Powder: -20°C for 3 years | In solvent: -80°C for 1 year
CHF-4227 是一种新型高效且具有选择性的雌激素受体调节剂,可降低胆固醇合低密度脂蛋白胆固醇浓度。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 1,300 | 现货 | ||
5 mg | ¥ 3,250 | 现货 | ||
10 mg | ¥ 4,750 | 现货 | ||
25 mg | ¥ 7,480 | 现货 | ||
50 mg | ¥ 9,870 | 现货 | ||
100 mg | ¥ 13,600 | 现货 | ||
500 mg | ¥ 27,300 | 现货 |
产品描述 | CHF-4227 is a novel, potent and selective estrogen receptor modulator that reduces cholesterol and LDL cholesterol concentrations. |
体内活性 | 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] |
别名 | Chf4227, Chf 4227 |
分子量 | 471.59 |
分子式 | C30H33NO4 |
CAS No. | 444643-64-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 7.5 mg/mL (15.9 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.1205 mL | 10.6024 mL | 21.2049 mL | 53.0122 mL |
5 mM | 0.4241 mL | 2.1205 mL | 4.241 mL | 10.6024 mL | |
10 mM | 0.212 mL | 1.0602 mL | 2.1205 mL | 5.3012 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
CHF-4227 444643-64-5 Endocrinology/Hormones Estrogen Receptor/ERR CHF 4227 CHF4227 Chf4227 Chf 4227 Inhibitor inhibitor inhibit