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N-Desmethyltamoxifen 

Cat. No. M29903
N-Desmethyltamoxifen  Structure
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Quality Control & Documentation
Biological Activity

N-Desmethyltamoxifen is the major metabolite of tamoxifen in humans. N-Desmethyltamoxifen, a poor antiestrogen, is a ten-fold more potent protein kinase C (PKC) inhibitor than Tamoxifen. N-Desmethyltamoxifen is also a potent regulator of ceramide metabolism in human AML cells, limiting ceramide glycosylation, hydrolysis, and sphingosine phosphorylation.

Chemical Information
Molecular Weight 357.49
Formula C25H27NO
CAS Number 31750-48-8
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yung-Yi Cheng, et al. Biomed Pharmacother. Dose-dependent effects of Hedyotis diffusa extract on the pharmacokinetics of tamoxifen, 4-hydroxytamoxifen, and N-desmethyltamoxifen

[2] A B Sanchez-Spitman, et al. Expert Rev Clin Pharmacol. Clinical pharmacokinetics and pharmacogenetics of tamoxifen and endoxifen

[3] Geniey Yang, et al. Pharmacol Ther. Toxicity and adverse effects of Tamoxifen and other anti-estrogen drugs

[4] Jennifer Gjerde, et al. Breast Cancer Res Treat. Tissue distribution of 4-hydroxy-N-desmethyltamoxifen and tamoxifen-N-oxide

[5] Tanios S Bekaii-Saab, et al. Biopharm Drug Dispos. Interactions of tamoxifen, N-desmethyltamoxifen and 4-hydroxytamoxifen with P-glycoprotein and CYP3A

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Keywords: N-Desmethyltamoxifen  supplier, PKC, inhibitors, activators


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