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Chlorzoxazone P450 (e.g. CYP17) chemical

Name: Chlorzoxazone
Brand: Selleck Chemicals
SKU: S4155
Rating: 5 (1 reviews)

Cat.No.S4155

Chlorzoxazone(Chlorzoxazon,Paraflex) is a muscle-relaxing drug, and this compound is a probe for human liver cytochrome P-450IIE1.

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%

Cited in Nature Medicine for its top-tier quality
COA
NMR
SDS
Datasheet

99.8

Related Targets	Dehydrogenase HSP Transferase PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Other P450 (e.g. CYP17) Inhibitors	Apigenin Baicalein Avasimibe Naringenin Diosmetin Alizarin Orteronel Benzbromarone Sodium Danshensu Naringin

Chemical Information, Storage & Stability

Molecular Weight	169.57	Formula	C₇H₄ClNO₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	95-25-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	Chlorzoxazon,Paraflex			Smiles	C1=CC2=C(C=C1Cl)NC(=O)O2

Solubility

In vitro
Batch:

DMSO : 34 mg/mL (200.5 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 34 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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 catalysed 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. 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.

References

[1] https://pubmed.ncbi.nlm.nih.gov/8791768/
[2] https://pubmed.ncbi.nlm.nih.gov/11181893/

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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