Home Metabolism P450 (e.g. CYP17) inhibitor Methoxsalen For research use only.

Methoxsalen

Synonyms: Xanthotoxin, NCI-C55903

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; A CYP2A5/6 inhibitor.

Methoxsalen Chemical Structure

Methoxsalen Chemical Structure

CAS No. 298-81-7

Purity & Quality Control

Methoxsalen Related Products

Signaling Pathway

P450 (e.g. CYP17) Signaling Pathways

P450 (e.g. CYP17) Signaling Pathway

Biological Activity

Description 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; A CYP2A5/6 inhibitor.
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). Methoxsalen shows noncompetitive inhibition of nicotine metabolism, with an apparent Ki value of 0.1 μM in cDNA-expressing microsomes. [1] Methoxsalen 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). Methoxsalen 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. Methoxsalen also significantly reduces circulating estrogen levels in blood serum of oogenesis Balb/C mice. [3] Methoxsalen dose-dependently stimulates a sustained increase in short-circuit current in the mouse jejunum. Methoxsalen increases the open probability of the basolateral IK(Ca) channel of isolated crypts in the mouse jejunum. [4] Methoxsalen effectively reverses trimethyltin (TMT)-induced memory impairment on both Y-maze and passive avoidance tests in mice. Methoxsalen inhibits brain AchE activity. Methoxsalen 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

Chemical Information & Solubility

Molecular Weight 216.19 Formula

C12H8O4
CAS No. 298-81-7 SDF Download Methoxsalen SDF
Smiles COC1=C2C(=CC3=C1OC=C3)C=CC(=O)O2
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


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In vivo
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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.

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