Raloxifene 4'-glucuronide
Based on 1 Customer Validation
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. . 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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 98.19%
- CAS. Nr.: 182507-22-8
- Formel: C34H35NO10S
- Molecular Weight:649.71
-
Speicherung:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
IC50: 370 μM (Estrogen receptor)[2]
Expressed UGT1A8 catalyzes Raloxifene 4'-glucuronide with an apparent Km of 59 μM and a Vmax of 2.0 nmol/min/mg. Based on rates of Raloxifene glucuronidation and known extrahepatic expression, UGT1A8 and 1A10 appear to be primary contributors to Raloxifene glucuronidation in human jejunum microsomes. For human liver microsomes, the variability of Raloxifene 4'-glucuronide formation is 4-fold. Treatment of expressed UGTs with alamethicin results in minor increases in enzyme activity, whereas in human intestinal microsomes, maximal increases of 9-fold for the Raloxifene 4'-glucuronide are observed. Intrinsic clearance values in intestinal microsomes are 95 μl/min/mg for the Raloxifene 4'-glucuronide[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS. Nr. 182507-22-8
-
Appearance Solid
-
Molecular Weight 649.71
-
Formel C34H35NO10S
-
Color Light yellow to yellow
-
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
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Reinheit & Dokumentation
-
Data Sheet (274 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
Verweise
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Raloxifene 4'-glucuronide Related Classifications
HY-135582 Related Classifications
Powered by Bioz