Raloxifene 4'-glucuronide-d4, CAS 1279033-52-1

Product 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].

Applications: Metabolism-protein/nucleotide metabolism

Formula: C34H31D4NO10S

References: [1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216./[2]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./[3]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./[4]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: 1279033-52-1

Molecular Weight: 653.73

Research Area: Endocrinology

Solubility: 10 mM in DMSO

Target: Estrogen Receptor/ERR;Isotope-Labeled Compounds

• Artikelnummer: MEXHY-135582S-0
• Hersteller: MedChemExpress
• Hersteller Artikelnummer: HY-135582S-0
• Verpackungseinheit: Get quote
• Mengeneinheit: STK