1. GPCR/G Protein Neuronal Signaling Autophagy
  2. Adrenergic Receptor Autophagy
  3. Prazosin hydrochloride

Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM.Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively.

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Prazosin hydrochloride Chemical Structure

Prazosin hydrochloride Chemical Structure

CAS No. : 19237-84-4

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10 mM * 1 mL in DMSO
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Based on 9 publication(s) in Google Scholar

Other Forms of Prazosin hydrochloride:

Top Publications Citing Use of Products

    Prazosin hydrochloride purchased from MedChemExpress. Usage Cited in: Biomed Pharmacother. 2020 Apr;124:109731.  [Abstract]

    The expression of TNS1 in U937 and HL60 cells treated with different concentration of Prazosin is detected by Western blot analysis

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    • Purity & Documentation

    • References

    • Customer Review

    Description

    Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders[1]. Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM[2].Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively[3].

    IC50 & Target

    α adrenergic receptor

     

    In Vitro

    Prazosin (0, 2.5, 5, 7.5, 10, 15, 20, 30, 40 and 50 μM) effectively inhibits the proliferation of U251 and U87 cells[4].
    ? Prazosin inhibits the migration and invasion of U251 and U87 cells[4].
    ? Prazosin treatment decreases the protein expression of components of the PI3K/AKT/mTOR signaling pathway. Prazosin (13.16 and 11.57 μM for U251 and U87 cells, 48 hours) decreases the expression levels of P70 and cyclin D1, which are downstream target genes of the PI3K/AKT/mTOR signaling pathway[4].

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

    Cell Proliferation Assay

    Cell Line: U251 and U87 cells
    Concentration: 0, 2.5, 5, 7.5, 10, 15, 20, 30, 40 and 50 µM.
    Incubation Time: 48 hours
    Result: The IC50s were 13.16±0.95 and 11.57±0.79 µM for U251 and U87 cells, respectively.

    Western Blot Analysis

    Cell Line: U251 and U87 cells
    Concentration: 13.16 and 11.57 µM for U251 and U87 cells, respectively
    Incubation Time: 48 hours
    Result: Protein expression levels of Bax and active Caspase-3 were increased.
    Bcl-2 levels were also decreased after prazosin treatment (P<0.05).
    The expression of p-AKT and p-mTOR, P70 and cyclin D1 were decreased.
    In Vivo

    Peripheral administration of Prazosin (0, 0.5, 1.0, 1.5 or 2.0 mg/kg; i.p.) can suppress not only central α1-adrenergic-mediated hyperexcitability but also stress-induced anxiety[1].

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

    Animal Model: Fifty-five alcohol-naive male rats from the 60th generation of selective breeding for alcohol preference[1]
    Dosage: 0.5, 1.0, 1.5, or 2.0 mg/kg
    Administration: Injected intraperitoneally (IP); 0.5 mg/mL; once a day at 15 min prior to onset of the daily two hour two-bottle choice, alcohol versus water, access period for two consecutive days and then three weeks later for five consecutive days.
    Result: Significantly reduced alcohol intake during the initial two daily administrations, and this reduction of alcohol intake was maintained for five consecutive days by daily prazosin treatment in the subsequent more prolonged trial.
    Clinical Trial
    Molecular Weight

    419.86

    Formula

    C19H22ClN5O4

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)C4=CC=CO4.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 14.29 mg/mL (34.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 0.59 mg/mL (1.41 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.3817 mL 11.9087 mL 23.8175 mL
    5 mM 0.4763 mL 2.3817 mL 4.7635 mL
    View the 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, 1 years; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.43 mg/mL (3.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

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

      Solubility: ≥ 1.43 mg/mL (3.41 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References

    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, 1 years; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 years. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.3817 mL 11.9087 mL 23.8175 mL 59.5437 mL
    DMSO 5 mM 0.4763 mL 2.3817 mL 4.7635 mL 11.9087 mL
    10 mM 0.2382 mL 1.1909 mL 2.3817 mL 5.9544 mL
    15 mM 0.1588 mL 0.7939 mL 1.5878 mL 3.9696 mL
    20 mM 0.1191 mL 0.5954 mL 1.1909 mL 2.9772 mL
    25 mM 0.0953 mL 0.4763 mL 0.9527 mL 2.3817 mL
    30 mM 0.0794 mL 0.3970 mL 0.7939 mL 1.9848 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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      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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