What is RAD-140 (Testolone)?
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Sports Technology Labs - Last Updated: February 29, 2024
Table of Contents
RAD-140 is a SARM developed by Radius Health, Inc. with the goal to target conditions like muscle wasting and breast cancer. It exerts anabolic activity in muscle and connective tissue with little effect on the prostate and seminal vesicles. In addition, researchers are studying its ability to selectively compete and antagonize testosterone in these tissues.
In a recent study, scientists administered testosterone propionate at 1mg/kg/day to castrated rats and co-administered RAD-140 at various quantities. It was determined that 0.3-1mg/kg of RAD-140 counteracted 1mg/kg testosterone propionate in prostate tissue where a protective effect on the prostate from this compound was seen.
RAD-140 has also displayed a dramatic increase in muscle tissue, muscle mass, and cardioprotective effects via lowering blood lipids LDL, HDL, and triglycerides in clinical research. The prostate weight was not evaluated in the study above.
Research On Rats
According to a study by Jayaraman and colleagues, the decline in testosterone levels in men during normal aging increases risks of dysfunction and disease in androgen-responsive tissues, including the brain. Testosterone therapy has been linked to increased risks of developing prostate cancer and accelerating its progression.
To address these concerns, further research of SARMs such as RAD 140 SARM are being studied. The efficacy of SARMs in the brain is not well understood .
In animal studies, the RAD 140 SARM was investigated for its ability to provide neuroprotection in cultured rat neurons and male rat brain, an important neural action of endogenous androgens that is relevant to neural health and resilience to neurodegenerative diseases.
Results From Above Research
Results showed that RAD140 causes the same effect as testosterone in reducing cell death induced by apoptotic insults in cultured hippocampal neurons. The half-life of this was not discussed.
The RAD 140 neuroprotective benefits were dependent upon MAPK signaling, as evidenced by the elevation of ERK phosphorylation and inhibition of protection by the MAPK kinase inhibitor U0126.
In vivo experiments with gonadectomized, adult male rats also demonstrated RAD140’s peripheral tissue-specific androgen action, its ability to activate androgenic gene regulation effects, and its neuroprotective effects on hippocampal neurons against cells death caused by systemic administration of the excitotoxin kainate .
According to these researchers, they believe these findings demonstrate the potential preclinical efficacy of SARMs in providing neuroprotective actions relevant to Alzheimer’s disease and related neurodegenerative diseases.
Research Continued
The purpose of this next animal study was to evaluate the efficacy of RAD 140, also known as testolone, in in vivo and in vitro models of androgen receptor and estrogen receptor-positive (AR/ER+) breast cancer .
According to these researchers, steroidal androgens have been used to treat breast cancer and the researchers sought to determine if RAD 140 could similarly suppress AR/ER+ breast cancer cells. In vitro assays showed that RAD 140 had a high level affinity and specificity for binding to AR, and activated AR in BC cells but not in prostate cancer cells.
Administration of RAD 140 inhibited the growth of AR/ER+ breast cancer patient-derived xenografts (PDX). Co-administration of RAD 140 and palbociclib showed improved efficacy in the AR/ER+ PDX models.
The study concluded that RAD140 is a potent AR agonist with a distinct mechanism of action, inhibits the growth of multiple AR/ER+ breast cancer PDX models, and warrants further clinical investigation in AR/ER+ breast cancer patients.
What Are the Observed Effects of RAD-140 in Research?
Scientists are intrigued by RAD-140 and its neuroprotective effects. Higher levels of testosterone have been associated with slower buildup of β-amyloid plaques in the brain.
In vitro, RAD 140 is shown to be as effective as testosterone in reducing cell death induced by apoptotic insults and requires only three times as much concentration as testosterone to protect against β-amyloid proteins. When tested in live rats, RAD 140 protected the brain against neuron loss from kainate exposure.
RAD 140 is prepared for a phase 1 clinical trial as a potential treatment for severe weight loss due to cancer cachexia.
What Benefits of RAD-140 Are Researchers Studying?
1. The effect on lean muscle and lean body mass.
2. The neuroprotective effects and β-amyloid-related dementia.
3. Blood LDL, HDL, and triglycerides.
4. The prostate and androgens like testosterone and DHT.
Sports Technology Labs supplies the highest quality pure RAD140 powder and a convenient liquid RAD140 solution.
AT THIS TIME, RAD140 / TESTOLONE IS ONLY APPROVED FOR LABORATORY RESEARCH AND IS NOT SOLD FOR HUMAN CONSUMPTION.
Abuse Warning
RAD 140 is one of many investigational compounds still awaiting FDA approval and like other research chemicals, they are not dietary supplements. At Sports Technology Labs we are chemical suppliers, not medical doctors, and our expertise is sourcing and quality control.
Sports Technology Labs does not encourage or condone consumer use of SARMs products, they are for research purposes only. Anecdotal reports and guides may not match those used in carefully designed medical research protocols and may pose a serious risk of adverse effects on users.
Individual variables, comorbidities, and polypharmacy can also contribute significantly to the risk of health problems.
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The best place to find RAD 140 and other sarms for sale is right here for your research institution’s lab. We offer a wide variety of research chemicals and take pride in our fast shipping times.
All of our products are third party tested and only available for research use. Are you not sure if this research chemical is suited for your testing needs? Contact us today and we will provide you and your company with great customer service, guaranteed. We have the new RAD 150 for sale as well.
Scientific References:
1. Anusha Jayaraman, Amy Christensen, V. Alexandra Moser, Rebekah S. Vest, Chris P. Miller, Gary Hattersley, Christian J. Pike, Selective Androgen Receptor Modulator RAD140 Is Neuroprotective in Cultured Neurons and Kainate-Lesioned Male Rats, Endocrinology, Volume 155, Issue 4, 1 April 2014, Pages 1398–1406
2. Miller, Chris P. et al. “Design, Synthesis, and Preclinical Characterization of the Selective Androgen Receptor Modulator (SARM) RAD140.” ACS Medicinal Chemistry Letters 2.2 (2011): 124–129. PMC.
3. Gouras GK, Xu H, Greenfield JP, Hai B, Wang R, Greengard P. Testosterone reduces neuronal secretion of Alzheimer’s beta-amyloid peptides. Proc Natl Acad Sci USA. 2000 Feb 1;97(3):1202-5.
4. Jayaraman A, Christensen A, Moser VA, Vest RS, Miller CP, Hattersley G, Pike CJ. Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and kainate-lesioned male rats. Endocrinology. 2014 Apr;155(4):1398-406. doi: 10.1210/en.2013-1725. Epub 2014 Jan 15. PMID: 24428527; PMCID: PMC3959610.
5. Yu, Z., He, S., Wang, D., Patel, H. K., Miller, C. P., Brown, J. L., … & Saeh, J. C. (2017). Selective Androgen Receptor Modulator RAD140 Inhibits the Growth of Androgen/Estrogen Receptor–Positive Breast Cancer Models with a Distinct Mechanism of ActionSARM Inhibits AR/ER+ Breast Cancer. Clinical Cancer Research, 23(24), 7608-7620.
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