Product Details
| Product Name:
CHF-4227 |
CAS No.:
444643-64-5 |
| Purity:
98.44% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| 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 | Shipping with blue ice. |
| Solubility Information | DMSO : 7.5 mg/mL (15.9 mM), Sonication is recommended.
|
| Keywords | CHF 4227 | CHF4227 | CHF-4227 |
| Inhibitors Related | Kaempferol | Tamoxifen | Estradiol | Estradiol benzoate | ARV-471 | Genistin | Cholesterol | Estriol | Chrysin | Ethisterone | Cyclofenil | Estrone |
| Related Compound Libraries | Bioactive Compound Library | Bioactive Compounds Library Max |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$3100.00/100mg |
VIP1Y
|
TargetMol Chemicals Inc.
|
2024-10-28 |
United States