Arzoxifene hydrochloride (Synonyms: LY353381 hydrochloride; SERM III hydrochloride)
目录号: PL03475 纯度: ≥98%
CAS No. :182133-27-3
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中文名称
Arzoxifene hydrochloride
中文别名
阿佐昔芬盐酸盐
英文名称
Arzoxifene hydrochloride
英文别名
Benzo[b]thiophene-6-ol,2-(4-methoxyphenyl)-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]-, hydrochloride(1:1);2-(4-methoxyphenyl)-3-[4-(2-piperidin-1-ylethoxy)phenoxy]-1-benzothiophen-6-ol,hydrochloride;Benzo[b]thiophene-6-ol,2-(4-methoxyphenyl)-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]-, hydrochlor...;Arzoxifene HCl;Arzoxifene hydrochloride;SERM 3;LY 353381 HCl;Ly 353381;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
Cas No.
182133-27-3
分子式
C28H29NO4S.HCl
分子量
512.06
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Arzoxifene (LY353381) 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。
生物活性
Arzoxifene (LY353381) hydrocloride is a selective estrogen receptor modulator that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol.
性状
Solid
IC50 & Target[1][2]
Estrogen receptor
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Suh N, et al. Arzoxifene, a new selective estrogen receptor modulator for chemoprevention of experimental breast cancer. Cancer Res. 2001 Dec 1;61(23):8412-5.
溶解度数据
In Vitro: DMSO : 25 mg/mL (48.82 mM; ultrasonic and warming and heat to 60°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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