Chlorzoxazone [95-25-0]

Cat# HY-B1462-5g

Size : 5g

Brand : MedChemExpress

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Description

Chlorzoxazone is a SK-type potassium channel activator. Chlorzoxazone modulates FOXO3 phosphorylation and . Chlorzoxazone enhances immunosuppression, attenuates vasoconstriction, attenuates cognitive deficits, and improves experimental autoimmune encephalomyelitis[1][2][3][4][5][6][7][8][9][10].

IC50 & Target

CYP2

 

In Vitro

Chlorzoxazone (200-1000 μM, 0-24 h) decreases viability and induces [Ca2+]i rises in a concentration‑dependent manner in OC2 cells[2].
Chlorzoxazone (2-20  μM, 4 days) augments immunosuppressive capacity of mesenchymal stem cells via modulation of FOXO3 phosphorylation[3].
Chlorzoxazone (1-30 μM, 30 min) inhibits IL-6 secretion of dendritic cells[4].
Chlorzoxazone (30 μM) suppresses voltage-dependent L-type Ca2+ current in pituitary GH3 cells[5].
Chlorzoxazone (2.5-80 μM, 24 h) attenuates inflammatory response and amyloidogenesis in the isolated astrocytes and microglial cells with Aβ[6].
Chlorzoxazone (300 μM) abolishs 4-aminopyridine (HY-B0604)-induced vasoconstriction in rat thoracic aorta[7].
Chlorzoxazone (600 μM) or 1-EBIO increases Na+ absorption across cystic fibrosis airway epithelial cells[8].

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

Cell Viability Assay[2]

Cell Line: OC2
Concentration: 200, 300, 400, 500, 600, 700 µM
Incubation Time: 24  h
Result: Decreased cell viability in a concentration‑dependent manner.
Showed that BAPTA loading failed to reverse chlorzoxazone‑evoked cell death.
In Vivo

Chlorzoxazone (30-100 mg/kg, p.o., daily, from day 3 following immunization until the end of the experiment) alleviates experimental autoimmune encephalomyelitis in mice[4].
Chlorzoxazone (25-100 mg/kg, p.o., daily, 4 weeks) attenuates cognitive deficits and neuron death in AD mice[6].
Chlorzoxazone (20 mg/kg, i.v.; 50 mg/kg, p.o.) is metabolized to OH-CZX via CYP2E1 in rat models of diabetes induced by Alloxan (HY-W017227) or Streptozotocin (HY-13753)[9].
Chlorzoxazone (10-50 mg/kg, i.p., 20-30 min before onset of access to alcohol) reduces excessive alcohol intake in IAA rats[10].

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

Animal Model: Male C57BL/6 mice with EAE[4]
Dosage: 10, 30, or 100 mg/kg
Administration: Oral gavage (p.o.), daily, from day 3 following immunization until the end of the experiment
Result: Displayed dose-dependent inhibition of EAE severity.
Delayed the onset of EAE and reduced clinical scores during remission of EAE.
Reduced CNS leukocyte infiltration and neuropathy.
Did not affect the size and weight of the spleen.
Clinical Trial
Molecular Weight

169.57

Formula

C7H4ClNO2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1OC2=CC=C(Cl)C=C2N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (589.74 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 5.8974 mL 29.4869 mL 58.9737 mL
5 mM 1.1795 mL 5.8974 mL 11.7947 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.

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: ≥ 2.5 mg/mL (14.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (14.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Purity & Documentation
References

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