Coumestrol
(Synonyms: 拟雌内酯) 目录号 : GC10002
A naturally-occurring phytoestrogen
Cas No.:479-13-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment: |
To determine dose-dependent effects of coumestrol, ES2 cells are treated with different concentrations (0, 1, 10, 20, 50 or 100 μM) of coumestrol[1]. Coumestrol is dissolved in DMSO to prepare a 3 mM stock. Breast cancer MCF-7 cells are treated with increasing concentrations of coumestrol for 24, 48 and 72 h. Then, 20 μL of MTT (5 mg/mL) is added each well and re-incubated for additional 3 h. Formazan blue crystals formed are dissolved in 100 μL of DMSO. Absorbance is read at 570 nm using ELISA plate reader[2]. |
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References: [1]. Lim W, et al. Coumestrol suppresses proliferation of ES2 human epithelial ovarian cancer cells. J Endocrinol. 2016 Mar;228(3):149-60. |
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Coumestrol is an antagonist of estrogen receptors with IC50 values of 11 nM and 2 nM for human ERα and human ERβ, respectively. Coumestrol is also a naturally occurring weak antagonist of the human pregnane X receptor with IC50 value of 12 μM [1][2][3].
Estrogen receptors (ERs) are receptors that are activated by the hormone estrogen (17β-estradiol). ERα and ERβ are nuclear estrogen receptors, which are members of the nuclear receptor family of intracellular receptors. Selective estrogen receptor modulators (SERMs) have the potential ability to antagonize the proliferative effects of estrogen on uterine and breast tissue while mimicking estrogen’s effects on the bone and cardiovascular system [1].
Coumestrol is an antagonist of estrogen receptors with IC50 values of 11 nM and 2 nM for human ERα and human ERβ, respectively. Coumestrol increased de novo synthesis of secreted complement C3 [2]. Coumestrol is also a naturally occurring weak antagonist of the human pregnane X receptor (PXR) with IC50 value of 12 μM. In transient transfection assays, coumestrol inhibited the agonist effects of SR12813 on human PXR activity. In primary human hepatocytes, coumestrol inhibited the effects of PXR agonists on the expression of the known PXR target genes, CYP3A4 and CYP2B6. Coumestrol is also a potential inverse agonist of the constitutive androstane receptor with EC50 value of 30 μM [3].
References:
[1]. Chen HY, Dykstra KD, Birzin ET, et al. Estrogen receptor ligands. Part 1: The discovery of flavanoids with subtype selectivity. Bioorg Med Chem Lett. 2004 Mar 22;14(6):1417-21.
[2]. Hopert AC, Beyer A, Frank K, et al. Characterization of estrogenicity of phytoestrogens in an endometrial-derived experimental model. Environ Health Perspect. 1998 Sep;106(9):581-6.
[3]. Wang H, Li H, Moore LB, et al. The phytoestrogen coumestrol is a naturally occurring antagonist of the human pregnane X receptor. Mol Endocrinol. 2008 Apr;22(4):838-57.
| Cas No. | 479-13-0 | SDF | |
| 别名 | 拟雌内酯 | ||
| 化学名 | 3,9-dihydroxy-6H-benzofuro[3,2-c][1]benzopyran-6-one | ||
| Canonical SMILES | O=C1OC2=C(C=CC(O)=C2)C3=C1C4=CC=C(O)C=C4O3 | ||
| 分子式 | C15H8O5 | 分子量 | 268.2 |
| 溶解度 | ≤25mg/ml 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7286 mL | 18.6428 mL | 37.2856 mL |
| 5 mM | 0.7457 mL | 3.7286 mL | 7.4571 mL |
| 10 mM | 0.3729 mL | 1.8643 mL | 3.7286 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。