Home Metabolism P450 (e.g. CYP17) inhibitor Methoxsalen

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Methoxsalen P450 (e.g. CYP17) inhibitor

Methoxsalen (Xanthotoxin, NCI-C55903) is a naturally occurring photoactive substance found in the seeds of the Ammi majus (Umbelliferae) plant, used in the diagnosis and treatment of psoriasis; this compound is a CYP2A5/6 inhibitor.

Methoxsalen P450 (e.g. CYP17) inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 216.19

Purity & Quality Control

Related Products

Signaling Pathway

P450 (e.g. CYP17) Signaling Pathways

P450 (e.g. CYP17) Signaling Pathway

Mechanism of Action

Targets
CYP2A5 [6] CYP2A6 [6]

In vitro
In vitro Methoxsalen inhibits CYP2A6 (Ki = 0.8 μM) with about 3.5- 94-fold greater potency than other P450s, except for CYP1A2 (Ki = 0.2 μM). This compound shows noncompetitive inhibition of nicotine metabolism, with an apparent Ki value of 0.1 μM in cDNA-expressing microsomes. [1] It is metabolized in human liver microsomes at the rate of 50-100 pmol/mg protein/min (approx. 30% of the activity in mouse liver microsomes). This chemical is a very potent inhibitor of human cytochrome P450 2A6 (CYP2A6) and mouse Cyp2a-5-mediated coumarin 7-hydroxylation in vitro. [2]

In Vivo
In vivo Methoxsalen results in a significant decrease in the following factors: number and diameter of corpus lutei, Graafian follicles, diameter of granulosa cell layer and oocytes, number of primordial and primary and growing follicles, while the number of atretic follicle is increased. This compound also significantly reduces circulating estrogen levels in blood serum of oogenesis Balb/C mice. [3] It dose-dependently stimulates a sustained increase in short-circuit current in the mouse jejunum. The chemical increases the open probability of the basolateral IK(Ca) channel of isolated crypts in the mouse jejunum. [4] It effectively reverses trimethyltin (TMT)-induced memory impairment on both Y-maze and passive avoidance tests in mice. This agent inhibits brain AchE activity. It significantly ameliorates the level of oxidative stress. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04389281 Recruiting
Advanced Solid Tumor Cancer
Immunolight LLC
 December 8 2021 Phase 1

References
  • https://pubmed.ncbi.nlm.nih.gov/11353760/
  • https://pubmed.ncbi.nlm.nih.gov/7945434/
  • https://pubmed.ncbi.nlm.nih.gov/24381860/
  • https://pubmed.ncbi.nlm.nih.gov/12392107/
  • https://pubmed.ncbi.nlm.nih.gov/21979070/
  • https://pubmed.ncbi.nlm.nih.gov/24859605/

Chemical Information

Molecular Weight 216.19 Formula

C12H8O4
CAS No. 298-81-7 SDF Download SDF
Synonyms Xanthotoxin, NCI-C55903
Smiles COC1=C2C(=CC3=C1OC=C3)C=CC(=O)O2

Storage and Stability

Storage (From the date of receipt)

In vitro
Batch:

DMSO : 43 mg/mL ( (198.89 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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