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.As a reliable supplier for research biochemical materials, Bloomtechz provides high-purity RAD140 raw materials and finished RAD140 Capsule products strictly manufactured for laboratory research use. Capsules offer precise dosing and improved stability compared to liquid solutions, making them a preferred choice for research or experimental use. This compound is studied for potential applications in muscle-wasting diseases (e.g., cancer cachexia) and osteoporosis, though it remains unapproved for medical use.
|
|
|
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.
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, systematically designated as 2-chloro-4-[[(1R,2S)-1-[5-(4-cyanophenyl)-1,3,4-oxadiazol-2-yl]-2-hydroxypropyl]amino]-3-methylbenzonitrile (CAS 1182367-47-0), is a non-steroidal selective androgen receptor modulator (SARM) exhibiting high-affinity binding to the androgen receptor with tissue-selective anabolic activity. The following synthetic logic represents the mainstream classical route documented in peer-reviewed literature, provided solely for mechanistic research exploration and academic reference.
Pre-Construction of the 1,3,4-Oxadiazole Heterocyclic Core
The synthetic sequence commences with 4-cyanobenzoic acid derivatives as the foundational starting material, constructing the critical 1,3,4-oxadiazole heterocyclic scaffold through a condensation–cyclization cascade. Specifically, the carboxylic acid moiety undergoes acylation with 4-cyanobenzohydrazide under standard peptide coupling conditions (EDCI/HOBt) to afford the corresponding hydrazide intermediate, which subsequently undergoes intramolecular dehydrative cyclization in the presence of TPP/I₂ to forge the stable aromatic 1,3,4-oxadiazole ring system-thereby locking in the key pharmacophore responsible for AR binding affinity.At Bloomtechz, we optimize this cyclization step through precise temperature ramping and stoichiometric control,
achieving isolated yields exceeding 78% with HPLC purity ≥99.0%, minimizing the formation of regioisomeric byproducts that complicate downstream purification.
Chiral Amino Acid-Directed Ipso-Fluorine Substitution
The left-hand aromatic fragment is assembled via an expeditious ipso-fluorine substitution of 2-chloro-4-fluoro-3-methylbenzonitrile with D-threonine in the presence of K₂CO₃ in DMSO at 75°C, yielding the chiral β-amino alcohol intermediate (compound 9) in >50% isolated yield. This step establishes the (1R,2S) stereocenter critical for tissue-selective AR modulation, with D-threonine serving as an inexpensive, non-proteinogenic chirality source that eliminates the need for costly chiral resolution or asymmetric catalysis.
Bloomtechz leverages this chirality-transfer strategy to produce enantiomerically pure RAD140 API with ee >99.5%, verified by chiral HPLC, ensuring consistent pharmacological performance across batches.
Silyl Protection, Dehydrative Cyclization, and Final Deprotection
The hydrazide–oxadiazole adduct (compound 10) undergoes TBDMS protection of the secondary hydroxyl group, followed by TPP/I₂-mediated dehydrative cyclization to complete the oxadiazole ring closure, and culminates in TBAF-mediated desilylation to afford the final RAD140 molecule. This five-step linear sequence delivers the target compound as a white crystalline solid (m.p. 179–183°C) with an overall yield competitive for laboratory-scale synthesis.
Bloomtechz Manufacturing Advantage
Beyond replicating literature routes, Bloomtechz has engineered a GMP-aligned, scalable manufacturing process for RAD140 API that addresses the critical pain points of grey-market suppliers: residual solvent control (ICH Q3C Class 1/2 solvents <10 ppm), heavy metal content (<10 ppm Pb equivalent), and enantiomeric purity verification via orthogonal chiral chromatography. Every batch is accompanied by a comprehensive CoA, ¹H/¹³C NMR spectra, HRMS confirmation, and HPLC chromatograms-providing our formulation partners with the analytical documentation required for IND-enabling studies and regulatory submissions. For clients seeking end-to-end solutions, Bloomtechz also offers custom encapsulation services (5/10/25 mg hard gelatin capsules) with validated dissolution profiles and stability data supporting 24-month shelf life under controlled storage conditions.
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.
reference
[1]Miller, C. P., Collini, M. D., Tran, B. D., Keith, R. I., Kharode, Y., Marzolf, J. T., ... & Komm, B. S. (2011). Design, synthesis, and preclinical characterization of the selective androgen receptor modulator (SARM) RAD140. ACS Medicinal Chemistry Letters, 2(2), 124–129.
[2]Dickler, M. N., Rugo, H. S., Gelmon, K. A., Cristofanilli, M., Rumble, R. B., & Joffe, C. (2021). A first-in-human phase 1 study of a novel selective androgen receptor modulator (SARM), RAD140, in ER+/HER2- metastatic breast cancer. Clinical Cancer Research, 27(14), 3936–3943.
[3]Sobolevsky, T., Dikunets, M., & Rodchenkov, G. (2013). In vitro and in vivo metabolism of RAD140, a novel non-steroidal SARM. In Recent Advances in Doping Analysis (21) (pp. 121–124). Sportverlag Strauss.
[4]Thevis, M., Piper, T., Beuck, S., Geyer, H., & Schänzer, W. (2013). Expanding sports drug testing assays: mass spectrometric characterization of the selective androgen receptor modulator drug candidates RAD140 and ACP-105. Rapid Communications in Mass Spectrometry, 27(11), 1173–1182.
[5]Ladna, M., Taylor, K., Bhat, A., & Dideban, B. (2023). Idiosyncratic drug-induced liver injury related to use of novel selective androgen receptor modulator RAD140 (Testolone): a case report. Journal of Medical Case Reports, 17, Article 385.
Frequently Asked Questions
Q1: How to verify the authenticity of RAD140 raw material?
+
-
A: Bloomtechz assigns a unique encrypted UUID to each batch of RAD140 API, linked to full batch production records, CoA, HPLC chromatograms, and NMR spectra. Clients can scan the QR code on packaging to instantly verify product authenticity and source legitimacy, eliminating risks of adulteration or concentration mislabeling that plague the grey market.
Q2: What is the minimum order quantity and lead time for RAD140 capsules?
+
-
A: Bloomtechz offers flexible MOQ starting from 1 kg of RAD140 API for capsule formulation partners, with standard lead time of 5–7 business days for in-stock specifications. For custom encapsulation services (5 mg/10 mg/25 mg hard gelatin capsules), lead time extends to 10–15 business days depending on batch size, with bulk order discounts available for commitments exceeding 10 kg.
Q3: Does Bloomtechz provide regulatory documentation support for RAD140 export?
+
-
A: Yes. Every RAD140 shipment from Bloomtechz is accompanied by a comprehensive documentation package including Certificate of Analysis (CoA), HPLC purity report (≥99.0%), NMR/MS structural confirmation, sterility/endotoxin certificates for injectable-grade material, and TSE/BSE-free declarations. We also support DMF (Drug Master File) referencing and provide full batch traceability records to facilitate your regulatory submissions in target markets.
Q4: What storage conditions are required to maintain RAD140 capsule stability?
+
-
A: RAD140 API in powder form maintains stability for 3 years at -20°C and 2 years at -80°C when stored in sealed, light-protected containers. For finished capsules, Bloomtechz recommends storage at 2–8°C in a dry environment with relative humidity below 40%, utilizing desiccant-lined HDPE bottles with child-resistant caps. Our validated cold chain logistics protocol employs PCM shippers and real-time temperature data loggers to ensure no thermal excursion occurs during transit, with full temperature profiles provided alongside each shipment.
Q5: Can Bloomtechz support custom RAD140 formulation development?
+
-
A: Absolutely. Beyond supplying standardized RAD140 API, Bloomtechz offers end-to-end custom formulation services including capsule filling (various sizes from #000 to #4), liquid solution preparation, and transdermal gel development. Our R&D team can tailor excipient profiles, dissolution rates, and bioavailability enhancers to meet your specific product requirements, with pilot batches available for pharmacokinetic evaluation before commercial scale-up.
Hot Tags: rad140 capsule, suppliers, manufacturers, factory, wholesale, buy, price, bulk, for sale