RAD140 Capsule is an oral formulation of the selective androgen receptor modulator (SARM) Testolone, encapsulated for convenient dosing. Like its liquid counterpart, it selectively binds to androgen receptors in muscle and bone tissue, promoting anabolic effects such as increased lean muscle mass, strength, and recovery without the androgenic side effects associated with traditional steroids.
Capsules offer precise dosing and improved stability compared to liquid solutions, making them a preferred choice for research or experimental use. this is studied for potential applications in muscle-wasting diseases (e.g., cancer cachexia) and osteoporosis, though it remains unapproved for medical use. Athletes and bodybuilders sometimes use it off-label for performance enhancement, despite its prohibition by WADA.
Common side effects may include mild testosterone suppression, headaches, or fatigue, typically requiring post-cycle therapy (PCT) to restore natural hormone levels. Due to limited long-term safety data, caution is advised with its use. They are typically sold as "research chemicals" and not for human consumption.
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RAD140 COA
Core Biological Activity: Targeting Anabolic Effects on Muscles and Bones
RAD140 Capsule, as a non-steroidal selective androgen receptor modulator (SARM), exhibits unique properties in terms of biological activity, pharmacokinetic characteristics, application fields, and safety when in capsule form. The following provides an analysis from multiple dimensions:
This specifically binds to androgen receptors in skeletal muscles and bone tissues, triggering protein synthesis signaling pathways and promoting muscle growth and increased bone density. Its anabolic-to-androgenic ratio is 90:1, meaning that while significantly enhancing muscle mass, it has a very weak activating effect on sexual tissues such as the prostate and gonads, avoiding the side effects of traditional steroids such as testicular atrophy and clitoral enlargement.
Animal experiments show that it can increase the metabolic rate of muscle cells and indirectly accelerate fat breakdown. For example, monkeys gained over 10% in weight during a 28-day treatment period, with no significant increase in fat percentage, indicating that its muscle-building effect does not accompany fat accumulation.
Preclinical studies have shown that RAD140 can inhibit neuronal cell apoptosis and has potential therapeutic value for neurodegenerative diseases such as Alzheimer's disease and stroke. Its mechanism may be related to regulating the activity of glutamate receptors (such as glycine receptors), reducing excitotoxic damage.
Pharmacokinetic Characteristics: Optimizing Absorption and Stability
Oral Bioavailability
The design of RAD140 capsules needs to address the common first-pass effect problem of SARM compounds. Through micro-powdering technology or nano-crystal carriers, the solubility and absorption rate of the drug in the gastrointestinal tract can be significantly improved. For example, a certain enterprise used a wet granulation process to make the capsules have an in-solution degree of over 90% (within 10 minutes) in simulated gastric fluid.
Half-life and Dosage Frequency
The half-life of this is approximately 24 hours, supporting a once-daily dosing regimen.
The capsule formulation can further extend the drug release time through sustained-release coating technology, maintaining stable blood drug concentration and reducing fluctuations-related side effects (such as headache and insomnia).
Stability Optimization
The capsule shell material (such as hydroxypropyl methylcellulose) can effectively block light and oxygen, preventing RAD140 from undergoing photolysis or oxidation degradation during storage.
In the 40°C/75%RH accelerated test, the content of high-quality capsule products decreased by ≤5%/6 months, meeting the ICH stability guidelines.
Application Areas: Cross-Expansion from Medicine to Sports
Treatment of Muscular Atrophy-related Diseases
RAD140 capsules have been explored for use in cancer cachexia, sarcopenia, and chronic obstructive pulmonary disease leading to muscle loss. Phase I clinical trials showed that breast cancer patients gained 3.2% of lean body mass after medication.
Enhancement of Athletic
In the bodybuilding and training fields, they are favored for their significant improvement in muscle endurance and reduction in recovery time. User feedback indicates that a 5-10 kg increase in lean body mass can be achieved within an 8-12 week cycle.
Safe Use for Women
Due to its weak activation effect on sexual tissues, this is considered safer for women. The recommended dose is half of that for men, avoiding the appearance of male characteristics (such as hirsutism, deepening of voice).
Safety and Side Effect Management
Known Side Effects
Short-term: Mild headache, insomnia (occurrence rate about 5-8%), possibly related to glutamate receptor regulation.
Long-term: Currently, there is no human data to support liver toxicity or cardiovascular risks, but animal experiments suggest that attention should be paid to lipid fluctuations (such as increased LDL).
Risk Control Strategies
Dose Limitation: It is recommended not to exceed 30 mg per day to avoid receptor desensitization.
Cycle Management: Continuous use should not exceed 12 weeks, followed by PCT (post-circulation therapy) to restore endogenous testosterone levels.
Contraindications: Patients with prostate cancer, breast cancer (hormone receptor positive type) are prohibited from using.
Market and Regulatory Status
Legal status
RAD140 has not been approved by the FDA for use in humans. Currently, it is only used for researching the circulation of chemicals. In China, it is listed as a substance in the stimulant directory, and illegal production and sales may involve criminal liability.
Quality control standards
Compliant products must meet the following requirements:
Purity ≥ 98% (detected by HPLC);
Heavy metals (Pb, As) ≤ 0.005mg/kg;
Microbial limit (total bacterial count < 100 CFU/mL).
Female Users: Androgenization Risk and Dose Sensitivity
Androgenization Side Effects
Although RAD140 is marketed as "without androgenic activity", female users may still experience androgenization symptoms due to individual sensitivity, such as hair loss, deepening voice, and enlargement of the clitoris. Case studies show that a female user experienced weakness and fatigue after using 15mg/day, and the symptoms improved after reducing the dosage to 5-10mg/day. This indicates that females have a significantly higher dose sensitivity to it than males, and strict adherence to low-dose principles is necessary.
Endocrine Inhibition Risk
RAD140 may inhibit the hypothalamus-pituitary-testis axis (HPTA) and cause a decrease in testosterone levels, resulting in menstrual disorders or reduced sexual desire in female users. Studies show that a 17mg/day dose over 12 weeks can reduce male testosterone levels from 750ng/dL to 193ng/dL. Although there are no direct data for female users, caution should be exercised regarding similar endocrine interference.
Children and Adolescents: Growth Plate Closure and Development Risks
Growth Plate Closure Risk
RAD140 promotes skeletal muscle growth while potentially accelerating the closure of growth plates, resulting in limited height growth in children. Animal experiments show that this significantly increases lean body mass in monkeys, but children's bone development is not yet complete, and such intervention may cause irreversible physiological changes.
Psychological and Behavioral Effects
Adolescents using RAD140 may experience mood instability, increased aggression, or depressive tendencies due to hormonal fluctuations.
In a case study, a user reported experiencing irritability after using the drug, and caution should be exercised regarding the long-term impact of such side effects on the mental health of adolescents.
Patients with Liver and Kidney Dysfunction: Metabolic Burden and Toxicity Accumulation
Liver Toxicity Risk
The oral route of RAD140 requires metabolism by the liver, which may increase the burden on liver function. A 49-year-old male developed cholestatic liver injury after using it for 4 weeks, suggesting that patients with liver diseases or abnormal liver function have a significantly increased risk of using it. It is recommended that such individuals avoid using it or have their ALT/AST enzyme levels tested every 4 weeks during use.
Renal Excretion Pressure
Although there are no direct reports of renal toxicity, the metabolites of it may be excreted through the kidneys.
Patients with renal dysfunction should use it with caution. Long-term high-dose use may exacerbate renal burden, leading to electrolyte imbalance or edema.
Preparation of synthetic logic
RAD140, Chemical name: 2- (8- (6- (4-cyanophenyl) -1,2-benzisoxazole-3-yl) -3-azabicyclo [3.2.1] oct-3-yl) acetamide, belongs to the non steroidal SARM class of compounds. The following is the mainstream classical synthesis logic and segmented theoretical route in the literature, only used for scientific research mechanism exploration.
Pre construction method of benzimidazole parent nucleus (a common route in mainstream literature)
This scheme uses 4-cyanobenzoic acid derivatives as the initial starting material, and constructs a core heterocyclic skeleton of 1,2-benzimidazole through condensation and cyclization reactions. Firstly, oxime intermediates are obtained through acylation and hydroxylamine condensation, and then intramolecular cyclization is completed under weakly alkaline catalytic conditions to form a stable aromatic heterocyclic structure and lock in the key pharmacophore of the molecule.
After halogenated activation, heterocyclic intermediates obtain active sites that can undergo coupling reactions, providing a reaction basis for the subsequent splicing of bicyclic amine structures. The advantage of this synthesis sequence lies in the high stability of the parent ring, easy separation and purification of intermediate products, and suitability for small-scale laboratory synthesis research.
Cardiovascular Disease Patients: Lipid Fluctuations and Atherosclerosis
Dyslipidemia
This has a dose-dependent effect on cholesterol, potentially reducing HDL (beneficial cholesterol) levels and increasing LDL (harmful cholesterol) levels, thereby increasing the risk of atherosclerosis.
A user reported a sudden increase in blood pressure after using the drug, which may be related to the reduction of HDL caused by liver lipase stimulation.
Hypertension Risk
RAD140 lacks aromatization (conversion to estrogen) ability, which may reduce the protective effect of estrogen on the cardiovascular system.
Cardiovascular disease patients using this should closely monitor blood pressure and avoid using it simultaneously with antihypertensive drugs to prevent hypotension.
Pregnant and Lactating Women: Fetal/Infant Exposure
Fetal Development Risk
RAD140 may affect fetal development through the placental barrier. Animal experiments show that it may alter sex hormone levels, leading to abnormal fetal reproductive systems.
Pregnant women should absolutely avoid using it, and lactating women using it may affect infants through breast milk, and should suspend breastfeeding.
Long-term Reproductive Impact
The inhibition of the HPTA by this drug may affect female ovarian function, leading to ovulatory disorders or menstrual disorders.
Women planning to conceive should undergo hormone level testing at least 3 months after discontinuation to ensure endocrine recovery.
Frequently Asked Questions
What does RAD140 do to the brain?
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In cultured hippocampal neurons, RAD140 was as effective as testosterone in reducing cell death induced by apoptotic insults. Mechanistically, RAD140 neuroprotection was dependent upon MAPK signaling, as evidenced by elevation of ERK phosphorylation and inhibition of protection by the MAPK kinase inhibitor U0126.
Does RAD140 increase estrogen?
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In addition, due to its nonsteroidal structure, the SARM RAD140 is not subject to further conversion to estrogens by CYP19 aromatase, or to DHT by 5α-reductase, thus reducing the potential risk of stimulating ER+ tumor growth or increasing virilization.
How bad is RAD140 for the liver?
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The case illustrates that healthcare providers should be aware that nonmedical supplement use like RAD-140 can cause severe hepatotoxicity, and developing acute liver failure necessitating liver transplantation is always a possibility.
How long does RAD 140 stay in your system?
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Using liquid chromatography – electrospray mass spectrometry in negative ionization mode, unchanged RAD140 can be detected in urine at least 8 days after administration of a single oral dose of 10 mg.
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