Home Metabolism P450 (e.g. CYP17) chemical Chlorzoxazone

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Chlorzoxazone P450 (e.g. CYP17) chemical

Cat.No.S4155

Chlorzoxazone(Chlorzoxazon,Paraflex) is a muscle-relaxing drug, and this compound is a probe for human liver cytochrome P-450IIE1.
Chlorzoxazone P450 (e.g. CYP17) chemical Chemical Structure

Chemical Structure

Molecular Weight: 169.57

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Quality Control

Batch: S415501 DMSO]34 mg/mL]false]Ethanol]34 mg/mL]false]Water]Insoluble]false Purity: 99.8%
99.8

Chemical Information, Storage & Stability

Molecular Weight 169.57 Formula

C7H4ClNO2

 Storage (From the date of receipt)
CAS No. 95-25-0 Download SDF Storage of Stock Solutions

Synonyms Chlorzoxazon,Paraflex Smiles C1=CC2=C(C=C1Cl)NC(=O)O2

Solubility

In vitro
Batch:

DMSO : 34 mg/mL ( (200.5 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 34 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

In vitro

Chlorzoxazone is well documented to be metabolized mainly to 6-hydroxychlorzoxazone physically, which is catalyzed primarily by CYP2E1. Other human hepatic P450 enzymes, namely CYP1A1, CYP1A2 and CYP3A4 may also contribute to this compound metabolism. It has been used as a probe for CYP2E1 activity in microsomes from various sources (e.g., liver, kidney, lung cells) as well as directly in cell cultures. [1] This chemical is a centrally acting skeletal muscle relaxant, which acts on the spinal cord by depressing reflexes. It is able to activate rat brain SK2 channel currents in cells. The maximal response to this compound is achieved at 1 mM, which is 44% ( 62%) of the response to 1 mM 1-EBIO. [2]
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02654236 Completed
Alcohol Consumption
Suthat Liangpunsakul|National Institute on Alcohol Abuse and Alcoholism (NIAAA)|Intercept Pharmaceuticals|Indiana University
 April 2016 Not Applicable
NCT00138684 Completed
Insulin Resistance|Iron Overload
Rennes University Hospital|Ministry of Health France
 September 2003 Phase 2

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