Raloxifene-4'-glucuronide_d4
- Product Name
- Raloxifene-4'-glucuronide_d4
- CAS No.
- 1279033-52-1
- Chemical Name
- Raloxifene-4'-glucuronide_d4
- Synonyms
- Raloxifene-4'-glucuronide_d4;[2H4]-4'-Raloxifene glucuronide;Raloxifene 4 Glucuronide D4Q: What is Raloxifene 4 Glucuronide D4 Q: What is the CAS Number of Raloxifene 4 Glucuronide D4 Q: What is the storage condition of Raloxifene 4 Glucuronide D4 Q: What are the applications of Raloxifene 4 Glucuronide D4
- CBNumber
- CB94849217
- Molecular Formula
- C34H35NO10S
- Formula Weight
- 649.71
- MOL File
- 1279033-52-1.mol
Raloxifene-4'-glucuronide_d4 Chemical Properties,Usage,Production
Uses
Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide (HY-135582). Raloxifene 4'-glucuronide is a primary metabolite of Raloxifene. Raloxifene 4'-glucuronide formation is mediated mostly by UGT1A10 and UGT1A8. Raloxifene 4'-glucuronide binds to estrogen receptor with an IC50 of 370 μM. [1][2]. Raloxifene is a selective estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[3].
References
[1] Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. DOI:10.1177/1060028018797110
[2] Izgelov D, et al. The Effect of Piperine Pro-Nano Lipospheres on Direct Intestinal Phase II Metabolism: The Raloxifene Paradigm of Enhanced Oral Bioavailability. Mol Pharm. 2018 Apr 2;15(4):1548-1555. DOI:10.1021/acs.molpharmaceut.7b01090
[3] Kemp DC, et al. Characterization of raloxifene glucuronidation in vitro: contribution of intestinal metabolism to presystemic clearance. Drug Metab Dispos. 2002 Jun;30(6):694-700. DOI:10.1124/dmd.30.6.694
[4] Yang NN, et al. Estrogen and raloxifene stimulate transforming growth factor-beta 3 gene expression in rat bone: a potential mechanism for estrogen- or raloxifene-mediated bone maintenance. Endocrinology. 1996 May;137(5):2075-84. DOI:10.1210/endo.137.5.8612550
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