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Product Description
– 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-135582
Shipping
– Room temperature
Applications
– Metabolism-protein/nucleotide metabolism
Molecular Formula
– C34H35NO10S
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.
CAS Number
– 182507-22-8
Molecular Weight
– 649.71
SMILES
– O[C@H]([C@H]([C@@H]([C@@H](C(O)=O)O1)O)O)[C@@H]1OC2=CC=C(C3=C(C(C4=CC=C(OCCN5CCCCC5)C=C4)=O)C6=CC=C(O)C=C6S3)C=C2
Clinical Information
– No Development Reported
Research Area
– Endocrinology
Solubility
– 10 mM in DMSO
Target
– Estrogen Receptor/ERR
Pathway
– Vitamin D Related/Nuclear Receptor
Product type
– Reference compound
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