonist properties and currently in a phase II clinical development program as an adjunctive therapy for major depressive disorder. Mice given Rapastinel Trifluoroacetate (1.0 mg/kg) prior to acute ketamine (30 mg/kg) show clear preference for novel compare to familiar objects (P<0.01)[1]. Rapastinel Trifluoroacetate produces an antidepressant like effect in the USVs test, as indexed by an increase in hedonic 50-kHz USVs [F(1,20)=12.4, P<0.05] and a decrease in aversive 20-kHz USVs [F(1,20)=6.8, P<0.05]. Rapastinel Trifluoroacetate also produces an anxiolytic effect in the open field, as indexed by increased center time [F(1,20)=19.2, P<0.05] without altering locomotor activity as measured by line crosses [F(1,20)=0.0, P>0.05][2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    527.49

    Formula

    C20H32F3N5O8
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: 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)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: ≥98.0%

    COA (257 KB) HNMR (285 KB) MS (68 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    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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    Rapastinel Trifluoroacetate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Rapastinel1435786-04-1GLYX-13GLYX13GLYX 13iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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