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Product Description
– Raloxifene 6-glucuronide-d4 (lithium) is deuterium labeled Raloxifene 6-glucuronide. Raloxifene 6-glucuronide is a primary metabolite of Raloxifene. Raloxifene 6-glucuronide is mediated mostly by UGT1A1 and UGT1A8. Raloxifene 6-glucuronide binds to estrogen receptor with an IC50 of 290 μM. Raloxifene is a selective and nonsteroidal estrogen receptor modulator. Raloxifene activates TGFβ3 promoter as a full agonist at nanomolar concentrations, and inhibits the estrogen response element-containing vitellogenin promoter expression[1][2][3].
Web ID
– HY-135581S1
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)SC5=CC(O[C@@H]6O[C@@H]([C@H]([C@@H]([C@H]6O)O)O)C(O[Li])=O)=CC=C53
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
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