Ospemifene
Based on 3 publication(s) in Google Scholar
Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with Ki values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer.
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- 純度: 99.84%
- CAS 番号: 128607-22-7
- 分子式: C24H23ClO2
- 分子量:378.89
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Ospemifene
MoreCaspase アイソフォーム固有の製品をすべて表示
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生物活性
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Caspase-3 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
>100 μM
Compound: 1
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 25164760] |
| MCF7 | IC50 |
>50 μM
Compound: Ospemifene
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Cytotoxicity against human ER-positive MCF7 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human ER-positive MCF7 cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 26972118] |
| MCF7 | IC50 |
55 μM
Compound: 1
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 96 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 96 hrs by MTT assay
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[PMID: 25164760] |
| MDA-MB-231 | IC50 |
>100 μM
Compound: 1
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Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
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[PMID: 25164760] |
| MDA-MB-231 | IC50 |
>100 μM
Compound: 1
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Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 96 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 96 hrs by MTT assay
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[PMID: 25164760] |
| MDA-MB-231 | IC50 |
>50 μM
Compound: Ospemifene
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Cytotoxicity against human ER-negative MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
Cytotoxicity against human ER-negative MDA-MB-231 cells assessed as cell viability after 72 hrs by MTT assay
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[PMID: 26972118] |
Ospemifene (100 pM-30 μM) binds with essentially comparable affinity to the ER-α and ER-β isoforms and effectively antagonize ERE-mediated transactivation in MCF-7 cells[1].
Ospemifene (0.1 nM-10 μM) does not significantly promote the growth of MCF-7 cells[3].
Ospemifene (0.1-10 μM; 4-6 days) inhibits the growth of MCF-7 cells and has no significant effect on the growth of MDA-MB-231 cells[4].
Ospemifene (0.1-10 μM; posttreatment) decreases hypoxia- and ischemia- induced LDH release, caspase-3 activity, neuronal cell degeneration in primary neocortical cell cultures subjected to hypoxia and/or ischemia[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7
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Concentration:0.1 μM, 1.0 μM, 5.0 μM, 10.0 μM
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Incubation Time:4-6 days
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Result:Inhibited the growth of MCF-7 cells.
Increased its growth inhibitory effect as its concentration increases.
Had a cell growth rate of 95.4% of the control at 0.1 μM and 56.4% of the control at 10.0 μM.
Ospemifene (1-10 mg/kg; p.o.; 4 weeks) can prevent bone loss, maintain the trabecular bone volume of the distal femur, prevent the decrease of bone strength in ovariectomized rats[3].
Ospemifene (10-100 mg/kg; p.o.; once daily; 7 days) inhibits the growth of MCF-7 tumors in the athymic, ovariectomized mouse model with MCF-7 human tumor xenografts[4].
Ospemifene (5-50 mg/kg; p.o.; daily) effectively prevents breast cancer in the MTag.Tg transgenic mouse model[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Animal Model: Adult female Sprague Dawley rats (weight about 300 g at the beginning of the experiments, 2.5 months old), ovariectomized model[3]
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Dosage:0.1 mg/kg, 1 mg/kg, 10 mg/kg
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Administration:Orally, once daily, 4 weeks
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Result:Prevented bone loss by maintaining the trabecular bone volume of the distal femur and preventing the loss of bone strength at doses of 1 and 10 mg/kg.
Prevented the OVX-induced increase in serum cholesterol in a dose-dependent manner.
Had no significant effect on uterine wet weight or morphology at 0.1 or 1 mg/kg.
Had a slightly estrogenic effect at 10 mg/kg.
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Animal Model:Female Sprague Dawley rats, DMBA (HY-W011845)-induced breast carcinoma model[3]
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Dosage:10 mg/kg, 50 mg/kg
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Administration:Orally, 4 weeks
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Result:Reduced the number of breast tumors.
Reduced the number of growing tumors, increased the number of dormant or regressing tumors, and even caused some tumors to disappear.
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Animal Model:Female athymic nude mice (8-12 weeks old; nu/nu-BALB/cABom), MCF-7 cell-transplanted tumor model after OVX and estrogen supplementation[3]
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Dosage:1 mg/kg, 10 mg/kg, 50 mg/kg
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Administration:Oral gavage (p.o.), 48 days
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Result:Cannot sustain tumor growth in the absence of estrogen.
Had no effect at 1 mg/kg and resulted in slower tumor regression at 10 or 50 mg/kg.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 128607-22-7
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性状 Solid
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分子量 378.89
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分子式 C24H23ClO2
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Color White to off-white
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SMILES
ClCC/C(C1=CC=CC=C1)=C(C2=CC=C(OCCO)C=C2)\C3=CC=CC=C3
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別名
オスペミフェン; FC-1271a
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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J Med Chem
Screening and Reverse-Engineering of Estrogen Receptor Ligands as Potent Pan-Filovirus Inhibitors. [Abstract]2020 Oct 8;63(19):11085-11099. PMID: 32886512 -
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Res Sq
Sex differences in viral entry protein expression, host responses to SARS-CoV-2, and in vitro responses to sex steroid hormone treatment in COVID-19. [Abstract]2020 Dec 31:rs.3.rs-100914. PMID: 33173861
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (263.93 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.60 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (281 KB)
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SDS (398 KB)
- English - EN (398 KB)
- Français - FR (398 KB)
- Deutsch - DE (398 KB)
- Norwegian - NO (398 KB)
- Español - ES (398 KB)
- Swedish - SV (398 KB)
- Italian - IT (398 KB)
- Portuguese - PT (398 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Unkila M, et, al. Vaginal effects of ospemifene in the ovariectomized rat preclinical model of menopause. J Steroid Biochem Mol Biol. 2013 Nov;138:107-15. [Content Brief]
[2]. Bruyniks N, et, al. Systematic indirect comparison of ospemifene versus local estrogens for vulvar and vaginal atrophy. Climacteric. 2017 Jun; 20(3): 195-204. [Content Brief]
[3]. Qiang Qv.et al.Selective estrogenic effects of a novel triphenylethylene compound, FC1271a, on bone, cholesterol level, and reproductive tissues in intact and ovariectomized rats. Endocrinology.Feb;141(2):809-20. 25. (2000). [Content Brief]
[4]. Tracy L. Taras et al.In vitro and in vivo biologic effects of Ospemifene (FC-1271a) in breast cancer. The Journal of Steroid Biochemistry and Molecular Biology 77(4-5):271-9,(2001). [Content Brief]
[6]. Burich RA, et al. Ospemifene and 4-hydroxyospemifene effectively prevent and treat breast cancer in the MTag.Tg transgenic mouse model. Menopause. 2012 Jan;19(1):96-103. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6393 mL | 13.1964 mL | 26.3929 mL | 65.9822 mL |
| 5 mM | 0.5279 mL | 2.6393 mL | 5.2786 mL | 13.1964 mL | |
| 10 mM | 0.2639 mL | 1.3196 mL | 2.6393 mL | 6.5982 mL | |
| 15 mM | 0.1760 mL | 0.8798 mL | 1.7595 mL | 4.3988 mL | |
| 20 mM | 0.1320 mL | 0.6598 mL | 1.3196 mL | 3.2991 mL | |
| 25 mM | 0.1056 mL | 0.5279 mL | 1.0557 mL | 2.6393 mL | |
| 30 mM | 0.0880 mL | 0.4399 mL | 0.8798 mL | 2.1994 mL | |
| 40 mM | 0.0660 mL | 0.3299 mL | 0.6598 mL | 1.6496 mL | |
| 50 mM | 0.0528 mL | 0.2639 mL | 0.5279 mL | 1.3196 mL | |
| 60 mM | 0.0440 mL | 0.2199 mL | 0.4399 mL | 1.0997 mL | |
| 80 mM | 0.0330 mL | 0.1650 mL | 0.3299 mL | 0.8248 mL | |
| 100 mM | 0.0264 mL | 0.1320 mL | 0.2639 mL | 0.6598 mL |
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