Raloxifene 4'-glucuronide-d4

• UNSPSC Description:

  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].

• Target Antigen:

  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 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

• Clinical Information:

  No Development Reported

• CAS Number:

  1279033-52-1