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Raloxifene 4'-glucuronide-d4

CAT: 0804-HY-135582SSize: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-135582SSize:1 Each
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Description
Raloxifene 4'-glucuronide-d4 is deuterated labeled Raloxifene 4'-glucuronide. 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.[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].
CAS Number
1279033-52-1
UNSPSC
12352005
Target
Estrogen Receptor/ERR; Isotope-Labeled Compounds
Type
Isotope-Labeled Compounds
Related Pathways
Others; Vitamin D Related/Nuclear Receptor
Applications
Metabolism-protein/nucleotide metabolism
Field of Research
Endocrinology
Solubility
10 mM in DMSO
Smiles
O=C(C1=CC=C(C=C1)OC([2H])([2H])C([2H])([2H])N2CCCCC2)C3=C(C4=CC=C(C=C4)O[C@@H]5O[C@@H]([C@H]([C@@H]([C@H]5O)O)O)C(O)=O)SC6=CC(O)=CC=C63
Molecular Formula
C34H31D4NO10S
Molecular Weight
653.73
References & Citations
[1]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.|[2]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.|[3]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.|[4]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported

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