1. Vitamin D Related/Nuclear Receptor
  2. Progesterone Receptor Androgen Receptor Estrogen Receptor/ERR
  3. Tibolone

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.

Tibolone Chemical Structure

Tibolone Chemical Structure

CAS No. : 5630-53-5

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Description

Tibolone is a broad spectrum gonadal steroid agonist with progestagenic, androgenic, and estrogenic activities. Tibolone can be used for postmenopausal osteoporosis research[1][2].

In Vivo

Tibolone (1 mg/day; oral administration; for 12 weeks) treatment enhances the osseointegration process of intramedullary titanium implants in ovariectomized rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female albino Wistar rats bearing ovariectomy[1]
Dosage: 1 mg/day
Administration: Oral administration; daily; for 12 weeks
Result: Showed a significantly higher overall bone tissue and a higher body mass density.
Molecular Weight

312.45

Formula

C21H28O2

CAS No.
Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2005 mL 16.0026 mL 32.0051 mL
5 mM 0.6401 mL 3.2005 mL 6.4010 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
References

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Tibolone
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HY-123047
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