Molecular structure of Desacetyl diltiazem, CAS Number: 42399-40-6
Desacetyl diltiazem (CAS 42399-40-6)
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Alternate Names:
(2S-cis)-5-[(Dimethylamino)ethyl]-2,3-dihydro-3-hydroxy-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one; Deacetyl-d-diltiazem
Application:
Desacetyl diltiazem is a metabolite of Diltiazem
CAS Number:
42399-40-6
Purity:
≥97%
Molecular Weight:
372.48
Molecular Formula:
C20H24N2O3S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Desacetyl Diltiazem is a metabolite of Diltiazem (sc-204726), a calcium channel antagonist which also inhibits the enzyme CYP3A4. Studies indicate that Diltiazem is metabolized into its major metabolites such as Desacetyl Diltiazem in plasma. Desacetyl Diltiazem weakly inhibits nucleoside triphosphate diphosphohydrolases, which is believed to follow a mechanism that reduces the concentration of calcium required by the enzymes catalytic site. Furthermore, studies using gas chromatography determined that Desacetyl Diltiazem can be seperated from its parent molecule, Diltiazem, using a nitrogen detector, which allows for the determination of each molecule in plasma.
Desacetyl diltiazem (CAS 42399-40-6) References
- Extensive metabolism of diltiazem and P-glycoprotein-mediated efflux of desacetyl-diltiazem (M1) by rat jejunum in vitro. | Molden, E., et al. 2000. Drug Metab Dispos. 28: 107-9. PMID: 10640504
- Ca(2+)-channel blockers and nucleoside triphosphate diphosphohydrolase (NTPDase) influence of diltiazem, nifedipine, and verapamil. | Gendron, FP., et al. 2000. Biochem Pharmacol. 60: 1959-65. PMID: 11108813
- Desacetyl-diltiazem displays severalfold higher affinity to CYP2D6 compared with CYP3A4. | Molden, E., et al. 2002. Drug Metab Dispos. 30: 1-3. PMID: 11744603
- Pharmacokinetics of diltiazem and its metabolites in relation to CYP2D6 genotype. | Molden, E., et al. 2002. Clin Pharmacol Ther. 72: 333-42. PMID: 12235455
- Coadministration of grapefruit juice increases systemic exposure of diltiazem in healthy volunteers. | Christensen, H., et al. 2002. Eur J Clin Pharmacol. 58: 515-20. PMID: 12451428
- Effects of CYP3A5 and CYP2D6 genetic polymorphism on the pharmacokinetics of diltiazem and its metabolites in Chinese subjects. | Zheng, T., et al. 2013. Pharmazie. 68: 257-60. PMID: 23700791
- Calcium channel receptor binding studies for diltiazem and its major metabolites: functional correlation to inhibition of portal vein myogenic activity. | Schoemaker, H., et al. 1987. J Cardiovasc Pharmacol. 9: 173-80. PMID: 2435995
- Bioconcentration, metabolism and half-life time of the human therapeutic drug diltiazem in rainbow trout Oncorhynchus mykiss. | Steinbach, C., et al. 2016. Chemosphere. 144: 154-9. PMID: 26356646
- Simple sensitive and specific gas chromatographic method for the quantification of diltiazem human body fluids. | Rovel, V., et al. 1977. J Chromatogr. 138: 391-8. PMID: 893601
- Pharmacokinetic interactions of moricizine and diltiazem in healthy volunteers. | Shum, L., et al. 1996. J Clin Pharmacol. 36: 1161-8. PMID: 9013374
Inhibitor of:
Calcium Channel Protein, and CYP3A4.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Desacetyl diltiazem, 10 mg | sc-207527 | 10 mg | $330.00 |