| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Trestolone is a potent agonist of the Androgen Receptor (AR). It functions as an androgen by binding to and activating AR, which leads to the suppression of the hypothalamic-pituitary-gonadal (HPG) axis, specifically inhibiting the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).
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| ln Vitro |
Trestolone exhibits high binding affinity for the androgen receptor, with potency significantly greater than testosterone. It is a potent inhibitor of LH and FSH secretion in in vitro models of pituitary function. As a synthetic AAS, it has a high ratio of androgenic to anabolic activity compared to other AAS.
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| ln Vivo |
Trestolone is utilized in the form of trestolone acetate, an intramuscular injection that serves as a persistent prodrug of trestolone.
In vivo, trestolone induces a state of temporary infertility in males by reducing FSH (impairing spermatogenesis) and LH (suppressing intratesticular testosterone). It is also being studied for androgen replacement therapy, where it effectively maintains androgen-dependent physiological functions with fewer dose-related side effects than testosterone. |
| Enzyme Assay |
In vitro AR binding assays are performed using a standard radioligand competition format. The AR is incubated with a high-affinity radiolabeled ligand (e.g., 3H-R1881 or 3H-DHT) and varying concentrations of trestolone. After incubation to reach equilibrium, the bound and free fractions are separated by charcoal adsorption or filtration. The IC50 value is then determined by scintillation counting to calculate its binding affinity.
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| Cell Assay |
Trestolone is utilized in cell-based assays to assess its agonistic activity. Cells expressing the AR and a luciferase reporter gene under an androgen-responsive element are treated with a dilution series of trestolone. After 24 hours of incubation, the cells are lysed, and luciferase activity is measured. The EC50 for AR activation is calculated to determine the compound's potency.
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| Animal Protocol |
In animal studies, trestolone (as trestolone acetate, a prodrug) is administered to male rats or non-human primates via intramuscular injection. Efficacy is assessed by measuring serum hormone levels (LH, FSH, and testosterone), testes weights, and sperm counts in the epididymis to evaluate the suppression of spermatogenesis and the induction of infertility.
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| ADME/Pharmacokinetics |
Trestolone acetate is administered as a persistent intramuscular prodrug, providing sustained release of trestolone into the circulation. This results in a long-lasting pharmacokinetic profile, with steady-state levels achieved with monthly or bimonthly injections. This favorable profile is ideal for applications requiring long-term androgen suppression.
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| Toxicity/Toxicokinetics |
Toxicological studies of trestolone have focused on its effects on the male reproductive system, which are its intended on-target effects. Overall, trestolone has been shown to be well-tolerated at contraceptive doses, with no significant off-target toxicity reported in long-term studies. Its safety profile is a key factor in its development for male contraception.
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| Additional Infomation |
Tralodone (7α-methyl-19-nortestosterone) is a synthetic androgen developed by the Population Council as a potential candidate for male hormonal contraception. In men, regular use of adequate doses of tralodone can lead to temporary infertility.
Drug Indications It has been studied for contraception and treatment of male hormone deficiency/abnormalities. Mechanism of Action Tralodone is a potent inhibitor of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release. Since spermatogenesis requires testosterone and FSH, the decrease in FSH and LH caused by tralodone, which in turn leads to a decrease in testosterone, impairs spermatogenesis. Trestolone acetate has completed Phase II clinical trials for male contraception, demonstrating high efficacy in suppressing spermatogenesis. It remains a promising candidate for a hormonal male contraceptive and is currently being investigated by the Population Council. The compound is also used in research for hormone replacement therapy and muscle-wasting conditions. It is not approved for general clinical use. |
| Molecular Formula |
C19H28O2
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|---|---|
| Molecular Weight |
288.42
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| Exact Mass |
288.209
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| CAS # |
3764-87-2
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| PubChem CID |
9838899
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| Appearance |
White to off-white solid powder
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| Density |
1.11g/cm3
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| Boiling Point |
439.4ºC at 760mmHg
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| Flash Point |
187.3ºC
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| Index of Refraction |
1.557
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| LogP |
3.735
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
21
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| Complexity |
494
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| Defined Atom Stereocenter Count |
7
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| SMILES |
C[C@@H]1CC2=CC(=O)CC[C@@H]2[C@@H]3[C@@H]1[C@@H]4CC[C@@H]([C@]4(CC3)C)O
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| InChi Key |
YSGQGNQWBLYHPE-CFUSNLFHSA-N
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| InChi Code |
InChI=1S/C19H28O2/c1-11-9-12-10-13(20)3-4-14(12)15-7-8-19(2)16(18(11)15)5-6-17(19)21/h10-11,14-18,21H,3-9H2,1-2H3/t11-,14+,15-,16+,17+,18-,19+/m1/s1
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| Chemical Name |
(7R,8R,9S,10R,13S,14S,17S)-17-hydroxy-7,13-dimethyl-2,6,7,8,9,10,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (346.72 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (8.67 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.67 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (8.67 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4672 mL | 17.3358 mL | 34.6717 mL | |
| 5 mM | 0.6934 mL | 3.4672 mL | 6.9343 mL | |
| 10 mM | 0.3467 mL | 1.7336 mL | 3.4672 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Link: https://clinicaltrials.gov/ct2/show/NCT00812630
Conditions:Blood PressureProducts are for research use only; We do not sell to patients
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