RAD-140 (Testolone): Scientific Profile
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Non-steroidal selective androgen receptor modulator (SARM) with high affinity for the androgen receptor, investigated for its anabolic selectivity in musculoskeletal and bone tissue.
RAD-140, commonly called Testolone in research settings, is a selective androgen receptor ligand (SARM) developed to mimic the anabolic effects of endogenous androgens without the systemic side effects associated with synthetic steroids. Its non-steroidal chemical structure confers a high affinity for the androgen receptor (AR), demonstrating an anabolic-androgenic ratio of approximately 90:1 in preclinical models, which suggests significant potential for research on the preservation of lean mass.
In laboratory models, the compound has shown a unique capacity to selectively activate muscle and bone tissue, minimizing the activation of accessory organs such as the prostate or the sebaceous glands. This selectivity is of particular interest in studies on sarcopenia and cachexia, where the aim is to reverse muscle atrophy without inducing virilization or prostatic hypertrophy. In addition to its effects on protein anabolism, RAD-140 has been the subject of study for its possible neuroprotective effects, since androgen receptors in the brain play a critical role in neuronal health against degenerative processes.
Current research with RAD-140 focuses on evaluating its pharmacokinetics and its impact on bone mineralization and the hypertrophy of fast-twitch fibers. Since it is not a substrate for the 5-alpha reductase enzyme or for aromatase, research subjects do not present conversion to dihydrotestosterone (DHT) or to estrogenic metabolites, simplifying the analysis of the results in protocols of pure androgenic signaling.
Mechanism of action
RAD-140 acts as a high-affinity agonist ligand of the androgen receptor (AR). Upon binding to the receptor, it induces conformational changes that favor the recruitment of coactivators specific to muscle and bone tissue. Unlike testosterone, RAD-140 is neither reduced to DHT nor aromatized to estradiol, allowing for selective androgenic modulation. In neurons, a protective effect against apoptosis induced by chemical insults has been documented, mediated by the MAPK/ERK signaling pathway.
Mechanism summary
Selective androgen receptor agonist that promotes tissue-specific anabolism in muscle and bone without conversion to estrogenic metabolites or dihydrotestosterone.
Clinical Studies (7)
- Selective androgen receptor modulator abuse-induced heart failure: catastrophic effects of RAD-140 (Testolone) (Skorupski WJ et al. · Polish archives of internal medicine · 2024) PMID 38864168.
- RAD-140 Drug-Induced Liver Injury (Leung K et al. · Ochsner Journal · 2022) PMID 36561105.
- Acute Myocarditis From the Use of Selective Androgen Receptor Modulator (SARM) RAD-140 (Testolone) (Padappayil RP et al. · Cureus · 2022) PMID 35233331.
- Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor-Positive Breast Cancer Models with a Distinct Mechanism of Action (Yu, Z, et al. · Clinical Cancer Research · 2017) PMID 28974548.
- Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats (Jayaraman, A, et al. · Endocrinology · 2014) PMID 24428527.
- A First-in-Human Phase 1 Study of a Novel Selective Androgen Receptor Modulator (SARM), RAD140, in ER+/HER2- Metastatic Breast Cancer (LoRusso, P, et al. · Clinical Breast Cancer · 2022) PMID 34565686.
- Preclinical assessment of the selective androgen receptor modulator RAD140 to increase muscle mass and bone mineral density (Puskas, J, et al. · Physiological Reports · 2025) PMID 40680216.
Warnings
RAD-140 (Testolone) is a research-use-only (RUO) compound; the following warnings and handling considerations apply to its laboratory use:
- Product exclusively for use in laboratory settings
- Requires monitoring of hepatic parameters and lipid profiles
- Handle using appropriate personal protective equipment
- Research models with preexisting hepatic pathologies
- Subjects with androgen-sensitive prostate or breast carcinoma
- Protocols requiring stable natural LH and FSH levels
- Presence of severe dyslipidemia in the study subject
Technical data
- CAS
- 1182367-47-0
- Molecular formula
- C20H16ClN5O2
- Molecular weight
- 393.83 Da
- Compound type
- sarm
- Storage
- 15-30°C (cool, dry place)
- Shelf life (lyophilized)
- 36 months
- Shelf life (reconstituted)
- Not applicable (oral presentation)
- Light-sensitive
- No
Available for research
RAD-140 (Testolone) is available as a research reagent (RUO):
Frequently asked questions about RAD-140 (Testolone)
What is RAD-140 (Testolone)?
Non-steroidal selective androgen receptor modulator (SARM) with high affinity for the androgen receptor, investigated for its anabolic selectivity in musculoskeletal and bone tissue.
What is the mechanism of action of RAD-140 (Testolone)?
Selective androgen receptor agonist that promotes tissue-specific anabolism in muscle and bone without conversion to estrogenic metabolites or dihydrotestosterone.
What is RAD-140 (Testolone) researched for?
In preclinical research, RAD-140 (Testolone) is studied mainly in: Research on the increase in protein synthesis in lean tissue; Study of the improvement in bone mineral density; Modulation of muscle strength in atrophy models. Material exclusively for scientific research.
What are the chemical properties of RAD-140 (Testolone)?
Molecular formula C20H16ClN5O2; molecular weight 393.83 Da; CAS number 1182367-47-0.
How is RAD-140 (Testolone) stored?
Storage conditions: 15-30°C (cool, dry place); lyophilized stability: 36 months; once reconstituted: Not applicable (oral presentation).
What routes of administration are studied for RAD-140 (Testolone)?
In research models the following are described: Oral. Use is exclusively for scientific research.