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Pure RAD140 powder is a non-steroidal selective androgen receptor modulator (SARM) used primarily in studies of muscle growth and physical performance enhancement. Its chemical name is 2-chloro-4-[[(1R,2S)-1-[5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl]-2-hydroxypropyl]amino]-3-methylbenzonitrile with the molecular formula C20H17ClN6O2 and molecular weight 408.84 g/mol. It appears as a white to off-white crystalline powder with the melting point of about 160-165°C. It needs to be stored in a sealed place away from light. It should be stored in a dry environment at -20°C, protected from light and sealed.
It promotes muscle synthesis through selective activation of the androgen receptor, while reducing side effects such as prostate or body hair growth. It has been shown to have anti-catabolic properties and may be useful in muscular dystrophy research. The pure powder form requires solubilization in DMSO or ethanol and is highly bioavailable, but no human safety data are available and use is limited to laboratory studies. Strict safety protocols should be followed for use and direct contact should be avoided.
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RAD140 COA
Basic Chemical Information
Molecular Formula and Molecular Weight:
Molecular Formula: C₂₀H₁₆ClN₅O₂
Molecular Weight: 393.826 g/mol
The molecular structure of this molecule contains:
One chlorine atom (Cl), one cyanide group (-CN), an oxadiazole ring, and a hydroxypropyl side chain, which endows it with unique chemical stability and biological activity.
CAS Number:
The CAS number serves as the unique identifier for chemical substances, ensuring the precise tracking and compliant use of pure RAD140 powder in research and industry:1182367-47-0
Synonyms and aliases-Testolone,RAD-140,2-chloro-4-[[(1R,2S)-1-[5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl]-2-hydroxypropyl]amino]-3-methylbenzamide
These names reflect the chemical structure characteristics and brand naming in commercial applications of the substance.
Physical and Chemical Properties
Appearance and Properties&Solubility
White powder
High-purity this typically presents as a fine, non-crystalline powder, facilitating precise weighing and dissolution operations in research.
Slightly soluble in chloroform, DMSO
It requires ultrasonic treatment or heating assistance for dissolution, often used in preparing solution systems for cell experiments or animal models.
Melting Point and Boiling Point&Density
Melting Point: 179-183°C
Boiling Point: 687.7±65.0°C (predicted value)
The high melting point indicates the stability of its crystal structure, while the high boiling point suggests that it is not easily volatile under routine experimental conditions, making it suitable for long-term storage.Density: 1.41±0.1 g/cm³ (predicted value);Refractive Index: 1.652;The density data is helpful for optimizing the compression molding process of the powder, while the refractive index can be used in optical property research in materials science.
Acidity Coefficient (pKa)&Storage conditions
pKa: 13.76±0.20 (predicted value)
The strong basic environment (pKa > 12) indicates that the molecule is prone to carry a negative charge under physiological pH, which may affect the binding affinity with target receptors.
-20°C cryopreservation.
A low-temperature environment can inhibit oxidative degradation, extend the shelf life (usually 2-3 years), and prevent the formation of lumps or loss of activity due to repeated freezing and thawing.
Chemical Stability and Reactivity
Thermal stability
Below the boiling point (< 687.7°C), it remains chemically inert, but at high temperatures it may decompose to produce hydrogen chloride.
Light stability
The white powder has a low sensitivity to visible light, but long-term exposure to ultraviolet light may lead to the hydrolysis of the cyano group (-CN).
Redox activity
The hydroxy and cyano groups in the molecule may participate in redox reactions, and it is necessary to avoid coexistence with strong oxidants.
pH sensitivity
Under extreme acidity (pH < 2) or alkalinity (pH > 12), the oxadiazole ring may open, resulting in structural disruption and loss of activity.
Biochemical Characteristics
Selective Androgen Receptor Modulator Mechanism
It binds to the androgen receptor with high affinity, activating the AR signaling pathway in muscle, promoting protein synthesis and increasing bone density, while avoiding side effects on the prostate and sebaceous glands.
Metabolic Stability
The non-steroidal structure makes it less susceptible to 5α-reductase or aromatase metabolism, and its oral bioavailability is significantly higher than traditional steroids (such as testosterone).
Pharmacokinetic Parameters
Half-life: approximately 24 hours, supporting a once-daily dosing regimen.Distribution Volume: The high lipid solubility enables it to easily penetrate cell membranes, with a higher concentration accumulated in muscle tissue than in plasma.
Safety and Handling Guidelines
01.Toxicity Data
LD₅₀ (rat, oral): Not disclosed, but preclinical studies show that its therapeutic index (TI) is significantly higher than testosterone, suggesting a lower acute toxicity risk.
Long-term toxicity: No significant organ damage was observed in the 28-day rat experiment, but its carcinogenicity or reproductive toxicity needs further verification.
02.Operational protection
Personal Protective Equipment (PPE): Laboratory coat, goggles, N95 mask, nitrile gloves.
Waste Disposal: Classified as "non-hazardous chemicals" by the EPA, but it should not be directly discharged into the sewer. It is recommended to destroy it through high-temperature incineration (> 800°C).
03.Emergency Measures
Inhalation: Transfer to fresh air and keep the respiratory tract unobstructed.
Skin Contact: Wash with soap and water for 15 minutes, seek medical attention if necessary.
Leakage Handling: Absorb with inert materials (such as vermiculite) to avoid dust.
Applications and Research Directions
Muscle Atrophy Treatment:Preclinical studies show that it can reverse cancer cachexia or age-related muscle loss, and potential indications include chronic obstructive pulmonary disease (COPD) and AIDS-related wasting syndrome.
Osteoporosis:Pure RAD140 powder can increase bone density and reduce fracture risk, especially for postmenopausal women.
Enhanced Athletic Performance:Although listed as a prohibited substance by the World Anti-Doping Agency (WADA), its selective action mechanism still attracts illegal use by fitness enthusiasts, and enhanced regulation and public education are needed.
Breast Cancer Adjuvant Therapy:As an androgen receptor agonist, it can inhibit the proliferation of estrogen receptor-positive (ER+) breast cancer cells. Currently, it is in phase I clinical trials (NCT03901419).
Mechanism of Light Stability: Molecular Structure and Photodegradation Risk
The molecular structure of pure RAD140 powder (chemical formula: C₂₀H₁₆ClN₅O₂) includes the following key features that directly affect its light stability:
Cyano(-CN) and chlorine atom (Cl):
The cyano group acts as a strong electron-withdrawing group and may participate in photolysis reactions through an electron transfer mechanism. Experimental data show that under ultraviolet light (UV-C band, 200-280 nm) irradiation, the cyano group may undergo hydrolysis, generating carboxylic acid derivatives (such as benzoic acid derivatives), resulting in a decrease in the content of active ingredients. Although the chlorine atom is itself stable, it may intensify the photoactivity of the cyano group through an induction effect.
Oxadiazole ring:
This conjugated ring structure may undergo electronic transition under light, absorbing ultraviolet light energy and triggering a ring-opening reaction, generating chain compounds. Although the thermal stability of the oxadiazole ring is relatively high (melting point 179-183°C), the risk of photolysis still needs to be vigilant.
Hydroxypropyl side chain:
The hydroxyl group (-OH) may stabilize the molecule through hydrogen bonding, but long-term exposure to light may lead to oxidation of the side chain, generating carbonyl compounds (such as aldehydes or ketones), affecting biological activity.
Photolysis experiment data: Stability quantitative assessment
Light-protected vs. unprotected storage
Light-protected storage: In brown glass bottles or aluminum foil bags, the powder has a stable content (≥99%) for 2 years, with impurities (such as cyano group hydrolysis products) content <0.1%.
Unprotected storage: After being exposed to indoor light (about 500 lux) for 6 months, the content decreased by approximately 5%, and the impurity content increased to 1.2%; exposed to a UV lamp (365 nm, 10 W) for 24 hours, the content decreased by 15%, and the impurity content reached 3.5%.
Photolysis kinetics model
According to first-order reaction kinetics, the degradation rate constant (k) of this under ultraviolet light is approximately 0.006 h⁻¹, and the half-life (t₁/₂) is about 115 hours. Under light-protected conditions, the k value can be reduced to <0.0001 h⁻¹, and the half-life is extended to >7000 hours.
The necessity of light-protected storage: From laboratory to industrial application
Laboratory research scenario
Weighing and dissolution: During operation, it is necessary to complete quickly in the dark or under a yellow light to avoid prolonged exposure of the powder to light.
Solution stability: Dissolved in DMSO, the solution stored under light-protected conditions can maintain activity for 1 month at -20°C, while the un-protected solution loses 20% of its activity within 7 days.
Industrial production and storage
Raw material storage: It is recommended to use brown glass bottles or aluminum foil bags for packaging, stored in a -20°C freezer environment, avoiding repeated freezing and thawing.
Long-term stability: Under light-protected, dry (humidity < 40%), and low-temperature conditions, the shelf life of its powder can reach 3 years; if not protected from light, the shelf life is shortened to 6-12 months.
Development challenges of formulations
Transdermal patches: UV absorbers (such as titanium dioxide) need to be added to enhance photostability to ensure consistent drug release under light.
Nanocrystal formulations: Through surface coating technology (such as polyethylene glycol modification), the risk of photolysis can be reduced, but a balance must be achieved between solubility and stability.
Strategies for optimizing photostability: From molecular modification to packaging innovation
New packaging materials
Multi-layer composite film: Using the PET/Al/PE (polyester/aluminum/polyethylene) structure can block 99.9% of ultraviolet light, extending the shelf life of the powder to 5 years.
Smart label: Integrating photo-sensitive color-changing indicators, when the light intensity inside the packaging exceeds the safety threshold, the label color changes to indicate the need to replace the packaging.
Storage Condition Monitoring
Internet of Things sensors:Embed light intensity sensors in storage containers to monitor real-time light exposure data and issue alerts for abnormal exposure incidents through the cloud platform.Blockchain traceability: Record the entire chain of light exposure data of the powder from production to use to ensure traceability of quality.
FAQ
Yes, RAD-140 (Testolone) is hepatotoxic and can cause severe drug-induced liver injury (DILI). While marketed as a safer alternative to anabolic steroids, evidence indicates it can lead to cholestatic liver injury (bile buildup) and elevated liver enzymes, with cases of jaundice and severe liver damage reported in users.
RAD-140 (Testolone) is an investigational Selective Androgen Receptor Modulator (SARM) designed for treating muscle wasting, bone loss, and specific breast cancers. While popular among bodybuilders for promoting rapid muscle growth and fat loss, it is not FDA-approved, carries high risks of severe liver injury, and is banned by WADA.
In a study in rats, RAD-140 activates receptors in regions of the brain that are injured. This triggers a signal called the MAPK pathway that helps protect cells against injury from amyloid beta. Additionally, RAD-140 and testosterone were equally effective at protecting against neurotoxins [R].
RAD-140 (Testolone) is not necessarily "stronger" than testosterone in absolute terms, but it is a highly potent and selective SARM (Selective Androgen Receptor Modulator) designed to mimic testosterone's anabolic effects on muscle and bone while limiting androgenic effects on other tissues like the prostate. It acts as an agonist, stimulating anabolic tissues similarly to testosterone, and is sometimes described as having a higher affinity for androgen receptors.
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