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

Rapastinel Trifluoroacetate (Synonyms: GLYX-13 Trifluoroacetate)

Cat. No.: HY-16728B Purity: >98.0%
Handling Instructions

Rapastinel Trifluoroacetate (GLYX-13 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.

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
10 mM * 1 mL in DMSO USD 244 In-stock
Estimated Time of Arrival: December 31
1 mg USD 70 In-stock
Estimated Time of Arrival: December 31
5 mg USD 210 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
25 mg USD 650 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Rapastinel Trifluoroacetate (GLYX-13 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.

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].

Clinical Trial
Molecular Weight

527.49

Formula

C₂₀H₃₂F₃N₅O₈

CAS No.

1435786-04-1

SMILES

O=C([[email protected]]1N(C([[email protected]]2N(C([[email protected]@H](N)[[email protected]](O)C)=O)CCC2)=O)CCC1)N[[email protected]@H]([[email protected]](O)C)C(N)=O.O=C(O)C(F)(F)F

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 : 125 mg/mL (236.97 mM; Need ultrasonic)

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
10 mM 0.1896 mL 0.9479 mL 1.8958 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.94 mM); Clear solution

*All of the co-solvents are provided by MCE.
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

Purity: >98.0%

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Rapastinel Trifluoroacetate
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