Molecular structure of Raloxifene 6-Glucuronide, CAS Number: 174264-50-7
Raloxifene 6-Glucuronide (CAS 174264-50-7)
See product citations (1)
Alternate Names:
2-(4-Hydroxyphenyl)-3-[4-[2-(1-piperidinyl)ethoxybenzoyl]benzo[b]thien-6-yl]-?-D-glucopyranosiduronic Acid
Application:
Raloxifene 6-Glucuronide is A metabolite of Raloxifene, a nonsteroidal estrogen receptor mixed agonist/antagonist.
CAS Number:
174264-50-7
Molecular Weight:
649.71
Molecular Formula:
C34H35NO10S
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
QUICK LINKS
Ordering Information
Product Citations
Description
Technical Information
Safety Information
SDS & Certificate of Analysis
Raloxifene 6-glucuronide, a byproduct of raloxifene, which is a selective estrogen receptor modulator, is synthesized through the UDP-glucuronosyltransferase (UGT) isoforms UGT1A1 and UGT1A8. It possesses a binding affinity to the estrogen receptor with an IC50 value of 290 nM. In contrast to raloxifene, raloxifene 6-glucuronide does not exert inhibitory effects on the voltage-gated potassium channel Kv4.3.3.
Raloxifene 6-Glucuronide (CAS 174264-50-7) References
- Development and validation of a liquid chromatography-tandem mass spectrometry assay for determination of raloxifene and its metabolites in human plasma. | Trontelj, J., et al. 2007. J Chromatogr B Analyt Technol Biomed Life Sci. 855: 220-7. PMID: 17537683
- Pharmacokinetics of raloxifene in male Wistar-Hannover rats: influence of complexation with hydroxybutenyl-beta-cyclodextrin. | Wempe, MF., et al. 2008. Int J Pharm. 346: 25-37. PMID: 17644287
- Effects of UGT1A1*28 polymorphism on raloxifene pharmacokinetics and pharmacodynamics. | Trontelj, J., et al. 2009. Br J Clin Pharmacol. 67: 437-44. PMID: 19371317
- The role of pH in the glucuronidation of raloxifene, mycophenolic acid and ezetimibe. | Chang, JH., et al. 2009. Mol Pharm. 6: 1216-27. PMID: 19449843
- In vitro metabolism, permeability, and efflux of bazedoxifene in humans. | Shen, L., et al. 2010. Drug Metab Dispos. 38: 1471-9. PMID: 20516255
- A novel method for the determination of the site of glucuronidation by ion mobility spectrometry-mass spectrometry. | Shimizu, A., et al. 2012. Drug Metab Dispos. 40: 1456-9. PMID: 22611068
- Regulation of UDP-glucuronosyltransferase 1A1 expression and activity by microRNA 491-3p. | Dluzen, DF., et al. 2014. J Pharmacol Exp Ther. 348: 465-77. PMID: 24399855
- Quantitative assessment of intestinal first-pass metabolism of oral drugs using portal-vein cannulated rats. | Matsuda, Y., et al. 2015. Pharm Res. 32: 604-16. PMID: 25163980
- Key determinants of the circulatory exposure of organic anions: differences in hepatic uptake between multidrug resistance-associated protein 2 (Mrp2)-deficient rats and wild-type rats. | Kosaka, K., et al. 2015. Xenobiotica. 45: 556-62. PMID: 25539456
- Milk Thistle Constituents Inhibit Raloxifene Intestinal Glucuronidation: A Potential Clinically Relevant Natural Product-Drug Interaction. | Gufford, BT., et al. 2015. Drug Metab Dispos. 43: 1353-9. PMID: 26070840
- Development and validation of ultra-high-performance liquid chromatography-mass spectrometry method for the determination of raloxifene and its phase II metabolites in plasma: Application to pharmacokinetic studies in rats. | Du, T., et al. 2020. J Sep Sci. 43: 4414-4423. PMID: 33119204
- Hepatoenteric recycling is a new disposition mechanism for orally administered phenolic drugs and phytochemicals in rats. | Tu, Y., et al. 2021. Elife. 10: PMID: 34196607
- Age-and Region-Dependent Disposition of Raloxifene in Rats. | Du, T., et al. 2021. Pharm Res. 38: 1357-1367. PMID: 34322833
- Evaluation of the major metabolites of raloxifene as modulators of tissue selectivity. | Dodge, JA., et al. 1997. J Steroid Biochem Mol Biol. 61: 97-106. PMID: 9328215
Inhibitor of:
Estrogen Receptor.Activator of:
Estrogen Receptor.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Raloxifene 6-Glucuronide, 1 mg | sc-222243 | 1 mg | $448.00 | |||
Raloxifene 6-Glucuronide, 1 mg | sc-222243-CW | 1 mg | $562.00 | |||
Raloxifene 6-Glucuronide, 5 mg | sc-222243A | 5 mg | $1977.00 | |||
Raloxifene 6-Glucuronide, 5 mg | sc-222243A-CW | 5 mg | $2081.00 |