RAD-140 Testolone 60 capsules

RAD-140 (Testolone) – SARM research reagent | One-Peptides

Chemical reagent intended exclusively for laboratory tests (Research Use Only). It is not a medicinal product, dietary supplement or food. It is not intended for administration to humans or animals outside a controlled experimental environment.

RAD-140, also known in the literature under the name Testolone, belongs to non-steroidal selective androgen receptor modulators (SARMs). In laboratories, it is a chemical reagent for preclinical research – work in vitro and on animal models. The following description organizes what has actually been reported in the peer-reviewed literature: receptor mechanism, results from preclinical models, documented hepatotoxicity signal, and regulatory and anti-doping status of the compound. It does not and cannot contain directions for administration to humans.

What is RAD-140 (Testolone) – origin and place in the SARM class

RAD-140 was developed by the Radius Health research team, and the first full characterization of the compound was published by Miller et al. (2011). This work described the molecule’s design, synthesis, and preclinical profile – from androgen receptor affinity to behavior in animal models. The compound was designed as an orally bioavailable, non-steroidal androgen receptor ligand with a profile different from classic androgens.

The creation of RAD-140 is part of a broader trend of development SARM class, which Narayanan, Coss and Dalton (2018) describe as an attempt to separate the two actions that are inherent in the testosterone molecule: the anabolic effect on skeletal muscle and bone and the androgenic effect on tissues such as the prostate or skin. Subsequent generations of non-steroidal compounds – from the first arylpropionamides to structures such as RAD-140 – were created to shift this balance. The class is not homogeneous: different molecules exhibit different profiles of affinity, intrinsic activity and tissue selectivity.

In the market, RAD-140 is sometimes described as the “strongest SARM”. This is a marketing narrative, not a clinical finding. “Potency” comparisons between compounds in this class are based on parameters measured in a specific model, at a specific endpoint – and change with the model. Bond et al. (2025), in a critical review of the class, point out that inferring the superiority of one SARM over another based on preclinical data is invalid because there is a lack of direct comparisons in humans under controlled conditions. This description does not replicate the promise of “power”. Limited to what is reported and the model in which it is reported.

Chemical characteristics of the RAD-140 reagent

The identity, purity and content of substances in the unit are confirmed by the analytical documentation of a specific batch. The batch number allows you to link the material to a specific certificate – without this link, no quality declaration has any verifiable value.

Androgen receptor – how SARM selectivity arises

The androgen receptor (AR) belongs to the nuclear receptor superfamily and functions as a ligand-dependent transcription factor. It is composed of several functional fragments: the N-terminal domain (NTD), responsible for most of the transcriptional activity and containing the AF-1 activation region; a DNA-binding domain (DBD) with zinc-finger motifs that recognizes androgen response sequences in the promoters of target genes; and a C-terminal ligand-binding domain (LBD), which houses the binding pocket of the androgen molecule or its non-steroidal equivalent.

Ligand binding in the LBD pocket induces a conformational change of the receptor. It changes the arrangement of helix 12, frees the receptor from chaperones, enables dimerization, translocation to the cell nucleus and binding to DNA. What is decisive for the biological effect is what happens on the surface of the altered receptor: a groove is created to which regulatory proteins are recruited – coactivators from the p160 family (SRC-1, SRC-2, SRC-3) that enhance transcription or corepressors (NCoR, SMRT) that silence it.

Herein lies the explanation for a phenomenon called tissue selectivity. Different ligands stabilize slightly different receptor conformations and so recruit different sets of accessory proteins. Because the profile of available coactivators and corepressors differs in muscle, bone, and prostate, the same compound may behave as an agonist in one tissue and as a partial agonist or antagonist in another. Narayanan et al. (2018) describe this model as the conceptual basis of the entire SARM class.

Why SARM is not an anabolic-androgenic steroid

The difference is structural and has metabolic consequences. Anabolic-androgenic steroids come from the steroid skeleton of testosterone. RAD-140 does not have this framework – it is a non-steroidal molecule. Consequence one: it is not a substrate of 5α-reductase, an enzyme that converts testosterone into dihydrotestosterone (DHT), a stronger androgen responsible for a significant part of androgenic activities in peripheral tissues. Second consequence: it does not undergo aromatization to estrogens because aromatase acts on steroid substrates. Solomon et al. (2019) and Narayanan et al. (2018) point to these two points as the pharmacological distinguishing features of the class.

However, the lack of these changes does not mean that there is no impact on the hormonal system. Signaling through the androgen receptor in the hypothalamus and pituitary is preserved, which translates into the possibility of inhibiting endogenous testosterone production – as discussed below in the section on the reported safety profile. Nonsteroidal therapy changes metabolic pathways and does not eliminate the effect on the hormonal axis.

RAD-140 mechanism of action – what has been described in the studies

Miller et al. (2011) reported that RAD-140 binds the androgen receptor with high affinity and acts in cellular systems as its agonist, activating the transcription of AR-dependent genes. In animal models, a discrepancy between the effects on muscle tissue and the effects on prostate tissue was observed – exactly the pattern that defines the concept of selectivity in the description of SARM compounds. This discrepancy is sometimes expressed numerically as the ratio of anabolic to androgenic effects.

This parameter requires careful interpretation. It is not a physical constant of the molecule, but a value that depends on the species, end point and method of measurement. Bond et al. (2025) emphasize that anabolic-androgenic indicators determined in the rodent model do not transfer directly to humans, and their comparison between the work of different teams is subject to methodological error. In other words: the number describes the model, not the promise.

The second objection concerns selectivity itself. It has been described in animal models and cellular systems. There is no evidence that it translates to humans in the form of a guaranteed separation of effects – there are no controlled phase III clinical trials to verify this (Bond et al. 2025).

Overview of preclinical research on RAD-140

The preclinical literature on RAD-140 includes three main pieces of work leading in three different directions. We discuss each separately, including its model and limitations.

Miller et al. (2011) – preclinical characteristics and AR binding profile

Introductory work. Model: cellular systems and rodents and primates in some preclinical experiments. Reported endpoints: binding affinity to the androgen receptor, transcriptional activity in reporter assays, and changes in the mass of target tissues – the levator ani muscle and the prostate – in the castrated rat model, a classic system assessing the separation of anabolic and androgenic effects. Anabolic activity on muscle tissue has been reported with limited effects on prostate tissue compared to testosterone.

Limitations: This is a preclinical characterization, designed for the selection of a molecule for further development, and not for human safety assessment. Endpoints are surrogates. Castrated animals are a model with reduced levels of endogenous androgens, which increases the sensitivity of the system to exogenous ligand.

Jayaraman et al. (2014) — neuroprotection in the kainate model

Model: primary cultures of hippocampal neurons and male rats with kainic acid damage. Kainate is an agonist of glutamatergic receptors and causes excitotoxicity – excessive neuronal stimulation leading to calcium influx, oxidative stress and cell death. This is the standard model of neuronal damage used in experimental neuroscience.

What was reported: RAD-140 reduced neuronal death in culture and limited hippocampal neuronal damage in kainate-exposed rats. The effect was reported to be mediated by the androgen receptor present in neurons, involving the MAPK pathway – the same receptor axis that produces the effect in muscle, just in a different tissue.

What it doesn’t prove: It doesn’t prove a neuroprotective effect in humans. It does not constitute the basis for making any claims about the effects on cognitive functions, neurodegenerative diseases or brain health. The kainate model is an acute experimental injury, not an equivalent of a chronic disease process in humans. The result has value as a mechanistic clue for further basic research – and only that.

Yu et al. (2017) – inhibition of AR+/ER+ breast cancer growth

Model: breast cancer cell lines expressing androgen receptor and estrogen receptor (AR+/ER+) and xenograft models. Biological context: In this tumor subtype, estrogen signaling drives proliferation, and the androgen receptor is present in most ER+ tumors. The researchers’ hypothesis was that AR activation may act as an alternative pathway to suppress estrogen signaling – the androgen receptor, stimulated by a ligand, affects the expression of ER-dependent genes, including the estrogen receptor itself.

What was reported: RAD-140 inhibited the growth of AR+/ER+ cancer cells under experimental conditions and in a xenograft model, and the mechanism was associated with AR activation and the resulting effect on the estrogen axis. The work is preclinical and exploratory in nature.

What this does not prove: It does not mean that RAD-140 is an anticancer drug or that it is safe or effective in human oncology. It also does not mean that the compound “protects against cancer” – such a claim would be a misuse of the data. The xenograft model is a system with limited translation; the history of oncology knows many compounds that are effective in the xenograft and ineffective in patients.

Common thread – one receptor, three tissues

Three works, three different areas – and one mechanistic axis. A muscle, a neuron, a breast cancer cell: in each of these systems, the described effect is carried out through the androgen receptor. This is a coherent pharmacological picture and at the same time an interpretative warning. The androgen receptor is present in many tissues of the body, and the ligand that activates it acts wherever the receptor is present. The selectivity described in the model does not mean the lack of action outside the target tissue.

RAD-140 Safety Profile – What has been reported in the literature

The information below describes the substance and events reported in the literature. They are not instructions, consumer warnings or solicitations – they are characteristics of the reagent that should be known by everyone working with it.

• Suppression of the hypothalamic-pituitary-gonadal axis. Activation of the androgen receptor in the central elements of the HPG axis triggers negative feedback: LH and FSH secretion decreases, followed by endogenous testosterone production. Solomon et al. (2019) and Bond et al. (2025) describe suppression as a reported effect of the SARM class, observed in data from early phase studies of various compounds of this class.
• Decrease in HDL cholesterol concentration. The reduction in the HDL fraction is one of the most consistently reported biochemical changes in SARM research and is treated as a class effect (Bond et al. 2025; Solomon et al. 2019). The long-term significance of this change on cardiovascular risk remains unexplored in this class of compounds.
• Hepatotoxicity. Described above – two case reports, including one with a cholestatic pattern (Barbara et al. 2020; Niazi et al. 2025). Elevations in liver parameters have also been reported in other class reports.
• Adverse events reported for the class. In a review on the safety of SARMs, Leciejewska et al. (2024) compare the reported side effects of compounds of this group, pointing to the paucity of data from controlled studies and the dominance of case reports and spontaneous reports. The authors emphasize the discrepancy between the image promoted in non-medical circulation and the state of actual knowledge.
• Self-reported data – limited evidentiary value. Joshi et al. (2025) analyzed information from people declaring contact with SARM compounds. This type of data has only indicative value: it is subject to selection error, lack of verification of the identity of the substance, lack of laboratory confirmation and a tendency to underreport adverse events. They do not replace controlled studies and should not be considered evidence of safety.
• No phase III and no long-term data. RAD-140 has not undergone full clinical development. Bond et al. (2025) formulate it clearly: no registration studies confirming safety and effectiveness in the population have been completed for any SARM class compound, and there is no data on long-term consequences.

RAD-140 and anti-doping control – WADA S1

RAD-140 is on the List of Prohibited Substances and Methods of the World Anti-Doping Agency (WADA) in the category S1 – anabolic agents, in the subgroup “other anabolic agents” which includes selective androgen receptor modulators. The ban is in force at any time — both during the competition period and outside the competition. The presence of a compound or its metabolites in an Athlete’s sample constitutes an anti-doping rule violation.

Detectability is not a technical problem for accredited laboratories. Thevis and Schänzer (2018) describe SARM detection methods based on liquid chromatography coupled with mass spectrometry (LC-MS/MS), allowing the identification of both the parent compound and its metabolites in urine at trace concentrations. Characteristic metabolic transformations have been described for RAD-140, including hydroxylation and demethylation products, used as analytical markers. The detection window for metabolites is sometimes significantly longer than the detection window for the parent compound.

A practical conclusion for anyone subject to doping control: contact with this material means the risk of a positive result and disciplinary consequences. The reagent is intended for laboratory use only.

RAD-140 in capsule form – a form of packaging the reagent

The reagent is supplied in capsule form. The capsule is only a form of packaging research material: portioning into repeatable units with declared contents facilitates records, inventory control and linking the material with batch documentation.

The capsule form does not change the status of the reagent. Packaging into capsules is a technical solution, not a suggestion of intended use. RAD-140 remains a Research Use Only chemical reagent it is not intended for consumption by humans or animals.

It is worth saying it directly, because in everyday speech the form is sometimes confused with the regulatory class. The character is not a regulatory class. What a given material is under the law is determined by its composition, purpose and registration status – not the shape of the individual packaging. The capsule does not make the research reagent a dietary supplement or a medicinal product – it is only a unit package of material with declared contents. RAD-140 is not a dietary supplement, is not a food and is not a medicinal product.

The material is stored in its original packaging, in a dry and cool place, away from light and moisture. The capsule form does not require a cold chain. Work with the reagent should be carried out in accordance with the internal procedures of the research unit and by qualified personnel.

Regulatory status of RAD-140

RAD-140 is not registered as a medicinal product. It has not been approved for marketing by the European Medicines Agency (EMA) or the US Food and Drug Administration (FDA) and has not undergone the registration procedure for any indication. It remains a research union with status Research Use Only.

It is also not a dietary supplement or an ingredient approved for use in foodstuffs. Marketing it as a product intended for human consumption is inconsistent with food and pharmaceutical regulations.

In organized sports, RAD-140 is a prohibited substance – WADA category S1 (anabolic agents), prohibition at any time.

Limitations of the evidence – what we don’t know about RAD-140

An honest description of the research relationship ends with a list of what was not established.

• There are no phase III clinical trials. A full clinical development program has not been completed for RAD-140. There are no regulatory data supporting efficacy or safety for any indication (Bond et al. 2025).
• The evidence base is based on preclinical models and case reports. Three preclinical studies (Miller 2011, Jayaraman 2014, Yu 2017) and two case reports of hepatotoxicity (Barbara 2020, Niazi 2025) constitute the core of the literature on this compound. Animal and cell models do not transfer directly to humans; case reports do not allow for risk estimation.
• No data on long-term effects. It is not known what the long-term effects of exposure to RAD-140 are – on the hormonal axis, lipid profile, liver, cardiovascular system or oncological risk. There are no observational studies with an appropriate time horizon.
• Unknown frequency of adverse events. The hepatotoxicity signal is documented, but its scale is not.
• Uncertainty about material in circulation outside the laboratory. Van Wagoner et al. (2017) showed that products sold as SARMs often do not contain the declared substance. Some reports of effects and adverse events may therefore concern other compounds.

FAQ – RAD-140 (Testolone)

What is RAD-140 (Testolone)?
It is a non-steroidal selective androgen receptor modulator (SARM), first characterized by Miller et al. (2011). In the laboratory, it functions as a chemical reagent for preclinical research – for research use only (RUO).

Is RAD-140 a drug or dietary supplement?
NO. RAD-140 is not registered as a medicinal product (no EMA or FDA approval) and is not a dietary supplement or food. It is a reagent for laboratory testing and is not intended for consumption.

How does RAD-140 differ from an anabolic-androgenic steroid?
Structure and metabolism. Steroids are derived from the steroid skeleton of testosterone, RAD-140 is a non-steroidal molecule – it is not a substrate of 5α-reductase or aromatase (Narayanan et al. 2018; Solomon et al. 2019). However, this does not mean there is no effect on the hormonal axis: suppression of the hypothalamic-pituitary-gonadal axis is a reported effect of the SARM class.

What is known about the effect of RAD-140 on the liver?
Published in peer-reviewed literature two independent case reports drug-induced liver injury (DILI) associated with RAD-140: Barbara et al. (2020) and Niazi et al. (2025). The second one describes cholestatic pattern — damage consisting in impaired bile outflow, with increased alkaline phosphatase and bilirubin, treated with corticosteroids. The hepatotoxicity signal is a documented point of concern, not a hypothesis. However, this remains at the level of case reports, not controlled studies.

What is the difference between a cholestatic pattern and a hepatocellular pattern?
The hepatocellular pattern is direct damage to liver cells with a predominant increase in transaminases (ALT, AST). The cholestatic pattern is a disorder of bile outflow with a predominant increase in alkaline phosphatase (ALP) and bilirubin. The distinction is clinically important because drug-induced cholestasis can be persistent and resolves more slowly.

Is “the most powerful SARM” a fact?
NO. It’s a marketing narrative. Comparisons of \”potency\” are based on parameters dependent on the experimental model and endpoint, and direct comparisons in humans under controlled conditions have not been performed (Bond et al. 2025).

What does “neuroprotection” mean in the context of RAD-140?
It only means what has been reported in a specific model: an androgen receptor-mediated reduction in neuronal death was observed in neuronal cultures and in kainic acid-lesioned rats (Jayaraman et al. 2014). This is not evidence of effect in humans and does not support any claims about effects on brain health.

What does breast cancer research mean?
In a preclinical model of breast cancer expressing androgen and estrogen receptors (AR+/ER+), inhibition of tumor cell growth mediated by the androgen receptor, acting as an alternative pathway to suppress estrogen signaling, has been reported (Yu et al. 2017). This is a preclinical and exploratory result. It does not indicate efficacy or safety in human oncology.

Is RAD-140 banned in sports?
Yes. WADA classifies it in a category S1 (anabolic agents), with the prohibition in force at all times. LC-MS/MS methods allow the detection of the compound and its metabolites in urine (Thevis and Schänzer 2018).

Why do HPLC purity and COA matter?
Because the analysis of \”SARM\” products from the Internet showed that a significant part of them did not contain the declared substance, some contained other unapproved compounds, and the content differed from the label (Van Wagoner et al. 2017). Without confirmed identity (MS) and purity (HPLC >=98%) and a certificate of analysis assigned to the batch, the material is not suitable for reliable testing.

Does a capsule mean it’s a supplement?
NO. The character is not a regulatory class. The capsule is only a form of packaging research material. RAD-140 remains a Research Use Only reagent and is not intended for consumption.

How to store the reagent?
In the original packaging, in a dry and cool place, away from light and moisture – in accordance with the batch documentation and internal procedures of the research facility. The capsule form does not require a cold chain.

Are there phase III clinical trials for RAD-140?
NO. The evidence base is based on preclinical models and case reports. Registration studies have not been completed and there is no data on long-term consequences (Bond et al. 2025; Leciejewska et al. 2024).

More in the knowledge base: the RAD-140 (Testolone) category and a profile article on RAD-140.

Scientific sources

1. Miller CP et al. (2011). Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140
2. Jayaraman A et al (2014). Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats
3. Yu Z et al. (2017). Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer
4. Barbara M et al (2020). Drug-Induced Liver Injury Associated With Alpha Bolic (RAD-140) and Alpha Elite
5. Niazi B et al. (2025). Cholestatic Drug-Induced Liver Injury From Rad-140 Successfully Treated With Corticosteroids
6. Solomon ZJ et al. (2019). Selective Androgen Receptor Modulators: Current Knowledge and Clinical Applications
7. Narayanan R, Coss CC, Dalton JT (2018). Development of selective androgen receptor modulators (SARMs)
8. Bond P et al (2025). Selective androgen receptor modulators: a critical appraisal
9. Leciejewska N et al. (2024). Selective androgen receptor modulator use and related adverse events
10. Thevis M, Schänzer W (2018). Detection of SARMs in doping control analysis
11. Van Wagoner RM et al. (2017). Chemical Composition and Labeling of Substances Marketed as Selective Androgen Receptor Modulators and Sold via the Internet
12. Joshi A et al (2025). Self-Reported Effects and Adverse Events Associated With Selective Androgen Receptor Modulators