Tibolone
Based on 1 Customer Validation
Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research.
For research use only. We do not sell to patients.
- Purity: 99.9%
- CAS No.: 5630-53-5
- Formula: C21H28O2
- Molecular Weight:312.45
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female albino Wistar rats bearing ovariectomy[1]
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Dosage:1 mg/day
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Administration:Oral administration; daily; for 12 weeks
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Result:Showed a significantly higher overall bone tissue and a higher body mass density.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 5630-53-5
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Appearance Solid
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Molecular Weight 312.45
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Formula C21H28O2
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Color White to off-white
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SMILES
C[C@H]1[C@@]2([H])[C@@]3([H])[C@@]([C@@](O)(CC3)C#C)(CC[C@]2([H])C4=C(CC(CC4)=O)C1)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (320.05 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.00 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.00 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Dragos Apostu, et al. Tibolone, alendronate, and simvastatin enhance implant osseointegration in a preclinical in vivo model. Clin Oral Implants Res. 2020 Jul;31(7):655-668. [Content Brief]
[2]. Marcos García-Juárez, et al. Tibolone induces lordosis behavior, but not concurrent or sequential inhibition, in Sprague Dawley rats. Neurosci Lett. 2021 Apr 24;755:135916. [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 | 3.2005 mL | 16.0026 mL | 32.0051 mL | 80.0128 mL |
| 5 mM | 0.6401 mL | 3.2005 mL | 6.4010 mL | 16.0026 mL | |
| 10 mM | 0.3201 mL | 1.6003 mL | 3.2005 mL | 8.0013 mL | |
| 15 mM | 0.2134 mL | 1.0668 mL | 2.1337 mL | 5.3342 mL | |
| 20 mM | 0.1600 mL | 0.8001 mL | 1.6003 mL | 4.0006 mL | |
| 25 mM | 0.1280 mL | 0.6401 mL | 1.2802 mL | 3.2005 mL | |
| 30 mM | 0.1067 mL | 0.5334 mL | 1.0668 mL | 2.6671 mL | |
| 40 mM | 0.0800 mL | 0.4001 mL | 0.8001 mL | 2.0003 mL | |
| 50 mM | 0.0640 mL | 0.3201 mL | 0.6401 mL | 1.6003 mL | |
| 60 mM | 0.0533 mL | 0.2667 mL | 0.5334 mL | 1.3335 mL | |
| 80 mM | 0.0400 mL | 0.2000 mL | 0.4001 mL | 1.0002 mL | |
| 100 mM | 0.0320 mL | 0.1600 mL | 0.3201 mL | 0.8001 mL |