CHF-4227

SKU: orb1905855

Description

CHF-4227 is a selective estrogen receptor modulator (SERM) characterized by its potent ability to lower serum cholesterol and LDL levels. It is a valuable research tool for investigating lipid metabolism and cardiovascular disease models in both cellular and animal studies.

Research Area

Metabolism Research

Key Properties

• CAS Number: 444643-64-5
• MW: 471.59
• Purity: 98.44% (May vary between batches)
• Formula: C₃₀H₃₃NO₄
• SMILES: C(C1=C(COC=2C1=CC=C(O)C2)C3=CC=C(OC)C=C3)C4=CC=C(OCCN5CCCCC5)C=C4
• Target: Estrogen Receptor/ERR
• Solubility: DMSO:7.5 mg/mL (15.9 mM)

Bioactivity

• Target IC50:
  ERα (human):0.017 nM (Ki)|ERβ (human):0.099 nM (Ki)
• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CHF 4227, Chf 4227, CHF4227, Chf4227, CHF-4227, estrogen receptor, EstrogenReceptor, Estrogen Receptor, ERR

Compound Identifiers

PubChem CID

9912639