2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. Coluracetam

Coluracetam (MKC-231) is an orally taken choline uptake enhancer. Coluracetam can improve the reduced acetylcholine levels in the hippocampus of rats and mice, enhancing learning difficulties, memory deficits, and cognitive impairments. Coluracetam induces a lower degree of hepatic venous hyperglycemia.

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CAS. Nr. : 135463-81-9

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Based on 3 publication(s) in Google Scholar

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    Coluracetam purchased from MedChemExpress. Usage Cited in: J Pain Res. 2018 Sep 21:11:1971-1982.  [Abstract]

    Immunoblots for CHT1 in the colon of WAS and WAS-MKC-231-treated rats reveal that the ratios of CHT1 to β-actin expression in WAS rats are considerably increased after 10 consecutive days of MKC-231 treatment.

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    Beschreibung

    Coluracetam (MKC-231) is an orally taken choline uptake enhancer. Coluracetam can improve the reduced acetylcholine levels in the hippocampus of rats and mice, enhancing learning difficulties, memory deficits, and cognitive impairments. Coluracetam induces a lower degree of hepatic venous hyperglycemia[1][2][3].

    In Vivo

    Coluracetam (0.3-3 mg/kg, oral, once a day for 11 days) improves the memory deficits and hippocampal acetylcholine depletion in mice induced by AF64A[1].
    Coluracetam (1-3 mg/kg, oral, once a day for 8 days) improves cognitive and learning impairments in rats[2].
    Coluracetam (5×10-8 and 5×10-7 mol, ventricular injection, single dose) slightly increases hepatic venous glucose levels[3].

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

    Animal Model: Mice induced by AF64A induced[1]
    Dosage: 0.3, 1.0, 3.0 mg/kg, once a day, for 11 days
    Administration: Oral
    Result: Improved memory deficits and significantly reversed cetylcholine depletion.
    Animal Model: Mice induced by AF64A induced[2]
    Dosage: 1.0, 3.0 mg/kg, once a day, for 8 days
    Administration: Oral
    Result: Showed the platform latency in the Morris water maze task shortened, cognitive impairment improved, and high-affinity choline uptake increased.
    Animal Model: Male albino Wistar rats[3]
    Dosage: 5×10-8 and 5×10-7 mol, single dose
    Administration: Intracerebroventricular injection (ICV)
    Result: Slight increased in hepatic venous glucose.
    Molekulargewicht

    341.40

    Formel

    C19H23N3O3
    CAS. Nr.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=C2C(OC(C)=C2C)=NC3=C1CCCC3)CN4C(CCC4)=O
    Versand

    Room temperature in continental US; may vary elsewhere.
    Speicherung
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Lösungsmittel & Löslichkeit
    In Vitro: 

    DMSO : ≥ 20 mg/mL (58.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 0.4 mg/mL (1.17 mM; Need ultrasonic and warming)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.9291 mL 14.6456 mL 29.2912 mL
    5 mM 0.5858 mL 2.9291 mL 5.8582 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 2.9291 mL 14.6456 mL 29.2912 mL 73.2279 mL
    DMSO 5 mM 0.5858 mL 2.9291 mL 5.8582 mL 14.6456 mL
    10 mM 0.2929 mL 1.4646 mL 2.9291 mL 7.3228 mL
    15 mM 0.1953 mL 0.9764 mL 1.9527 mL 4.8819 mL
    20 mM 0.1465 mL 0.7323 mL 1.4646 mL 3.6614 mL
    25 mM 0.1172 mL 0.5858 mL 1.1716 mL 2.9291 mL
    30 mM 0.0976 mL 0.4882 mL 0.9764 mL 2.4409 mL
    40 mM 0.0732 mL 0.3661 mL 0.7323 mL 1.8307 mL
    50 mM 0.0586 mL 0.2929 mL 0.5858 mL 1.4646 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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    Keywords:

    Coluracetam135463-81-9MKC-231MKC231MKC 231iGluRIonotropic glutamate receptorsInhibitorinhibitorinhibit

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