1. Anti-infection Metabolic Enzyme/Protease Apoptosis Membrane Transporter/Ion Channel Neuronal Signaling
  2. Bacterial Antibiotic HIF/HIF Prolyl-Hydroxylase Apoptosis MDM-2/p53 Potassium Channel Calcium Channel
  3. Minocycline hydrochloride

Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect.

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

Minocycline hydrochloride Chemical Structure

Minocycline hydrochloride Chemical Structure

CAS No. : 13614-98-7

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Customer Review

Based on 38 publication(s) in Google Scholar

Other Forms of Minocycline hydrochloride:

Top Publications Citing Use of Products

36 Publications Citing Use of MCE Minocycline hydrochloride

Proliferation Assay
IF

    Minocycline hydrochloride purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2018 Aug 30;15(1):245.  [Abstract]

    Immunostaining of the trigeminal nucleus caudalis (TNC) for Iba1 in the NTG group and the NTG+Minocycline (Mino) group on day 9.

    Minocycline hydrochloride purchased from MedChemExpress. Usage Cited in: Neurochem Res. 2017 Oct;42(10):2698-2711.  [Abstract]

    a Statistical analysis showing the prevention effect of minocycline pretreatment (40 mg/kg/day) on CUS-, CRS- or CSDS-induced decreases in hippocampal microglial numbers. b, c Statistical analysis showing the prevention effect of minocycline pretreatment (40 mg/kg/day) on CUS-, CRS- or CSDS-induced increases in the immobile time in the TST (b) and FST (c).
    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect[1][2][3][4][5][6][7].

    IC50 & Target

    L-type calcium channel

     

    In Vitro

    Minocycline hydrochloride (0-100 μM, 24-72 h) suppresses proliferation and clonogenic activity of ovarian cancer cell-lines (OVCAR-3, SKOV-3 and A2780)[3].
    Minocycline hydrochloride (0-100 μM, 24-48 h)arrests cell cycle through inhibition of cyclins and suppression of DNA incorporation[3].
    Minocycline hydrochloride (0-100 μM, 72 h) induces cell apoptosis in ovarian cancer cell lines[3].
    Minocycline hydrochloride shows direct neuronal protection, and this mode of protection is likely to be associated with the preservation of mitochondrial integrity and cytochrome c, followed by the suppression of caspase-dependent as well as caspase-independent cell death[2].
    Minocycline hydrochloride leads to suppression of Hypoxia-inducible factor (HIF)-1α accompanied by up-regulation of p53 protein levels and inactivation of AKT/mTOR/p70S6K/4E-BP1 pathway[6].

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

    Cell Proliferation Assay[3]

    Cell Line: Human ovarian cancer cell lines (OVCAR-3, SKOV-3 and A2780) and primary cells (HEK-293, HMEC, HUVEC, ATCC)
    Concentration: 0, 1, 10, 50 and 100 μM
    Incubation Time: 24, 48 or 72 h
    Result: Inhibited proliferation of OVCAR-3, SKOV-3 and A2780 cells in a concentration-dependent manner, with IC50 values of 62.0, 56.1 and 59.5 μM, respectively. Had no effect on the viability of HEK-293 or HUVEC.

    Western Blot Analysis[3]

    Cell Line: OVCAR-3, SKOV-3 and A2780 cells
    Concentration: 0, 10, 50 and 100 μM
    Incubation Time: 72 h
    Result: Expressed lower levels of cyclins A, B and E. Increased caspase-3 levels by more than 3.0 fold in the 100 μM. Minocycline-activated caspase-3 in turn led to cleavage of PARP-1. Increased the degradation product p89 of PARP-1 by caspase-3.

    Cell Cycle Analysis[3]

    Cell Line: OVCAR-3, SKOV-3 and A2780 cells
    Concentration: 0, 10, 50 and 100 μM
    Incubation Time: 24 or 48 h
    Result: Arrested cells in the G0-G1 phase in a concentration and time-dependent manner. Declined percentage of cells in the S and G2-M phases in excess of 80% each at 100 μM.
    In Vivo

    Minocycline hydrochloride (0-30 mg/kg, orally, daily for 4 weeks) suppresses OVCAR-3 tumor growth in female nude mice[3].
    Minocycline hydrochloride (IP) is an effective neuroprotective agent in animal models of cerebral ischemia when given in high doses intraperitoneally[1].
    Minocycline hydrochloride (0-40 mg/kg, IP, once) significantly attenuats METH-induced hyperlocomotion and the development of behavioral sensitization in mice[2].
    Minocycline hydrochloride (3 and 10 mg/kg, IV, once) is effective at reducing infarct size in a Temporary Middle Cerebral Artery Occlusion model (TMCAO)[1].
    Minocycline hydrochloride (3-10 mg/kg, IV, once) results in serum levels (at 3 mg/kg) similar to that achieved in humans after a standard 200 mg dose[1].
    Minocycline hydrochloride attenuates ischemia-induced ventricular arrhythmias in rats. This effect may be associated with activations of PI3K/Akt signaling pathway, mitochondrial KATP channels and L-type Ca2+ channels[7].

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

    Animal Model: Female nude mice (6 weeks old, 9 per group, OVCAR-3 cells were injected s.c. into the left flank of each mouse)[3]
    Dosage: 10 or 30 mg/kg
    Administration: Administered orally in the drinking water, initiated on day 8 of cell inoculation, daily for 4 weeks
    Result: Suppressed OVCAR-3 tumor growth in these female nude mice, and reduced microvessel density.
    Animal Model: Male Balb/cAnNCrICrIj mice (8 weeks old, 23-30 g, methamphetamine (METH, 3 mg/kg) was injected subcutaneously (s.c.) in a volume of 10 ml/kg)[2]
    Dosage: 0, 10, 20, or 40 mg/kg
    Administration: IP, once, 30 min before the administration of METH
    Result: Significantly attenuated METH-induced hyperlocomotion and the development of behavioral sensitization in mice at 40 mg/kg. Did not exert any effect on the induction of METH-induced hyperthermia in mice. Significantly attenuated the reduction of DA and DOPAC in the striatum. Significantly attenuated the reduction of DAT-immunoreactivity in the mouse striatum. Significantly attenuated the increase in MAC1-immunoreactivity in the striatum after the administration of METH.
    Animal Model: Male Sprague-Dawley rats (270-330 g, TMCAO model)[1]
    Dosage: 3 mg/kg and 10 mg/kg
    Administration: IV, once, 4, 5, or 6 hours post TMCAO
    Result: Reduced infarct size by 42% while 10 mg/kg reduced infarct size by 56% at doses of 3 mg/kg; significantly reduced infarct size at 5 hours by 40% at doses of 10 mg/kg and the 3 mg/kg dose significantly reduced infarct size by 34%. With a 6 hour time window there was a non-significant trend in infarct reduction.
    Animal Model: Male Sprague-Dawley rats (270-330 g)[1]
    Dosage: 3, 10, or 20 mg/kg
    Administration: IV, once
    Result: Peak concentrations of serum levels of minocycline averaged 3.6, 13.0 and 28.8 mg/L with 3, 10 and 20 mg/kg doses respectively. The serum levels of minocycline at a 3 mg/kg dose (3.6 mg/L) were similar to that reported in humans after a standard 200 mg dose. Did not significantly affect hemodynamic and physiological variables.
    Clinical Trial
    Molecular Weight

    493.94

    Formula

    C23H28ClN3O7

    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    OC1=C(C(N)=O)C([C@@]2(O)C(O)=C3C(C4=C(O)C=CC(N(C)C)=C4C[C@@]3([H])C[C@@]2([H])[C@@H]1N(C)C)=O)=O.Cl

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 19.23 mg/mL (38.93 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 9.09 mg/mL (18.40 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0245 mL 10.1227 mL 20.2454 mL
    5 mM 0.4049 mL 2.0245 mL 4.0491 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 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. 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
    =
    Concentration
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  PBS

      Solubility: 7.69 mg/mL (15.57 mM); Clear solution; Need ultrasonic

    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.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation

    Purity: 99.79%

    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 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. 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 2.0245 mL 10.1227 mL 20.2454 mL 50.6134 mL
    5 mM 0.4049 mL 2.0245 mL 4.0491 mL 10.1227 mL
    10 mM 0.2025 mL 1.0123 mL 2.0245 mL 5.0613 mL
    15 mM 0.1350 mL 0.6748 mL 1.3497 mL 3.3742 mL
    DMSO 20 mM 0.1012 mL 0.5061 mL 1.0123 mL 2.5307 mL
    25 mM 0.0810 mL 0.4049 mL 0.8098 mL 2.0245 mL
    30 mM 0.0675 mL 0.3374 mL 0.6748 mL 1.6871 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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    • 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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