2. Membrane Transporter/Ion Channel Neuronal Signaling Stem Cell/Wnt MAPK/ERK Pathway PI3K/Akt/mTOR
  3. iGluR ERK mTOR
  4. Rapastinel

Rapastinel (GLYX-13) is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel is applicable to the research of major depressive disorder and hepatocellular carcinoma.

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CAS. Nr. : 117928-94-6

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Based on 1 publication(s) in Google Scholar

Other Forms of Rapastinel:

Rapastinel Related Antibodies

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.

    Alle iGluR Isoform-spezifische Produkte anzeigen:

    Alle Isoformen anzeigen
    AMPA Receptor NMDA Receptor Kainate Receptor

    Alle ERK Isoform-spezifische Produkte anzeigen:

    Alle Isoformen anzeigen
    ERK ERK1 ERK2 ERK5 ERK8

    Alle mTOR Isoform-spezifische Produkte anzeigen:

    Alle Isoformen anzeigen
    mTOR mTORC1 mTORC2

    • Biologische Aktivität

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    Beschreibung

    Rapastinel (GLYX-13) is a potent NMDAR modulator capable of crossing the blood-brain barrier, and it exhibits extremely high affinity for human NMDAR (EC50=0.0017-9.9 nM). Rapastinel enhances ERK signaling and activates the mTOR pathway, thereby upregulating the expression of BDNF and VGF, and inducing significant neuroplastic changes such as enhanced LTP and increased mature dendritic spine density in the hippocampus. Rapastinel moderately elevates the efflux of dopamine, norepinephrine and 5-HT in the prefrontal cortex, and uniquely avoids side effects of traditional antidepressants such as dissociation, addiction or sedation. Rapastinel is applicable to the research of major depressive disorder and hepatocellular carcinoma[1][2][3][4][5].

    IC50 & Target

    NMDA Receptor

     

    In Vitro

    Rapastinel (20 μM; 4 h) reverses the propofol-induced reductions in CaMKII phosphorylation, AKT phosphorylation, HIF-1α expression, intracellular Ca2+ concentration, glycolysis protein levels, adhesion molecule levels, and tumor cell-endothelial cell adhesion in Huh7 tumor conditioned medium-treated HUVECs[2].
    Rapastinel (tested concentrations; 15 min preincubation, 15 min with [3H] MK-801) partially enhances [3H] MK-801 binding to recombinant human NR2A-, NR2B-, NR2C-, and NR2D-containing NMDARs with EC50 values of 9.8 pM, 9.9 nM, 2.2 pM, and 1.7 pM, respectively[5].
    Rapastinel (100 nM-1 μM) has its modulatory effects on NMDAR-mediated calcium mobilization completely abolished by mutations of critical amino acids in the NR2A(R392E) or NR2B(R393E) NMDAR amino terminal domain, confirming this domain is required for rapastinel's activity[5].

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

    Rapastinel Related Antibodies

    Western Blot Analysis[2]

    Cell Line: human umbilical vein endothelial cells (HUVECs) pretreated with Huh7 tumor conditioned medium
    Concentration: 20 μM (co-administered with 25 μM propofol)
    Incubation Time: 4 h
    Result: Reversed the inhibitory effect of propofol on CaMKII phosphorylation, AKT phosphorylation, and HIF-1α expression in HUVECs.
    Reversed the propofol-induced reduction in intracellular Ca2+ concentration.
    Reversed the propofol-induced downregulation of glycolysis proteins (GLUT1, HK2, LDHA) and restored ECAR levels.
    Reversed the propofol-induced downregulation of adhesion molecules (E-selectin, VCAM-1, ICAM-1).
    Reversed the propofol-induced reduction in Huh7 cell adhesion to HUVECs.
    All effects were statistically significant relative to the propofol-only treated group.
    In Vivo

    Rapastinel (5-10 mg/kg; intravenous injection, once daily for 3 consecutive days) exerts rapid antidepressant-like effects in mice with CUS-induced depression, reverses behavioral deficits, and normalizes the ERK/mTOR/VGF/BDNF signaling pathway in the hippocampus and prefrontal cortex (PFC); in contrast, Rapastinel (0.5 mg/kg; intravenous injection, once daily for 3 consecutive days) shows no activity[1].
    A single intravenous administration of Rapastinel (3 mg/kg) produces sustained antidepressant-like and anxiolytic-like effects in male Sprague-Dawley rats for at least 1 week, as evidenced by significant changes in ultrasonic vocalizations, time spent in the central zone of the open field test, and immobility time in the Porsolt forced swim test. It also induces sustained cognitive-enhancing effects, as reflected by improved behavioral performance of rats in spontaneous alternation, positive affective learning, Morris water maze, and contextual fear extinction tests[3].
    Rapastinel (1 mg/kg; subcutaneous injection; twice daily; administered for 3 or 5 days) reverses subchronic Phencyclidine-induced novel object recognition (NOR) impairment for at least 9 or 10 weeks, respectively, whereas Rapastinel (1 mg/kg; subcutaneous injection; 30 minutes in advance; single dose) only transiently reverses NOR function when the test interval is 24 hours[4].
    Rapastinel (10-30 mg/kg; subcutaneous injection; single administration) produces rapid and sustained antidepressant-like effects in rats, corresponding to concentrations of approximately 30 nM and ~100 nM in the medial prefrontal cortex (mPFC), respectively[5].

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

    Animal Model: C57BL/6J (male, adult, 20-25 g, CUS-induced depression)[1]
    Dosage: 0.5 mg/kg; 5 mg/kg; 10 mg/kg
    Administration: i.v.; daily for 3 consecutive days
    Result: Significantly reversed CUS-induced reductions in OFT line crossings and rearings, and significantly reversed CUS-induced reductions in sucrose preference (5 and 10 mg/kg).
    Significantly reversed CUS-induced increases in NSFT feeding latency and FST immobility time (5 and 10 mg/kg).
    Significantly reversed CUS-induced downregulation of phosphorylated ERK1/2, phosphorylated mTOR, phosphorylated p70S6k, and phosphorylated 4E-BP1 in the hippocampus and PFC (5 and 10 mg/kg).
    Significantly reversed CUS-induced reductions in BDNF and VGF expression in the hippocampal CA1, CA2/3, and DG subregions, as well as in the PFC (5 and 10 mg/kg).
    Did not produce significant changes in measured behavioral or molecular measures (0.5 mg/kg).
    Animal Model: C57BL/6J (2-3-month-old male; subchronic PCP-induced cognitive impairment)[4]
    Dosage: 1 mg/kg (NOR testing); 3 mg/kg (ORL testing)
    Administration: s.c.; single dose 30 min prior to NOR/ORL testing
    Result: Blocked the ability of rapastinel 1 mg/kg s.c.
    to increase DI in the NOR task, with DI remaining at 0.07 (comparable to subchronic PCP+vehicle levels) following rapamycin pre-treatment.
    Blocked the ability of rapastinel 3 mg/kg s.c.
    to increase percent correct responses in the ORL task, with responses remaining at 48% (comparable to subchronic PCP+vehicle levels of 38%) following rapamycin pre-treatment.
    Animal Model: Sprague-Dawley (male; 6-10 weeks old for mPFC slice studies; unspecified age for forced swim test and microdialysis)[5]
    Dosage: 3 mg/kg; 10 mg/kg; 30 mg/kg
    Administration: s.c.; single dose
    Result: Produced a rapid (within 1 hour) and sustained (>7 days) dose-dependent antidepressant-like effect in the forced swim test at 10 and 30 mg/kg.
    Reached a Tmax of ~20 minutes and a half-life of ~20 minutes in rat mPFC extracellular fluid.
    Achieved a brain concentration of ~30 nM at 10 mg/kg, associated with minimal antidepressant efficacy.
    Achieved a brain concentration of ~100 nM at 30 mg/kg, associated with maximal antidepressant efficacy.
    Klinische Studie
    Molekulargewicht

    413.47

    Formel

    C18H31N5O6
    CAS. Nr.
    Appearance

    Solid

    Color

    White to off-white

    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
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    Room temperature in continental US; may vary elsewhere.
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    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.

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    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
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    * 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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    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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    • 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:

    Rapastinel117928-94-6GLYX-13GLYX13GLYX 13iGluRERKmTORIonotropic glutamate receptorsExtracellular signal regulated kinasesMammalian target of RapamycinBDNFHuh7blood-brain barrierVGFERK signalingmajor depressive disorderhuman NMDARhippocampal LTPhepatocellular carcinomaInhibitorinhibitorinhibit

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