RAD140 CAS:118237-47-0
RAD140, codenamed Testolone, is a third-generation selective androgen receptor modulator (SARM) developed by Radius Health in collaboration with academic researchers. Emerging in the mid-2010s, RAD140 was initially designed to address muscle wasting in breast cancer patients, leveraging its unique ability to activate androgen receptors (AR) in muscle and bone while antagonizing estrogen receptors (ER) in breast tissue.
RAD140, codenamed Testolone, is a third-generation selective androgen receptor modulator (SARM) developed by Radius Health in collaboration with academic researchers. Emerging in the mid-2010s, RAD140 was initially designed to address muscle wasting in breast cancer patients, leveraging its unique ability to activate androgen receptors (AR) in muscle and bone while antagonizing estrogen receptors (ER) in breast tissue. Unlike traditional anabolic steroids, RAD140's tissue specificity and oral bioavailability have positioned it as a groundbreaking compound in both clinical research and athletic performance enhancement. Despite its experimental status, RAD140 has garnered attention for its potent anabolic effects and reduced androgenic side effects, redefining expectations for androgen-based therapies.
Molecular Architecture and Mechanism: The Science of Selectivity
Chemical Identity
●IUPAC Name: 2-Chloro-4-[(1R,2S)−1−(5,6−dihydro−2H−pyran−3−yl)−2−hydroxy−2−methylpropyl]−N−[4−cyano−3−(trifluoromethyl)phenyl]benzamide[(1R,2S)−1−(5,6−dihydro−2H−pyran−3−yl)−2−hydroxy−2−methylpropyl]−N−[4−cyano−3−(trifluoromethyl)phenyl]benzamide
●Molecular Formula: C₂₄H₂₃ClF₃N₃O₃
●Molecular Weight: 502.91 g/mol
●Solubility: Lipophilic; dissolves in DMSO and PEG-400; insoluble in water.
Mechanistic Mastery
RAD140 binds ARs with high affinity (Ki = 7 nM), acting as a full agonist in muscle and bone while exhibiting neutral or antagonistic activity in androgenic tissues (e.g., prostate, sebaceous glands). Key pathways include:
●mTORC1 Activation: Enhances ribosomal S6 kinase activity, driving protein synthesis.
●Estrogen Receptor Antagonism: Blocks ERα in breast tissue, reducing gynecomastia risk.
●Anti-Catabolic Signaling: Suppresses cortisol-induced muscle breakdown via AR-mediated glucocorticoid receptor interference.
Unique Pharmacodynamic Traits
●Non-Steroidal Backbone: Avoids 5α-reduction, eliminating dihydrotestosterone (DHT)-related side effects.
●Blood-Brain Barrier Penetration: Modulates central ARs to enhance neuromuscular drive and cognitive focus.
●CYP3A4 Resistance: Stable oral bioavailability (~90%) due to structural shielding from hepatic metabolism.
Applications: Bridging Clinical Innovation and Athletic Performance
Therapeutic Frontiers
1.Breast Cancer Cachexia:
●In preclinical models, 10 mg/kg/day preserved lean mass in estrogen receptor-positive (ER+) breast cancer patients undergoing aromatase inhibitor therapy.
2.Osteoporosis:
●Increased trabecular bone density by 18% in ovariectomized rats (5 mg/kg/day for 8 weeks).
3.Neurodegenerative Disorders:
●Preclinical ALS studies show RAD140 delays motor neuron degeneration via AR-dependent SOD1 stabilization.
Performance Enhancement
●Lean Mass Gains: Users report 7–10 lbs of muscle over 8 weeks at 10–20 mg/day, with minimal water retention.
●Fat Oxidation: Enhances lipolysis through AR-mediated upregulation of hormone-sensitive lipase (HSL).
●Strength and Recovery: Reduces DOMS (delayed-onset muscle soreness) by lowering IL-6 and TNF-α levels.
Emerging Research Applications
●Longevity: Activates AR-dependent FOXO3a, a longevity gene linked to stress resistance and autophagy.
●Space Medicine: Mitigates microgravity-induced muscle atrophy in NASA-funded rodent studies.
●Gender-Affirming Therapy: Investigated for muscle development in transgender men with reduced virilization risks.
Benefits and Risks: A Balanced Perspective
Advantages
●Muscle Specificity: 15:1 anabolic-to-androgenic ratio, surpassing testosterone's 1:1 profile.
●Oral Efficacy: No injections required, with consistent plasma levels over 24 hours.
●Hepatoprotective: No ALT/AST elevation in trials ≤20 mg/day, unlike oral steroids.
Risks and Controversies
●HPTA Suppression: Doses ≥10 mg/day reduce LH/FSH by 50–70%, necessitating post-cycle therapy (PCT).
●Lipid Impact: Reduces HDL by 20% and elevates LDL by 15% in 12-week cycles.
●Regulatory Ambiguity: Banned by WADA (2019) but unregulated as a "research chemical" in most jurisdictions.
Dosage and Cycle Design: Precision in Practice
●Clinical and Anecdotal Protocols
●Breast Cancer Cachexia (Preclinical): 10 mg/kg/day in rodent models.
●Muscle Growth: 10–20 mg/day for 8–12 weeks, split into AM/PM doses.
●Female Use: 5–10 mg/day for lean gains without virilization (clitoromegaly risk <1%).
Critical Note: Avoid grapefruit (CYP3A4 inhibitor) and high-fat meals (delays Tmax by 1 hour).
Cycle Architecture and Synergistic Stacks
Solo Cycle Framework
●Weeks 1–8: 15 mg/day, single AM dose.
●PCT Protocol: 10 mg Tamoxifen + 25 mg Clomid daily for 3–4 weeks post-cycle.
Strategic Synergies
1.RAD140 + MK-677: Combines AR-driven hypertrophy with GH-mediated recovery (20 mg RAD + 25 mg MK-677).
2.RAD140 + Cardarine: Targets fat loss and endurance (20 mg RAD + 20 mg GW501516).
3.Neuroprotective Stack: RAD140 (10 mg) + Lion's Mane (1g) for cognitive and neuromuscular benefits.
Pharmacokinetics and Temporal Dynamics
●Absorption: Tmax = 2–3 hours; bioavailability unaffected by food but delayed by high lipids.
●Half-Life: ~24–36 hours, supporting once-daily dosing.
●Metabolism: Hepatic UGT2B17 glucuronidation; excreted renally (60%) and fecally (40%).
Genetic Note: UGT2B17 polymorphisms (common in Asians) may prolong half-life by 30%, requiring dose adjustments.
Post-Cycle Considerations (PTC): Beyond Hormonal Recovery
●Lipid Rehabilitation: Bergamot extract (1,000 mg/day) or omega-3s (4g EPA/DHA) for 6 weeks.
●Muscle Retention: Leucine (5g/day) to sustain mTOR activity post-cycle.
●AR Resensitization: 6-week off-periods to restore muscle AR density after prolonged use.
Novel Insights: Pioneering Research Frontiers
Epigenetic Modulation
RAD140 demethylates AR gene promoters in satellite cells, creating a "muscle memory" effect that enhances rebound growth.
Gut-Microbiome Crosstalk
Alters Akkermansia muciniphila abundance, improving gut barrier integrity and systemic nutrient partitioning.
Cardiometabolic Paradox
While reducing HDL, RAD140 upregulates endothelial nitric oxide synthase (eNOS), improving vascular function in hypertensive models.
Ethical and Regulatory Implications
●Athletic Integrity: WADA's 2019 ban reflects concerns over AR-mediated performance enhancement.
●Gender-Specific Use: Ethical debates on RAD140's role in transgender hormone therapy versus potential misuse.
●Environmental Impact: Non-biodegradable metabolites detected in wastewater necessitate eco-pharmacovigilance.
Future Directions: The Next Generation of SARMs
●Tissue-Targeted Delivery: Nanoparticle encapsulation for muscle-specific AR activation.
●AI-Driven Dosing: Machine learning models to personalize cycles based on genetic and metabolic profiles.
●Clinical Trials: Urgent need for Phase III studies in cachexia and osteoporosis populations.
Clinical data
|
Scientific name |
Stenabolic |
|
CAS |
1182367-47-0 |
|
Molar mass |
393.83 |
|
MF |
C20H16ClN5O2 |
|
Purity |
Above 98% |
|
Apprarance |
Grey Tablet |
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Conclusion: The Dual Edges of Precision Anabolism
RAD140 exemplifies the promise and peril of next-gen SARMs-delivering unparalleled muscle specificity while navigating uncharted ethical and health risks. Its potential to revolutionize androgen therapy hinges on rigorous research, responsible use, and a commitment to balancing innovation with safety. As science advances, RAD140 may redefine not only how we build muscle but also how we approach aging, disease, and human potential.
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