CHF 4227 free base

CAS: 444643-64-5 F: C30H33NO4 W: 471.59

CHF 4227 free base is an orally active and selective estrogen receptor modulator (SERM) with high affinity to the human

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Bioactivity	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)[1][2].
In Vivo	在未成熟大鼠中，口服 CHF 4227 游离碱 3 天可抑制炔雌醇 (EE2) (HY-B0216) 的子宫增生作用 (ED50 = 0.016 mg/kg · 天)，而其无子宫增生活性。与其雌激素拮抗作用一致，CHF 4227 游离碱可显著阻止 DMBA (HY-W011845) 诱发的乳腺肿瘤的发展，DMBA 给药 6 个月后发病率从 87.5% 降至 26.3%[1]。在口服 4 周的卵巢切除 (OVX) 大鼠中，CHF 4227 游离碱可完全抑制 OVX 对骨密度 (ED50 = 0.003 mg/kg · 天) 和血清骨钙素水平的影响[1]。 CHF 4227 游离碱可降低血清胆固醇（ED50 = 0.007 mg/kg · 天），对子宫重量、子宫过氧化物酶活性和子宫内膜上皮厚度几乎没有刺激作用[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.
CAS	444643-64-5
Formula	C30H33NO4
Molar Mass	471.59
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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. [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.

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