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Product Description
– Raloxifene 4′-glucuronide-d4 (lithium) is deuterium 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. [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].
Web ID
– HY-135582S1
Shipping
– Room temperature
Applications
– Metabolism-protein/nucleotide metabolism
Molecular Formula
– C34H30D4LiNO10S
References
– [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;53(2):211-216.
Molecular Weight
– 659.67
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[Li])=O)SC6=CC(O)=CC=C63
Clinical Information
– No Development Reported
Research Area
– Endocrinology
Solubility
– 10 mM in DMSO
Target
– Estrogen Receptor/ERR;Isotope-Labeled Compounds
Pathway
– Others;Vitamin D Related/Nuclear Receptor
Product type
– Isotope-Labeled Compounds
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
