VaughnTrue
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OSTA-PLEX® — Legal Gear for Competitive Athletes!
A bomb has just been dropped on the supplement world that will change the face of sports supplements forever! This new technology could be the biggest advance in sports supplements since the introduction of “andro” back in 1996. The technology we are referring to is SARMs (Selective Androgen Receptor Modulators), which are the next generation of muscle building compounds, however, until now there are no lawful dietary SARM products. Structurally, SARMs can be categorized into steroidal and nonsteroidal SARMs. The steroidal SARMs are formed by modifying the chemical structure of testosterone molecule.
OSTA-PLEX® is a combination of steroidal and nonsteroidal SARMs that work together synergistically to produce phenomenal gains. According to Hi-Tech's scientists OSTA-PLEX® is the most revolutionary product to hit the market in 10 years.....“With the advent of OSTA-PLEX® and its patented technology, the bodybuilding community boasts this new muscle building product is capable of superseding the effectiveness of all previous SARMs in producing massive muscle building effects…OSTA-PLEX® has the unique ability to selectively target androgen receptors specifically in muscle tissue and not bind to the androgen receptors in other tissues and organs. This greatly increases its anabolic activity in muscle tissue.”
The initial efforts to develop steroidal SARMs, based on modifications of the testosterone molecule, date back to the 1940s. The modern era of nonsteroidal SARMs was unleashed by independent work at Ligand Pharmaceuticals. The last decade has witnessed unprecedented discovery effort to develop selective androgen receptor modulators (SARMs) that improve physical function and bone health without adversely affecting the prostate and cardiovascular outcomes. OSTA-PLEX® describes the extensive research and development, historical evolution, the rationale for SARM development, and the mechanisms of testosterone action and SARM selectivity that makes this truly a one-of-a-kind muscle building product.
Steroidal Based SARMs
19nor-DHEA is the only legal prohormone that converts to 19-norAndrostenedione and/or nandrolone. 19nor-DHEA, which is a extremely powerful and a patented compound converts to three different powerful hormones:19-norAndrostenedione, 19-norAndrostenediol & 19-NorTestosterone also known as nandrolone. 19Nor-Dehydroepiandrosterone (also known as 19 Nor-DHEA) is not to be confused with DHEA, 19nor-Dehydroepiandrosterone lacks a carbon molecule in the 19-position dramatically differentiating it from DHEA. 19Nor-DHEA binds to the androgen receptor better than testosterone and is also a 5-alpha-reduced compound, meaning it cannot convert to dihydrotestosterone (DHT) or estrogen.
Now that you have a basic understanding of the importance of SARMs we will tell you how to achieve a similar effect by utilizing our product OSTA-PLEX®. A recent study suggests we can achieve SARM like effects with the prohormone 19-¬‐norandrostenedione. OSTA-PLEX® is based upon 19-norDHEA, which is a one step prohormone to both 19-norandrosteneDIONE, and 19-¬ norandrosteneDIOL. It is a two step prohormone to nandrolone (otherwise known as nortestosterone). Removal of the 19-methyl group increases the anabolic activity of testosterone. Thus, 19-nortestosterone has formed the basis of the nandrolone series of molecules. Nandrolone is reduced by 5-α reductase in target tissues to a less potent androgen, dihydronandrolone, but it is less susceptible to aromatization to an estrogen. A depiction of these conversions is shown:
Another recent study on 19-norandrostenediol was published (Schrader et al., 2006). This study showed that a 25mg sublingual tablet of 19-norAndrostenediol had a Cmax equivalent or greater than 100mg’s of nandrolone injections. Cmax is simply peak blood levels of the target hormone (nandrolone in this case). This again illustrates much like 1-DHEA and 4-DHEA, that the delivery system is critical to strength and mass gains when using this prohormone.
One of the most frequently used steroid precursors (prohormones) mentioned above is 19-Nor Androstenedione (NORDIONE). Recently studies have shown that NORDIONE stimulates skeletal muscle growth after usage in a highly selective manner but exhibits only weak androgenic activity. Receptor binding tests demonstrate that NORDIONE binds with high selectivity to the Androgen Receptor. The potency of NORDIONE to transactivate androgen receptor (AR) dependent reporter gene expression was 10 times lower as compared to dihydrotestosterone (DHT). The prohormone 19-nor-androstenedione came on to the supplements market in the late nineties, as a follow-up to the commercially successful androstenedione. Enzymes in the body convert androstenedione into testosterone, and likewise, enzymes convert 19-nor-androstenedione into nandrolone.
As a result, nonsteroidal selective androgen receptor modulators with anabolic activity but less prostate stimulation are being developed. We hypothesized the anabolic precursor 19-nor-DHEA would increase muscle, lean body mass (LBM), and bone mineral density (BMD) with little stimulation of prostate growth. In summary, OSTA-PLEX® increases muscle and bone mass without significant stimulation of prostate growth, suggesting it may have some properties of a steroidal selective androgen receptor modulator.
Non- Steroidal Based SARMs
SARM stands for selective androgen receptor modulator. They are hormone like molecules that act like androgens in certain tissues without having the androgenic side effects of testosterone. SARMs are in development from many sources and the popular prohormone 19Nor-Androstenediol was just reported to have SARM-like effects in men (see above). Some SARMS are in development already including ARYL-PROPIONAMIDE like Ostarine and Andarine. The problem with these is that they don’t provide fully equal muscle stimulation to testosterone and its metabolites so they lack the potency to be used as proper muscle building agents in younger men. SARMs are improving in potency and some day we may see a commercially available SARM but, for now, OSTA-PLEX® technology provides the most benefit to men that want the muscle building properties and bone density increase that one receives from testosterone, but don’t want the side effects like prostate enlargement.
Hi-Tech's sister company, LG Sciences, was the first to introduce what is considered a Phytochemical Selective Androgen Receptor Modulator or P-SARM in 2008, which was a full 7 years before SARMs were in vogue for bodybuilders! Its parent company — Hi-Tech Pharmaceuticals — was the first to bring the main pSARM compound in OSTA-PLEX® to market, 7-methoxy-8-(3-methyl-2-butenyl)-2H-1-benzopyran-2-one. A P-SARM is a phytochemical (plant-derived) compound that mimics the effects of androgens on muscle mass, strength, bone growth, drive, and sexual function, while at the same time not negatively effecting blood lipids or blood pressure. Androgens are essential for male development and the maintenance of male secondary characteristics, such as bone mass, muscle mass, body composition, and spermatogenesis. The recent discovery of nonsteroidal selective androgen receptor modulators (SARMs) provides a promising alternative for testosterone replacement therapies with advantages including oral bioavailability, flexibility of structural modification, androgen receptor specificity, tissue selectivity, and the lack of steroid-related side effects.
As usual, without the heavy and crazy regulation, the supplement industry can bring this technology to market much faster than the pharmaceutical companies. We do owe them a debt of thanks though, since they give us the direction in which to find natural alternatives to the problem at hand. Hi-Tech will show you real scientific studies showing the amazing anabolic effects of our pSARM technology, but first let’s look how pSARMs function. pSARMs act like testosterone in specific tissues like muscle. This gives us the unique benefit of being anabolic without the negative side effects found with illegal compounds. The key to the pSARM is in the shape of the molecule which is similar to testosterone and acts like it in specific muscle tissues, giving the bodybuilder a very potent anabolic agent without the negative side effects. If you look at the diagram on the bottom of the page, you can see figure 1 is of the testosterone molecule in molecular position. Figure 2 is a molecular position diagram of 7-methoxy-8-(3-methyl-2-butenyl)-2H-1-benzopyran-2-one, the main pSARM in OSTA-PLEX®. In figure 3 you can see how they overlap and therefore have similar activity in tissues like muscle without being negative on the liver or prostate. This overlap technology is what makes pSARMs so amazing.
In a recent study researchers found “RESULTS: Testosterone, LH and FSH were significantly increased at the high dose of 7-methoxy-8-(3-methyl-2-butenyl)-2H-1-benzopyran-2-one treatment. The high and low dose of 7-methoxy-8-(3-methyl-2-butenyl)-2H-1-benzopyran-2-one treatment significantly enhanced the activity of NOS (P < 0.01). CONCLUSION: 7-methoxy-8-(3-methyl-2-butenyl)-2H-1-benzopyran-2-one could increase androgen, gonadotropin and nitric oxide synthase (NOS) activity. It suggested that 7-methoxy-8-(3-methyl-2-butenyl)-2H-1-benzopyran-2-one had androgen-like effect and gonadotropin-like effect.” OSTA-PLEX® is the most advanced muscle building agent on the market today. The pSARM effect in OSTA-PLEX® along with the 19-NorDhea and advanced delivery matrix give OSTA-PLEX® the anabolic punch to build muscle! There has never been anything like OSTA-PLEX® for increasing size and strength!
Plants containing compounds such as the isoflavonoids, with female hormone-like effects that bind to human estrogen receptors, are known. But none has been previously shown to have corresponding male hormone-like effects that interact with the human androgen receptor. However, Hi-Tech has developed one proprietary extract from the tree bark of Eucommia ulmoides that possesses bimodal phytoandrogenic and hormone potentiating effects by lipidic components. OSTA-PLEX® also utilizes this Novel Phytoandrogen from Eucommia ulmoides extract called EU 80®, which is based upon an Ethanolic 80:1 extract of Eucommia ulmoides. Hi-Tech was able to isolate the key compounds responsible for the steroidogenic effects where previously these were unknown. The bioactivities of Eucommia ulmoides were found to have a phenomenal tripartite synergism between the androgen sex steroid receptors, their cognate steroidal ligands and lipidic augmenters isolated from E. ulmoides. Phytoandrogenic activity of Eucommia ulmoides was also mediated by plant triterpenoids binding cognately to the androgen receptor (AR) ligand binding domain.
pSARMs are phyto-SARMS or plant based SARMs. pSARMs can come in a variety of plant based sources and constituents that act as phyto-androgens in certain tissues. Phyto-androgens are great because they give similar muscle building effects like testosterone yet seem to lack the prostate and hair loss stimulation effects of testosterone and pro-hormones. The extract used in this study is from the bark of the tree Eucommia ulmoides which has a VERY high caprylic acid content. The ethanolic extract of the bark from Eucommia ulmoides is able to bind to and activate the androgen receptor with enough affinity to displace testosterone with efficacy at a 5-25ng/mL range. The addition of the extract to a medium containing DHT noted that even at saturating levels of DHT, Eucommia ulmoides augmented signalling in the range of 112-204% of baseline. Importantly, this was found with the fractions containing triterpenoids, the caprylic acid content of Eucommia ulmoides not any ordianary powder or extract. Hi-Tech's scientific team researched and found there are One-hundred twelve compounds in Eucommia ulmoides, including the main active constituents, lignans, triterpenoids, fatty acids and iridoids. Previous herbal extracts have had secondary androgenic effects (increase LH/FSH and androgen secretion or change in SHBP binding) but none directly activated the AR. Eucommia ulmoides also acts as an androgen booster/helper, by augmenting endogenous and/or exogenous testosterone signaling at the androgen receptor. What this means that any outside sources of androgens getting into your body (including Eucommia ulmoides itself, and other testosterone boosters/SARMs), as well as your own natural circulating testosterone, will now have an even stronger effect (approximately 200%) with the help of LG's Eucommia ulmoides extract called EU 80®.
Eucommia ulmoides Oliv. is the sole species of the genus Eucommia. The leaf, stem, and bark as well as staminate flower of Eucommia ulmoides have been traditionally used in China, Japan, Korea, among others. The ethnopharmacology, phytochemistry, biological activities, and phytoandrogenicity of Eucommia ulmoides is unique as the androgen receptor (AR), ligand binding to the carboxy-terminal domain regulates transcriptional activation functions in the LBD and amino-terminal domain.
The study set out to determine what effect if any does an extract of the bark of the tree Eucommia ulmoides have on creating synergism between sex steroids receptors, sex hormones and lipids derived from plants.
What they discovered is that the extract demonstrated androgenic activities by weakly activating Androgen Receptors (AR) in a dose-dependent manner. The scale that is used to measure androgenic activity is such that a saturation dose of the androgen receptor’s native ligand (testosterone) will produce a 100 fold Luciferase assay (LUC) activity. The extract produced a 6.4 fold LUC activity.
However when they combined a saturation dose of testosterone and the extract they found synergy. When a saturation dose of androgen, either DHT or testosterone is added together with the extract the increases in Androgen Receptor (AR)-mediated reporter gene expression goes up beyond what the saturation dose of testosterone or DHT alone could produce. The synergy with DHT moved up above the 200% mark while the synergy with testosterone moved androgen receptor activity close to the 240% mark. The extract acted as an amplifier of androgen receptor transcriptional activity.
In the words of the study “This is highly unusual as normally, androgen mediated AR transcriptional capacity, akin to all ligand dependent steroid receptors, plateaus at saturating doses of its cognate ligand.”
So to restate, testosterone activates androgen receptor transcriptional activity to their normal capacity of 100%. The extract by itself weakly activates the androgen receptor by 6%. Together the extract and testosterone activate the androgen receptor and propel it to transcribe at a rate more than twice what it is normally capable of. In this case increasing activity to 240%.
The study then attempted to ascertain the components of the extract responsible for the synergism. To this end they fractionated the extract into components and found two active components. One component was found to exert its effect (labeled phytoandrogenic activity by the authors) on the Androgen Receptor by changing its binding characteristics. That compound is completely unrelated to caprylic acid.
The second active fraction contained 8-carbon polysaturated fatty acid, caprylic acid, and other lipids. In the words of the authors:
“Bioassays using pure caprylic acid and other polysaturated fatty acids (PFAs) correlated with the augmenting effect of E. ulmoides on the AR [androgen receptor] in varying degrees. Ethanolic extract of coconut (Cocos nucifera) flesh, rich in C-8 caprylic acid and other polysaturated fatty acids, replicated the hormone potentiating effect of both E. ulmoides extract and pure caprylic acid in AR bioassays (data not shown).”
In my words, Equally effective were: Ethanolic extract of coconut;Pure caprylic acid; and E. ulmoides. The major constituent in all three is caprylic acid which as the authors show in the figure below had the strongest augmenting effect of all the lipids. So a blend of PFAs in ethanolic extract of coconut the vast majority of which is caprylic acid replicated the hormone potentiating effect of E. ulmoides extract whose primary constituent is caprylic acid which all by itself in pure caprylic acid form replicated the hormone potentiating effect of E. ulmoides extract.
“Okadaic acid, a known phosphorylation promoter, is able to strongly augment androgen-dependent AR activity. Interestingly, fatty acids can also promote phosphorylation. One instance is oleic acid, a C-18 cis-monosaturated fatty acid. It is possible that AR [androgen receptor] and ER augmentation by both E. ulmoides extract and caprylic acid arise from a common tripartite synergism between the steroid receptors, sex steroids and fats, based on a phosphorylation mechanism.”
The action of caprylic acid labeled a “lipid augmenter” by the authors is postulated to result from increased phosphorylation. This differs from the action of the other non-caprylic component labeled a “phytoandrogen” which changes the ligand binding characteristics.The study concludes, “the novel discoveries reported in this study add phytoandrogens and lipidic augmenters to the emerging list of hormomimetics (such as phytoestrogens) known to exist in plants. Pharmaceutical utility of lipidic augmenters in the treatment of hypogonadal conditions such as menopause or andropause could be exploited based on this mechanism of tripartite synergism. The link between excess dietary lipids, hyper-androgenism and hormone-related disorders should also be further explored in the light of these findings.”
OSTA-PLEX® and its patented technology has turned the bodybuilding community on its head! Hi-Tech researchers believe this new muscle building product is capable of superseding the effectiveness of all previous SARMs in producing massive muscle building effects…OSTA-PLEX® has the unique ability to selectively target androgen receptors specifically in muscle tissue and not bind to the androgen receptors in other tissues and organs. This greatly increases its anabolic activity in muscle tissue. Hi-Tech is proud to introduce the first potent, and legal SARM to ever hit the market.
