Idoxifene (CB7432)
(Synonyms: 艾多昔芬; CB7432) 目录号 : GC33402
Idoxifene (CB7432) (CB7432) 是一种新型的组织特异性选择性雌激素受体调节剂 (SERM)。
Cas No.:116057-75-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Idoxifene (CB7432) is a novel tissue-specific selective estrogen receptor modulator (SERM).
Idoxifene possesses the protective roles in vascular smooth muscle cells by its blunting the angiotensin II-induced production of reactive oxygen species (ROS). Idoxifene evidently suppresses HSC activation, inhibits culture-activated HSC proliferation in a dose-dependent manner, and induces culture-activated HSC apoptosis in a time-dependent manner[1]. Idoxifene acts in bone as an estrogen agonist for osteoblasts, and shows negligible agonist activity in human endometrial cells. Idoxifene and E2 protect hepatocytes from inflammatory cell injury by inhibiting activation of the NF-κB proinflammatory transcription factor[2].
Animals receive daily intraperitoneal injections of Estradiol (0.5 mg/kg) and an oral gavage of Idoxifene (0.02, 0.1, and 0.5 mg/kg) for 3 days after Dimethylnitrosamine (DMN) treatment. The blood levels of LDH and Estradiol (E2) and histological grades (scores 0 to 5) of liver zone 3 necrosis are evaluated. Idoxifene at doses of over 0.1 mg/kg significantly reduces the hepatic levels of collagen and MDA in the DMN model in a dose-dependent manner. Although Idoxifene and E2 are administered by different routes, i.e., by oral ingestion and intraperitoneal injection, respectively, the antifibrotic effect of a dose of 0.5 mg/kg of Idoxifene is somewhat greater than that of the same dose of E2[2].
[1]. Zhou YJ, et al. Inhibitory effects of idoxifene on hepatic fibrosis in rats. Acta Pharmacol Sin. 2005 May;26(5):581-6. [2]. Lu G, et al. Antioxidant and antiapoptotic activities of idoxifene and estradiol in hepatic fibrosis in rats. Life Sci. 2004 Jan 2;74(7):897-907.
Cell experiment: | DNA synthesis in cultured HSCs is measured using a Cell Proliferation Biotrack ELISA system. HSCs are cultured in DMEM supplemented with 10% FBS in 96-well plate for 4 d. In the period, the medium is replaced every other day. After 4 d, the culture medium is removed and the same medium with or without 1, 10, or 100 nM of Idoxifene is added to the cells respectively. After the cells are cultured for an additional 24 h, bromodeoxyuridine (BrdU) is added into each well at a final concentration of 10 μM and the cells are incubated with BrdU for 24 h. The incorporated BrdU is detected[1]. |
Animal experiment: | Rats[2]Adult male Wistar rats weighing about 200 g are used for the DMN model of hepatic fibrosis. The animals (n=6 in each group), which comprise groups 2 through 6 are administered a single intraperitoneal injection of 40 mg/kg DMN, diluted with saline. The controls in group 1 (n=6) receive a single dose of saline. The rats in groups 4, 5, and 6 receive daily oral gavage of Idoxifene, in a dosing vehicle (1% methylcellulose) of 10 mL/kg at a dose of 0.02, 0.1, and 0.5 mg/kg/day, respectively, for 14 days after a single injection of DMN. Idoxifene is dissolved in vehicle at a dose of 10 mg/mL as a stock solution. The animals in group 3 receive intraperitoneal injections of Estradiol valerate in olive oil at a dose of 0.5 mg/kg/day, for 14 days after the DMN injection. The animals in group 2 receive vehicle only. Animals are anesthetized with 40 mg/kg sodium pentobarbital either 0, 3, 9, or 14 days after DMN injection, and sacrificed. Blood samples are drawn from the inferior vena cava for analyses of serum levels of E2 and lactate dehydrogenase (LDH), a biomarker for necrosis, and liver tissue specimens are taken for light microscopy and immunohistochemistry. |
References: [1]. Zhou YJ, et al. Inhibitory effects of idoxifene on hepatic fibrosis in rats. Acta Pharmacol Sin. 2005 May;26(5):581-6. | |
| Cas No. | 116057-75-1 | SDF | |
| 别名 | 艾多昔芬; CB7432 | ||
| Canonical SMILES | CC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCN3CCCC3)C=C2)\C4=CC=C(I)C=C4 | ||
| 分子式 | C28H30INO | 分子量 | 523.45 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.9104 mL | 9.552 mL | 19.104 mL |
| 5 mM | 0.3821 mL | 1.9104 mL | 3.8208 mL |
| 10 mM | 0.191 mL | 0.9552 mL | 1.9104 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet