1. Neuronal Signaling PI3K/Akt/mTOR Immunology/Inflammation
  2. Sigma Receptor Akt NO Synthase
  3. PRE-084

PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (PRE-084 hydrochloride) usually boasts enhanced water solubility and stability.

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PRE-084 Chemical Structure

PRE-084 Chemical Structure

CAS No. : 138847-85-5

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Top Publications Citing Use of Products

    PRE-084 purchased from MedChemExpress. Usage Cited in: Exp Neurol. 2022 Mar 5;114034.  [Abstract]

    The therapeutic effect of the σ-1R agonist PRE-084 (0.6 mg/kg; i.p.) in SPS rats is blocked by the mTOR signaling pathway inhibitor Rapamycin.

    PRE-084 purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2020 Apr;41(4):499-507.  [Abstract]

    Chronic PRE-084 treatment alleviates DA neuron loss in Dicer cKO mice. TH and Iba1 immunostaining. Representative photomicrographs are shown at ×20 magnification (scale bars, 100 μm).

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    Description

    PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway[1][2][3][4].

    In Vitro

    PRE-084 (0.1-100 µM; 24 h) protects cultured cortical neurons against β-amyloid toxicity (maximally neuroprotective at 10 µM) and reduces the levels of proapoptotic protein Bax at 10 µM[1].

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

    Cell Viability Assay[1]

    Cell Line: Cortical cells (βAP(25-35)-induced neurotoxicity model)
    Concentration: 0.1-100 µM
    Incubation Time: 24 h
    Result: Reduced neuronal toxicity in a bell shaped-manner and is maximally neuroprotective at 10 µM.

    Western Blot Analysis[1]

    Cell Line: Cortical cells (βAP(25-35)-induced neurotoxicity model)
    Concentration: 10 µM
    Incubation Time: 24 h
    Result: Reduced the levels of proapoptotic protein Bax in cortical neurons induced by βAP(25-35).
    In Vivo

    PRE-084 (0.25 mg/kg; i.p.; 3 times a week for 8 weeks) displays beneficial effects on motor performance (improves motor neuron survival, ameliorates paw abnormality and grip strength performance) in wobbler mice, and shows neuroprotective effects (increases the levels of BDNF in the gray matter)[2].
    PRE-084 (1 mg/kg; i.p.; single) protects the heart by activating the Akt‑eNOS pathway in myocardial infarction model[3].

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

    Animal Model: Wobbler mice (4-week-old)[2].
    Dosage: 0.25 mg/kg
    Administration: Intraperitoneal injection; 3 times a week for 8 weeks.
    Result: Significantly improved ameliorated paw abnormality from week 4, and notably improved paw grip strength at week 5.
    Reduced the number of reactive astrocytes whereas increased the number of pan-macrophage marker CD68-positive cells and CD206+ cells involved in tissue restoration.
    Showed 26.5% increase in the mean number of large-size NISSL-positive motor neurons.
    Animal Model: Adult male Sprague‑Dawley rats (220-250 g; myocardial infarction model)[3].
    Dosage: 1 mg/kg
    Administration: Intraperitoneal injection; single.
    Result: Significantly decreased the degree of myocardial apoptosis.
    Led to significantly increased expression of p‑Akt and p‑eNOS.
    Molecular Weight

    317.42

    Formula

    C19H27NO3

    CAS No.
    SMILES

    O=C(OCCN1CCOCC1)C2(CCCCC2)C3=CC=CC=C3

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Purity & Documentation
    References
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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.

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    Product Name:
    PRE-084
    Cat. No.:
    HY-18100
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