Droloxifene
Based on 1 publication(s) in Google Scholar
Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.89%
- CAS No.: 82413-20-5
- 화학식: C26H29NO2
- 분자량:387.51
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Droloxifene
More
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Vero | CC50 |
15.82 μM
Compound: Droloxifene
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Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
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10.1101/2020.03.20.999730 |
| Vero | IC50 |
6.6 μM
Compound: Droloxifene
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Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
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10.1101/2020.03.20.999730 |
Droloxifene (10 nM; 16-18 hours) induces apoptosis in MCF-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:10 nM
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Incubation Time:16-18 hours
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Result:Induced cells apoptosis
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:5-month-old sham-operate rats[3]
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Dosage:5, 10, 20 mg/kg
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Administration:Oral; daily for 4 weeks
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Result:BMD of DFM increased significantly at 10mg/kg; completely prevented the decrease of BMC and BMD of DFM induced by OVX at 20 mg/kg/day.
Chemical Information
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CAS No. 82413-20-5
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Appearance Solid
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분자량 387.51
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화학식 C26H29NO2
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Color White to off-white
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SMILES
OC1=CC=CC(/C(C2=CC=C(OCCN(C)C)C=C2)=C(C3=CC=CC=C3)\CC)=C1
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Synonyms
3-Hydroxytamoxifen
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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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
용액&용해도
DMSO : 50 mg/mL (129.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
순도&문서
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Data Sheet (275 KB)
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SDS (701 KB)
- English - EN (701 KB)
- Français - FR (701 KB)
- Deutsch - DE (701 KB)
- Norwegian - NO (701 KB)
- Español - ES (701 KB)
- Swedish - SV (701 KB)
- Italian - IT (701 KB)
- Korean - KR (701 KB)
- Portuguese - PT (701 KB)
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Handling Instructions (2659 KB)
References
[1]. Herrington DM, et al. Cardiovascular effects of droloxifene, a new selective estrogen receptor modulator, in healthypostmenopausal women. Arterioscler Thromb Vasc Biol. 2000 Jun;20(6):1606-12. [Content Brief]
[2]. Grasser WA, et al. Common mechanism for the estrogen agonist and antagonist activities of droloxifene. J Cell Biochem. 1997 May;65(2):159-71. [Content Brief]
[3]. Ke HZ, et al. Droloxifene, a new estrogen antagonist/agonist, prevents bone loss in ovariectomized rats. ndocrinology. 1995 Jun;136(6):2435-41. [Content Brief]
[4]. Huang Y, et al. Anti-implantation effect of droloxifene in rats and its relationship with anti-estrogenic activity. Acta Pharmacol Sin. 2005 Oct;26(10):1243-7. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.5806 mL | 12.9029 mL | 25.8058 mL | 64.5145 mL |
| 5 mM | 0.5161 mL | 2.5806 mL | 5.1612 mL | 12.9029 mL | |
| 10 mM | 0.2581 mL | 1.2903 mL | 2.5806 mL | 6.4514 mL | |
| 15 mM | 0.1720 mL | 0.8602 mL | 1.7204 mL | 4.3010 mL | |
| 20 mM | 0.1290 mL | 0.6451 mL | 1.2903 mL | 3.2257 mL | |
| 25 mM | 0.1032 mL | 0.5161 mL | 1.0322 mL | 2.5806 mL | |
| 30 mM | 0.0860 mL | 0.4301 mL | 0.8602 mL | 2.1505 mL | |
| 40 mM | 0.0645 mL | 0.3226 mL | 0.6451 mL | 1.6129 mL | |
| 50 mM | 0.0516 mL | 0.2581 mL | 0.5161 mL | 1.2903 mL | |
| 60 mM | 0.0430 mL | 0.2150 mL | 0.4301 mL | 1.0752 mL | |
| 80 mM | 0.0323 mL | 0.1613 mL | 0.3226 mL | 0.8064 mL | |
| 100 mM | 0.0258 mL | 0.1290 mL | 0.2581 mL | 0.6451 mL |
Droloxifene Related Classifications
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