Obacunone (AI3-37934)

For research use only. Not for use in humans.

目录号:S3784 别名: CCRIS 8657 中文名称:黄柏酮

Obacunone (AI3-37934) Chemical Structure

CAS No. 751-03-1

Obacunone (AI3-37934, CCRIS 8657), a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2.

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产品安全说明书

Aromatase抑制剂选择性比较

生物活性

产品描述 Obacunone (AI3-37934, CCRIS 8657), a natural compound present in citrus fruits, has been demonstrated for various biological activities including anti-cancer and anti-inflammatory properties. It significantly inhibits aromatase activity in an in vitro enzyme assay with an IC50 value of 28.04 μM; also a novel activator of Nrf2.
靶点
Nrf2 [2]
()
Aromatase [1]
(Cell-free assay)
28.4 μM
体外研究

Obacunone is strongly inhibited MCF-7 cell proliferation without affecting non-malignant breast cells. Treatment with obacunone increases apoptosis by upregulating expression of the pro-apoptotic protein Bax and down-regulating the anti-apoptotic protein Bcl2, as well as inducing G1 cell cycle arrest. In addition, obacunone significantly inhibits aromatase activity in an in vitro enzyme assay. Exposure of MCF-7 breast cancer cells to obacunone down-regulates expression of inflammatory molecules including nuclear factor-kappa B (NF-kB) and cyclooxygenase-2 (COX-2). Obacunone inhibits COX-2 and NF-kB by activation of the p38 mitogen-activated protein kinase (MAPK). Obacunone is reported as a glutathione S-transferase (GST) enzyme inducer as well as a neuroprotective agent acting by induction of heme oxygenase-1 via the p38 MAPK pathway[1]. Obacunone is a novel activator of Nrf2 by decreasing Nrf2 ubiquitination and increasing its stability. It can effectively protect cells from oxidative stress by activating the Nrf2 pathway. Obacunone could induce the expression of the ARE-dependent luciferase gene in a dose-dependent manner[2].

体内研究 The systemic administration of obacunone strongly inhibits bleomycin-induced lung fibrosis in mice. Obacunone can inhibit cancer proliferation and has some therapeutic effects on cardiovascular diseases[2]. In vitro and animal studies suggests that obacunone and a few other limonoids may have potential anticarcinogenic activity against certain types of cancers. A 500-mg/kg (of body weight) dose of obacunone per day is well tolerated and does not have adverse effects in rats, indicating a low toxicity[3].

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:[1]
- 合并
  • Cell lines: Human breast cancer (MCF-7) and non-malignant immortalized breast epithelial (MCF-12F) cell lines
  • Concentrations: 12.5, 25, 50,100 and 200 μM
  • Incubation Time: 24, 48, and 72 h
  • Method: The MCF-7 cells are cultured in DMEM medium containing 10% (v/v) fetal bovine serum, 200 U/mL penicillin G, and 200 mg/mL streptomycin. The MCF-12F cells are cultured in a 1:1 mixture of DMEM and Ham's F12 medium with 20 ng/mL of epidermal growth factor (EGF),100 ng/mL cholera toxin, 0.01 mg/mL insulin, 500 ng/mL hydrocortisone, and 5% (v/v) chelextreated horse serum, and then the cells are incubated at 37℃ with 5% CO2. To evaluate the anti-proliferate effects of obacunone, viability of the MCF-7 and MCF-12F cells are measured using the tetrazolium MTT reduction assay. The MCF-7 or MCF-12F cells (1×104/well) are seeded into a 96-well plate and allowed to adhere overnight. Cells are treated with different concentrations (12.5, 25, 50,100 and 200 μM) of either obacunone or OG and incubated for 24, 48, and 72 h. Tamoxifen, a well-known anti-estrogen drug used for breast cancer therapy, is used as a positive control. After the various time points, 10 ml of the MTT (5 mg/mL) reagent are added to each well and incubated for 2h at 37℃. After 2h incubation, the medium is removed and 200 ml of DMSO is added to dissolve the purple formazan. The absorbance is measured by an ELISA microplate reader at 570 nm.
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: Eight-week-old B6 mice
  • Dosages: 10 mg/kg
  • Administration: i.p.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 90 mg/mL (198.01 mM)

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 454.51
化学式

C26H30O7

CAS号 751-03-1
储存条件 粉状
溶于溶剂
别名 CCRIS 8657

动物体内配方计算器 (澄清溶液)

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
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Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

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Aromatase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID