Rapastinel Trifluoroacetate

SKU: orb1301461

Description

Rapastinel Trifluoroacetate, also known as GLYX-13 Trifluoroacetate, is a partial agonist at the glycine site of the NMDA receptor. This modulator is utilized in neuroscience research to investigate synaptic plasticity, cognition, and depression-related mechanisms in both cellular and animal models.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1435786-04-1
• MW: 527.49
• Purity: 99.96% (May vary between batches)
• Formula: C₂₀H₃₂F₃N₅O₈
• SMILES: OC(=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
• Target: iGluR,NMDAR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (7.58 mM);DMSO:125 mg/mL (236.97 mM)

Bioactivity

• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Rapastinel Trifluoroacetate, Rapastinel, Thr-Pro-Pro-Thr-NH2 Trifluoroacetate, inhibit, Ionotropic glutamate receptors, NMDA receptor, Inhibitor, iGluR, GLYX 13, GLYX 13 Trifluoroacetate, GLYX13, GLYX-13, GLYX13 Trifluoroacetate, GLYX-13 Trifluoroacetate

Compound Identifiers

PubChem CID

71311638