CHF-4227
CAS 444643-64-5 MFCD44643645
化学结构图
SMILES: COc1ccc(C2=C(Cc3ccc(OCCN4CCCCC4)cc3)c3ccc(O)cc3OC2)cc1
化学属性
| Mol. Weight | 471.59 |
|---|---|
| Appearance | Solid powder |
| Solubility | Soluble in DMSO, not in water |
别名和识别编码
| Chemical Name | CHF-4227 |
|---|---|
| Formula | C30H33NO4 |
| Synonym | CHF4227; CHF 4227; CHF-4227. |
| IUPAC Name | 3-(4-methoxyphenyl)-4-(4-(2-(piperidin-1-yl)ethoxy)benzyl)-2H-chromen-7-ol |
| InChIKey | ZUDXUNPSRMREOJ-UHFFFAOYSA-N |
| InChI | InChI=1S/C30H33NO4/c1-33-25-12-7-23(8-13-25)29-21-35-30-20-24(32)9-14-27(30)28(29)19-22-5-10-26(11-6-22)34-18-17-31-15-3-2-4-16-31/h5-14,20,32H,2-4,15-19,21H2,1H3 |
| Canonical SMILES | OC1=CC=C2C(CC3=CC=C(OCCN4CCCCC4)C=C3)=C(C5=CC=C(OC)C=C5)COC2=C1 |
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产品应用
- CHF-4227 is a novel potent and selective estrogen receptor modulator. CHF 4227 binds with high affinity to the human estrogen receptor-alpha and -beta (dissociation constant K(i) = 0.017 and 0.099 nM, respectively). CHF 4227 compares favorably in efficacy and potency with raloxifene in preventing bone loss and in antagonizing EE2 stimulation of the uterus. This profile along with the minimal uterine stimulation suggests a therapeutic advantage to CHF 4227 over EE2 or raloxifene for the treatment of postmenopausal women. 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.
