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

PRE-084 hydrochloride 

Cat. No.: HY-18100A Purity: 99.79%
COA Handling Instructions

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

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

PRE-084 hydrochloride Chemical Structure

PRE-084 hydrochloride Chemical Structure

CAS No. : 75136-54-8

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10 mM * 1 mL in DMSO USD 83 In-stock
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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    PRE-084 hydrochloride purchased from MCE. 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).

    PRE-084 hydrochloride purchased from MCE. 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.

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    Description

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

    In Vitro

    PRE-084 hydrochloride (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].

    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 hydrochloride (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 hydrochloride (1 mg/kg; i.p.; single) protects the heart by activating the Akt‑eNOS pathway in myocardial infarction model[3].

    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.
    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

    353.88

    Formula

    C19H28ClNO3

    CAS No.
    SMILES

    O=C(C1(C2=CC=CC=C2)CCCCC1)OCCN3CCOCC3.[H]Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 34 mg/mL (96.08 mM)

    H2O : 33.33 mg/mL (94.18 mM; ultrasonic and warming and heat to 60°C)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.8258 mL 14.1291 mL 28.2582 mL
    5 mM 0.5652 mL 2.8258 mL 5.6516 mL
    10 mM 0.2826 mL 1.4129 mL 2.8258 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 (5.88 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: ≥ 2.08 mg/mL (5.88 mM); Clear solution

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (5.88 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.79%

    References
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    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:
    PRE-084 hydrochloride
    Cat. No.:
    HY-18100A
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