| Size | Price | Stock | Qty |
|---|---|---|---|
| 2g |
|
||
| 5g |
|
||
| 10g |
|
||
| 25g |
|
||
| 50g |
|
||
| Other Sizes |
| Targets |
Testosterone acetate is a prodrug that targets the androgen receptor. The acetate ester at the 17β-position increases lipophilicity (experimental logP 4.16), enabling sustained release from intramuscular depots. Its relatively rapid hydrolysis by plasma and tissue esterases yields free testosterone, which then binds to androgen receptors to exert biological effects. DHT, the active metabolite, binds to the same androgen receptor even more strongly than testosterone.
|
|---|---|
| ln Vitro |
In vitro, testosterone acetate has antitumor activity. It binds to androgen receptors in target tissues, promoting anabolic effects such as muscle growth and increased bone density. As a prodrug, its activity depends on hydrolysis to free testosterone, which then activates androgen receptor-mediated gene transcription. The compound's in vitro activity is characterized by its ability to activate androgen receptor signaling pathways after esterase-mediated conversion to testosterone.
|
| ln Vivo |
In vivo, testosterone acetate is used as an androgen and anabolic steroid. It has been studied for the research of impotence, weakness, fatigue, and hypogonadism. The acetate ester provides a sustained release profile from intramuscular depots, with a half-life of approximately 2-3 days and rapid washout, making it suitable for crossover study designs. It serves as a reference compound for studying structure-activity relationships among androgen esters.
|
| Enzyme Assay |
The in vitro activity of testosterone acetate is assessed using androgen receptor binding assays and cell-based reporter assays. For receptor binding, the androgen receptor is incubated with a radiolabeled androgen (e.g., [³H]R1881) in the presence of varying concentrations of testosterone acetate, and the displacement of the radiolabeled ligand is measured. For functional assays, cells transfected with an androgen-responsive reporter gene (e.g., ARE-luciferase) are treated with testosterone acetate, and luciferase activity is measured. Esterase inhibitors may be used to study the contribution of hydrolysis to activity.
|
| Cell Assay |
For cellular assays, androgen receptor-positive cell lines such as LNCaP or PC-3 cells transfected with AR are used. Cells are cultured in steroid-depleted media and treated with various concentrations of testosterone acetate (typically 0.1 nM to 10 μM) for 24-72 hours. The expression of androgen-responsive genes (e.g., PSA, TMPRSS2) is analyzed by qPCR or Western blotting. Cell proliferation is assessed using MTT or CellTiter-Glo assays. The conversion of testosterone acetate to testosterone can be measured by LC-MS/MS in cell culture media.
|
| Animal Protocol |
In vivo, testosterone acetate is typically administered via intramuscular injection in animal models. The compound is formulated in oil-based vehicles (e.g., arachis oil or sesame oil) for sustained release. Doses typically range from 1-50 mg/kg depending on the species and study duration. Pharmacokinetic studies involve measurement of testosterone acetate and testosterone levels in plasma by LC-MS/MS. Androgenic and anabolic effects are assessed by measuring muscle mass, bone density, and organ weights (prostate, seminal vesicles).
|
| ADME/Pharmacokinetics |
Testosterone acetate has a molecular weight of 330.46 g/mol and a molecular formula of C21H30O3. It has an experimental logP of 4.16, indicating high lipophilicity. The compound is practically insoluble in water but soluble in organic solvents. It should be stored in dry, dark conditions at 0-4°C for short-term storage or -20°C for long-term storage. The acetate ester is labile and can be hydrolyzed.
|
| Toxicity/Toxicokinetics |
Testosterone acetate is regulated as a Schedule III compound in the United States. As an anabolic androgenic steroid, it has potential for abuse and is classified as a controlled substance. Side effects may include androgenic effects (acne, hirsutism, voice deepening), cardiovascular effects, hepatotoxicity, and suppression of endogenous testosterone production. The compound should be used with caution in patients with prostate cancer, cardiovascular disease, or liver disease.
|
| Additional Infomation |
Testosterone acetate is an androgen compound, an acetic acid derivative of testosterone. It plays a metabolic role in the human body. It is a sterol ester, androgen compound, and 3-oxo-Δ(4) steroid. Its function is related to testosterone.
Testosterone acetate is an analytical reference standard and research compound. It was one of the first androgen esters synthesized (first described in 1936) and serves as a reference compound for studying structure-activity relationships among androgen esters. Its short half-life (2-3 days) and rapid washout make it useful for crossover study designs. The compound is not commonly used clinically but remains important in research. It is available from chemical suppliers for research purposes. |
| Molecular Formula |
C21H30O3
|
|---|---|
| Molecular Weight |
330.468
|
| Exact Mass |
330.219
|
| CAS # |
1045-69-8
|
| PubChem CID |
92145
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.1±0.1 g/cm3
|
| Boiling Point |
441.8±45.0 °C at 760 mmHg
|
| Melting Point |
139 - 141ºC
|
| Flash Point |
191.5±28.8 °C
|
| Vapour Pressure |
0.0±1.1 mmHg at 25°C
|
| Index of Refraction |
1.541
|
| LogP |
4.37
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
24
|
| Complexity |
606
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
O(C(C([H])([H])[H])=O)[C@@]1([H])C([H])([H])C([H])([H])[C@@]2([H])[C@]3([H])C([H])([H])C([H])([H])C4=C([H])C(C([H])([H])C([H])([H])[C@]4(C([H])([H])[H])[C@@]3([H])C([H])([H])C([H])([H])[C@@]21C([H])([H])[H])=O
|
| InChi Key |
DJPZSBANTAQNFN-PXQJOHHUSA-N
|
| InChi Code |
InChI=1S/C21H30O3/c1-13(22)24-19-7-6-17-16-5-4-14-12-15(23)8-10-20(14,2)18(16)9-11-21(17,19)3/h12,16-19H,4-11H2,1-3H3/t16-,17-,18-,19-,20-,21-/m0/s1
|
| Chemical Name |
[(8R,9S,10R,13S,14S,17S)-10,13-dimethyl-3-oxo-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-17-yl] acetate
|
| Synonyms |
NSC-523836 NSC 523836 Testosterone acetate
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0260 mL | 15.1300 mL | 30.2599 mL | |
| 5 mM | 0.6052 mL | 3.0260 mL | 6.0520 mL | |
| 10 mM | 0.3026 mL | 1.5130 mL | 3.0260 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
