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182133-27-3

中文名称 阿佐昔芬盐酸盐
英文名称 ARZOXIFENE HCL
CAS 182133-27-3
分子式 C28H29NO4S.ClH
分子量 512.067
MOL 文件 182133-27-3.mol
182133-27-3 结构式 182133-27-3 结构式

基本信息

中文别名
阿佐昔芬盐酸盐
英文别名
Serm 3
Ly 353381
Ly 353381 HCl
ARZOXIFENE HCL
Arzoxifene hydrochloride
NHSNLUIMAQQXGR-UHFFFAOYSA-N
2-(p-Methoxyphenyl)-3-(p-(2-(1-piperidinyl)ethoxy)phenoxy)benzo(B)thiophene-6-ol hydrochloride
2-(4-Methoxyphenyl)-3-(4-(2-(1-piperidinyl)ethoxy)phenoxy)benzo(B)thiophene-6-ol hydrochloride
Benzo(B)thiophene-6-ol, 2-(4-methoxyphenyl)-3-(4-(2-(1-piperidinyl)ethoxy)phenoxy)-, hydrochloride

物理化学性质

熔点156-160°
形态Solid
颜色Off-white to light yellow

常见问题列表

生物活性
Arzoxifene hydrocloride是一种选择性的雌激素受体 (estrogen receptor) 调节剂,它是乳腺和子宫组织中有效的雌激素拮抗剂,同时作为维持骨密度和降低血清胆固醇的雌激素激动剂。
靶点

Estrogen receptor

体外研究

Arzoxifene inhibits cell growth as effectively as the antiestrogen tamoxifen. Northern analysis reveals that arzoxifene exerts a statistically significant inhibition of pS2 and progesterone receptor B mRNA expression. Significant agonistic effect is observed on the antitrypsin mRNA expression. In contrast to estradiol and tamoxifen, arzoxifene does not upregulate cathepsin D mRNA and protein expression.

体内研究

Arzoxifene prevents the ovariectomy-induced increase in body weight and serum cholesterol levels of treated rats and lowers them to below sham levels in a dose dependent manner, with maximum efficacy similar to estrogen or raloxifene. Arzoxifene (LY353381.HCl) prevents loss of bone due to ovariectomy with an ED 50 of about 0.01 mg/kg with maximal efficacy observed at 0.1-1 mg/kg/day. Arzoxifene (LY353381.HCl) antagonizes the estrogen-induced elevation in uterine weight down to vehicle-dosed control levels with ED 50 of 0.03 mg/kg/day.

"182133-27-3" 相关产品信息
628-13-7 593-81-7 590-46-5 593-51-1