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RAD-140 is a non-steroidal compound from the group of selective androgen receptor modulators (SARMs), was synthesized and introduced to the world in 2011 by Radius Health Inc. This supplement was conceived as a less invasive alternative to androgen therapy for bone and joint diseases and tumors associated with sex hormones.
In the sports industry, RAD-140 is also known as Testolone. Athletes and enthusiasts use it as a safer option, unlike anabolic androgenic steroids (AAS), to improve physical condition. Due to its high anabolic potential and specific properties regarding the nervous system and prostate, it is often also used as a supplement to substances with strong androgenic potential.
Although RAD-140 structurally differs from androgen hormones, it has the ability to interact with the androgen receptor (AR) in certain tissues. Thanks to this, this compound is able to provide the same benefits in the area of bone tissue, nerve cells, or glands as testosterone and 5-alpha-dihydrotestosterone (DHT) without causing side effects associated with the use of these hormones.
Regarding anabolic properties, after the compound was administered, an increase in muscle tissue was recorded compared to the control group, which received a short ester of testosterone.
RAD-140, by occupying androgen receptors, reduces the androgen potential of other agents from the AAS group.
Acting as an androgen mimetic, this compound can provide protective action on hippocampal cells, including protection from the harmful effects of beta-amyloid peptide. Furthermore, it can treat and alleviate symptoms of neurodegenerative diseases.
RAD-140 is capable of attenuating the action of estrogens on designated ER1 and ER2 receptors, which was used in a study involving women battling breast cancer.
The impact of RAD-140 on the total number of estrogen receptors remains unclear; it is predicted that it can inhibit the expression of the ESR1 gene, which encodes their formation.
RAD-140, by binding to the androgen receptor, can promote the development of muscle tissue similar to typical AAS. Interestingly, in animal studies, the anabolic potential of this agent was similar to testosterone, as illustrated by comparing muscle tissue growth.
Compared to the entire group of ligating agents, the compound demonstrates excellent properties for reducing the androgenic potential of other compounds. In studies, RAD-140, used in parallel with a short ester of testosterone, but also with a much stronger androgenic DHT, was able to reduce the effects of steroids on the prostate and seminal ducts. This effect can be explained by the strong affinity of RAD-140 to the androgen receptor, which, thanks to its selective action, did not cause changes in the tissues of the reproductive organs. However, this is just a hypothesis. Importantly, users of the agent report a decrease in hair loss during AAS treatment when using RAD-140 simultaneously.
In the case of using RAD-140 as part of therapy or as a doping agent, such as SARM, it is an alternative to AAS. However, in both cases, this compound has one significant advantage: it has few side effects compared to androgens.
AAS disrupts the balance of the endocrine system in the human body the most. However, RAD-140 cannot be converted to DHT and does not increase estrogen or prolactin levels. Thus, it is burdened with significantly fewer side effects.
Furthermore, RAD-140 can only slightly suppress testosterone secretion; this phenomenon occurs when using elevated doses on a scale that is incomparably lower than in standard anabolic androgenic steroids.
The agent has high bioavailability when taken orally; approximately 70% of the active ingredient is effectively absorbed into the bloodstream after oral administration. As an unmethylated compound, without the c-17-alpha group, RAD-140 is considered inert to the liver. However, when using very high doses, precautionary measures should be taken, such as regular liver function tests, and if necessary, appropriate prophylaxis.
Furthermore, in in vivo and in vitro studies, it was found that RAD-140 reduces neuronal damage by toxins such as peptide A1-42, as well as DHT and testosterone.
The use of RAD-140 is associated with the risk of suppressing the secretion of one's own testosterone. In the case of prolonged use of high doses of the agent, there is a high risk of lowering testosterone levels.
The agent is an interesting supplement for people interested in gaining muscle mass and can be used for this purpose in combination with any substance from the AAS/SARMs/Prohormones group.
Testosterone propionate + RAD140
Testosterone propionate + Nandrolone phenylpropionate + RAD-140.
Animal studies show that the agent has high androgenic properties at doses as low as 3 mg, but in athletes, it usually ranges around 10 mg once a day.
Rad-140 shows its full range of capabilities when combined with testosterone, but due to its specific action on androgen receptors, it is not a good supplement to DHT derivatives.
Before starting use, it is recommended to perform hormonal panel tests, paying particular attention to luteinizing and follicle-stimulating hormones, testosterone, and estradiol. Then, it is worth monitoring the levels of these parameters during and after the cycle.
In case of suppression of one's own testosterone secretion, it is usually sufficient to use a simple PCT (post-cycle therapy) with the use of Arimistane+
Sources:
Bhasin S., Jasuja R. Selective androgen receptor modulators (SARM) as stimulating treatment methods. Curr Opin Clin Nutr Metab Care. 2009; 12 (3): 232-40. Jayaraman A., Christensen A., Moser V.A., West R.S., Miller S.P., Hattersley G. et al. Selective androgen receptor modulator RAD140 is neuroprotective in cultured neurons and male rats affected by kainates. Endocrinology 2014. P. 1398-406. Miller S.P., Shomali M., Little S.R., O'Dea L.S., Herendeen H., Gallagher K. et al. Design, synthesis, and preclinical characterization of the selective androgen receptor modulator (SARM) RAD140 ACS Med Chem Lett.2011; 2 (2): 124-9. -105. Mass Spectr Rapid Commun. 2013; 27 (11): 1173-82. Tevis M., Schanzer V. Detection of SARM in doping control analysis. Mol Cell Endocrinol. 2018; Selective androgen receptor modulator RAD140 inhibits the growth of breast cancer models positive for androgen/estrogen receptors, with a specific mechanism of action. Clin Cancer Res. 2017; 23 (24): 7608-20. Zierau O, Kolodziejczyk A, Vollmer G, Machalz D, Wolber G, Thieme D, et al. Comparison of three SARM RAD-140, GLPG0492 and GSK-2881078 in two different bioanalyses in vitro and in silico androgen receptor binding analysis. J. Steroid Biochem Mol Biol. 2019; 189: 81-6. Rosario ER, Carroll JC, Oddo S, LaFerla FM, Pike CJ. Androgens regulate neurology development in a triple transgenic mouse model of Alzheimer's disease. J Neurosci. 2006; 26: 13384 – 13389. Leranth C, Hajszan T., MacLusky NJ. Androgens increase spine density in the CA1 hippocampal subfield in ovariectomized female rats. J Neurosci. 2004; 24: 495-499. Janowsky JS. The role of androgens in cognition and brain aging in men. Neurology. 2006; 138: 1015–1020. Moffat S.D., Zonderman A.B., Metter E.D. et al. Free testosterone and the risk of Alzheimer's disease in elderly men. Neurology. 2004; 62: 188-193.
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