2. Vitamin D Related/Nuclear Receptor Apoptosis Protein Tyrosine Kinase/RTK
  3. Androgen Receptor Apoptosis Insulin Receptor Caspase
  4. Ligandrol

Ligandrol is an orally active, selective androgen receptor (AR) agonist. Ligandrol enhances protein synthesis, inhibits muscle breakdown and oxidative stress, improves muscle cell viability and bone tissue microstructure, and reduces Cisplatin (HY-17394)-induced muscle toxicity and apoptosis. Ligandrol promotes muscle growth, protects bone structure, and has anti-diabetic, anti-apoptotic and antioxidant effects. Ligandrol can antagonize Streptozotocin (HY-13753) damage to pancreatic islets and improve the symptoms of type 2 diabetes.

For research use only. We do not sell to patients.

Ligandrol Chemical Structure

Ligandrol Chemical Structure

CAS No. : 1165910-22-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 2 publication(s) in Google Scholar

Ligandrol Related Antibodies

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Description

Ligandrol is an orally active, selective androgen receptor (AR) agonist. Ligandrol enhances protein synthesis, inhibits muscle breakdown and oxidative stress, improves muscle cell viability and bone tissue microstructure, and reduces Cisplatin (HY-17394)-induced muscle toxicity and apoptosis. Ligandrol promotes muscle growth, protects bone structure, and has anti-diabetic, anti-apoptotic and antioxidant effects. Ligandrol can antagonize Streptozotocin (HY-13753) damage to pancreatic islets and improve the symptoms of type 2 diabetes[1][2][3].

IC50 & Target

Caspase 3

 

Caspase-7

 

In Vitro

Ligandrol increases insulin secretion in MIN6 cells within 2 hours exprouse[1].
Ligandrol (0.5-50 mg/L; 24 h) increased cell viability, total antioxidant capacity (TAC) and caspase 3/7 expression in a concentration-dependent manner, and decreased lactate dehydrogenase (LDH) release, total oxidative state (TOS), DNA fragmentation, lipid peroxidation and intracellular calcium concentration in the mouse skeletal muscle cell line C2C12[2].

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

Ligandrol Related Antibodies

Cell Viability Assay[1]

Cell Line: Mouse C2C12 skeletal muscle cells
Concentration: 0.5, 5, 50 mg/L (Ligandrol); 10 μM (Cisplatin)
Incubation Time: 24 h
Result: Had no significant cytotoxicity, but co-treatment with Cisplatin significantly increased cell viability by 1.1-2.14-fold compared to Cisplatin alone.
Reduced LDH release, a marker of membrane damage, by 1.16-2.18-fold in Ligandrol + Cisplatin groups, indicating improved membrane integrity.
In Vivo

Ligandrol (0.3 mg/kg, 1 mg/kg; oral) significantly reduces body weight and fasting blood glucose levels in high-fat diet (HFD) and Streptozotocin (HY-13753)-induced type 2 diabetes mellitus (T2DM) mouse models, increases neurogenic differentiation of AR target genes, and prevents pancreatic islet degeneration[1].
Ligandrol (0.5 mg/kg; oral gavage; once daily; 3 weeks) improves muscle strength and function, increases muscle mass, and reduces Cisplatin (HY-17394)-induced oxidative stress and apoptosis in a mouse model of muscle atrophy[2].

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

Animal Model: Cisplatin-Induced Muscle Atrophy Model (male, 25 g, 8 weeks old)[2]
Dosage: 0.5 mg/kg
Administration: Oral gavage, once daily for 3 weeks
Result: -Muscle Strength and Function:
Significantly increased the grip strength of the mice than that in the Cisplatin-only group, indicating improved muscle strength. Enhanced the performance in the rotarod test, suggesting better muscle function.
-Muscle Mass:
Increased the weight of the gastrocnemius and quadriceps muscles compared to the Cisplatin-only group, demonstrating an increase in muscle mass.
-Oxidative Stress:
Decreased the levels of malondialdehyde (MDA), a marker of lipid peroxidation in the muscle tissues, while the activities of superoxide dismutase (SOD) and catalase (CAT) were increased, indicating a reduction in oxidative stress.
-Apoptosis:
Significantly decreased the number of apoptotic cells in the muscle tissues, as determined by TUNEL staining, than in the Cisplatin-only group. Decreased the expression of pro-apoptotic proteins such as Bax, while increased the expression of anti-apoptotic protein Bcl-2, suggesting apoptosis inhibition in muscle cells.
Molecular Weight

338.25

Formula

C14H12F6N2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC(F)(F)[C@@H]([C@]1([H])N(C2=CC(C(F)(F)F)=C(C=C2)C#N)CCC1)O
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 (295.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9564 mL 14.7819 mL 29.5638 mL
5 mM 0.5913 mL 2.9564 mL 5.9128 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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 (7.39 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 (7.39 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:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
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

Purity: 99.93%

SDS (393 KB)

COA (257 KB) HNMR (254 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
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 2.9564 mL 14.7819 mL 29.5638 mL 73.9096 mL
5 mM 0.5913 mL 2.9564 mL 5.9128 mL 14.7819 mL
10 mM 0.2956 mL 1.4782 mL 2.9564 mL 7.3910 mL
15 mM 0.1971 mL 0.9855 mL 1.9709 mL 4.9273 mL
20 mM 0.1478 mL 0.7391 mL 1.4782 mL 3.6955 mL
25 mM 0.1183 mL 0.5913 mL 1.1826 mL 2.9564 mL
30 mM 0.0985 mL 0.4927 mL 0.9855 mL 2.4637 mL
40 mM 0.0739 mL 0.3695 mL 0.7391 mL 1.8477 mL
50 mM 0.0591 mL 0.2956 mL 0.5913 mL 1.4782 mL
60 mM 0.0493 mL 0.2464 mL 0.4927 mL 1.2318 mL
80 mM 0.0370 mL 0.1848 mL 0.3695 mL 0.9239 mL
100 mM 0.0296 mL 0.1478 mL 0.2956 mL 0.7391 mL
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Ligandrol Related Classifications

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.

Keywords:

Ligandrol1165910-22-4LGD-4033LGD4033LGD 4033Androgen ReceptorApoptosisInsulin ReceptorCaspaseInhibitorinhibitorinhibit

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