| Name | CHF-4227 |
| 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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 7.5 mg/mL (15.9 mM), Sonication is recommended.
|
| Keywords | EstrogenReceptor | Estrogen Receptor | ERR | CHF-4227 | CHF4227 | CHF 4227 |
| Inhibitors Related | Tamoxifen | Estradiol | 2-Ethylhexyl trans-4-methoxycinnamate | Diisopropyl phthalate | Estradiol benzoate | Bisphenol B | Mequinol | Phthalic acid | Chlorothalonil | Ethisterone | Tamoxifen Citrate | Cholesterol |
| Related Compound Libraries | Nuclear Receptor Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Breast Cancer Compound Library | Anti-Ovarian Cancer Compound Library | Endocrinology-Hormone Compound Library | Bioactive Compounds Library Max |
United States
