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  3. Rapastinel

Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Rapastinel Trifluoroacetate) usually boasts enhanced water solubility and stability.

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

Rapastinel Chemical Structure

Rapastinel Chemical Structure

CAS No. : 117928-94-6

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Top Publications Citing Use of Products

1 Publications Citing Use of MCE Rapastinel

WB

    Rapastinel 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

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    Description

    Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist. Target: NMDA Rapastinel is a robust cognitive enhancer and facilitates hippocampal long-term potentiation (LTP) of synaptic transmission in slices.

    Clinical Trial
    Molecular Weight

    413.47

    Formula

    C18H31N5O6

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    Sequence

    Thr-Pro-Pro-Thr-NH2

    Sequence Shortening

    TPPT-NH2

    SMILES

    O=C(N(CCC1)[C@@H]1C(N[C@H](C(N)=O)[C@H](O)C)=O)[C@H](CCC2)N2C([C@@H](N)[C@H](O)C)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 32 mg/mL (77.39 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.4186 mL 12.0928 mL 24.1856 mL
    5 mM 0.4837 mL 2.4186 mL 4.8371 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    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.
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    Working solution concentration: mg/mL
    Purity & Documentation
    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. 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 2.4186 mL 12.0928 mL 24.1856 mL 60.4639 mL
    5 mM 0.4837 mL 2.4186 mL 4.8371 mL 12.0928 mL
    10 mM 0.2419 mL 1.2093 mL 2.4186 mL 6.0464 mL
    15 mM 0.1612 mL 0.8062 mL 1.6124 mL 4.0309 mL
    20 mM 0.1209 mL 0.6046 mL 1.2093 mL 3.0232 mL
    25 mM 0.0967 mL 0.4837 mL 0.9674 mL 2.4186 mL
    30 mM 0.0806 mL 0.4031 mL 0.8062 mL 2.0155 mL
    40 mM 0.0605 mL 0.3023 mL 0.6046 mL 1.5116 mL
    50 mM 0.0484 mL 0.2419 mL 0.4837 mL 1.2093 mL
    60 mM 0.0403 mL 0.2015 mL 0.4031 mL 1.0077 mL
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    Rapastinel 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.

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    Product Name:
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    Cat. No.:
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