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CHF-4227

Catalog No. T68042 CAS 444643-64-5

Synonyms: Chf4227, Chf 4227

CHF-4227 is a novel, potent and selective estrogen receptor modulator that reduces cholesterol and LDL cholesterol concentrations.

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CHF-4227, CAS 444643-64-5

Pack Size	Availability	Price/USD
1 mg	In stock	$ 195.00
5 mg	In stock	$ 483.00
10 mg	In stock	$ 692.00
25 mg	In stock	$ 1,080.00
50 mg	In stock	$ 1,490.00
100 mg	In stock	$ 1,970.00
500 mg	In stock	$ 3,930.00

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Purity: 98.44%

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Description

CHF-4227 is a novel, potent and selective estrogen receptor modulator that reduces cholesterol and LDL cholesterol concentrations.

In vivo

We evaluated the tolerability, adverse events profile, pharmacokinetics, and pharmacodynamics of CHF-4227, a new selective estrogen receptor modulator (SERM), in healthy postmenopausal women. METHODS: Two phase I studies were conducted according to a double-blind, placebo-controlled design. Subjects were randomized to receive six single (5-400 mg) or five multiple oral doses of CHF-4227 for 28 days (5-100 mg). RESULTS: No vaginal bleeding and no changes in either endometrial thickness or the placenta protein 14 markers were found after 4 weeks of treatment. The compound did not induce negative effects on the fibrinolytic system. After 28 days of treatment, CHF-4227 decreased both total and LDL cholesterol concentrations (maximum decreases from baseline of 17.4% (95% CI 7.0, 27.7) and 27.6% (95% CI 9.0, 46.3), respectively). Decreases in both serum and urinary type-I C-terminal collagen telopeptide were also observed producing maximum changes of 40.6% (95% CI 29.5, 51.7), and 41.7% (95% CI 20.3, 56.8), respectively. CHF-4227 (5 and 10 mg) induced near-maximal estrogen-like effects on bone markers and serum lipids without causing hot flushes. The pharmacokinetics of CHF-4227 were characterized by slow absorption, a long elimination half-life (31-42 h after single administration), and dose linearity with respect to C(max) and AUC up to 100 mg. CONCLUSIONS: CHF-4227 is a well-tolerated SERM when administered once daily for 28 days. It is potentially active on bone resorption and serum lipids, without affecting the endometrium and without worsening hot flushes. CHF-4227 is a promising agent for the treatment of several conditions in postmenopausal women.[1]

Synonyms	Chf4227, Chf 4227
Molecular Weight	471.59
Formula	C30H33NO4
CAS No.	444643-64-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Civelli M, 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.

Related compound libraries

This product is contained In the following compound libraries：

Bioactive Compound Library Bioactive Compounds Library Max

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α-Zearalenol Etonogestrel Iriflophenone Bazedoxifene hydrochloride Estrogen receptor antagonist 8 FLTX1 14-3-3σ/ERα stabilizer-1 DY131

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Keywords

CHF-4227 444643-64-5 Endocrinology/Hormones Estrogen Receptor/ERR CHF 4227 CHF4227 Chf4227 Chf 4227 inhibitor inhibit

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