CHF 4227 free baseCHF 4227 free base
MedChemExpress (MCE)
HY-107045
444643-64-5
Please store the product under the recommended conditions in the Certificate of Analysis.
Room temperature in continental US
may vary elsewhere.
CHF 4227 free base is an orally active and selective estrogen receptor modulator (SERM) with high affinity to the human estrogen receptor-α and -β (Ki values of 0.017 nM and 0.099 nM, respectively).
In immature rats, oral administration of CHF 4227 free base for 3 days inhibited the uterotrophic action of Ethinylestradiol (EE2) (HY-B0216) (ED50DMBA (HY-W011845)-induced mammary tumors, the incidence being reduced from 87.5 to 26.3% 6 months after DMBA administration[1]. In ovariectomized (OVX) rats treated orally for 4 weeks, CHF 4227 free basecompletely inhibits OVX effects on bone density (ED50[1]. CHF 4227 free base reduces serum cholesterol (ED50[1].
hERα 0.017 nM (Ki) hERβ 0.099 nM (Ki)
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[1]. Elisabetta Galbiati, et al. Pharmacological actions of a novel, potent, tissue-selective benzopyran estrogen. J Pharmacol Exp Ther. 2002 Oct
303(1):196-203. [Content Brief]
[2]. Maurizio Civelli, et al. Single and multiple ascending dose studies of a novel tissue-selective oestrogen receptor modulator, CHF 4227, in healthy postmenopausal women. Br J Clin Pharmacol. 2007 Sep
64(3):304-16. [Content Brief]