444643-64-5
444643-64-5 structure
- Name: 3-(4-methoxyphenyl)-4-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]-2H-chromen-7-ol
- Chemical Name: 3-(4-methoxyphenyl)-4-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]-2H-chromen-7-ol
- CAS Number: 444643-64-5
- Molecular Formula: C30H33NO4
- Molecular Weight: 471.58700
- Create Date: 2017-07-20 21:44:30
- Modify Date: 2024-01-02 11:53:28
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CHF-4227 is a novel, potent and selective estrogen receptor modulator that reduces cholesterol and LDL cholesterol concentrations.
| Name | 3-(4-methoxyphenyl)-4-[[4-(2-piperidin-1-ylethoxy)phenyl]methyl]-2H-chromen-7-ol |
|---|---|
| Synonyms |
BIDD:ER0112
CHF 4227 2H-1-Benzopyran-7-ol,3-(4-methoxyphenyl)-4-((4-(2-(1-piperidinyl)ethoxy)phenyl)methyl) |
| 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] |
| References | 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. |
| Molecular Formula | C30H33NO4 |
|---|---|
| Molecular Weight | 471.58700 |
| Exact Mass | 471.24100 |
| PSA | 51.16000 |
| LogP | 5.74930 |