AOD 9604
AOD 9604 is a modified form of amino acids 176-191 of the GH polypeptide. Investigators at Monash University discovered that the fat-reducing effects of GH appear to be controlled by a small region near one end of the GH molecule. This region, which consists of amino acids 176-191, is less than 10% of the total size of the GH molecule and appears to have no effect on growth or insulin resistance. It works by mimicking the way natural Growth Hormone regulates fat metabolism but without the adverse effects on blood sugar or growth that is seen with unmodified Growth Hormone. Like Growth Hormone, AOD 9604 stimulates lipolysis (the breakdown or destruction of fat) and inhibits lipogenesis (the transformation of nonfat food materials into body fat) both in laboratory testing and in animals and humans. Recent findings have shown, in addition to its fat loss properties, AOD 9604 processes many other regenerative properties associated with growth hormone. Currently trials are underway to show the application of AOD 9604 in osteoarthritis, hypercholesterolemia, bone and cartilage repair. AOD 9604 has an excellent safety profile, recently obtaining Human GRAS status in the USA.
CJC 1295
CJC 1295 is often prescribed by physicians as a growth hormone releasing hormone (GHRH) analog. CJC 1295 has been shown potentially to increase growth hormone and IGF-I secretion and effects, but it has been able to do so in very large amounts. CJC 1295 Stimulates Growth Hormone Secretion, and will keep a steady increase of HGH and IGF-1 with no increase in prolactin, leading to fat loss, and increased protein synthesis thereby promoting growth.
One of the reasons CJC 1295 may be prescribed over traditional GHRH or rHGH is its ability to bioconjugate with serum albumin, thus increasing its half-life and potential therapeutic window. It accomplishes this by using protecting groups around the amino acids of GHRH typically susceptible to enzymatic degradation.
CJC 1295 can be compounded in two forms (DAC and non-DAC). Drug affinity complex (DAC) is designed to prevent enzymatic degradation thus increasing the half-life. Consequently CJC 1295- DAC is often prescribed by physicians to be dosed as a single weekly injection. Administration of CJC 1295-DAC is designed to provide a GHRH-like stimulation around the clock. A potential drawback when using a weekly protocol can be attributed to ineffective GHRH stimulation when the body is due for a GH spike (usually 1:00am). This is referred to as a GH-bleed and the overall result is inferior to using CJC 1295-NON-DAC daily for 5 days out of 7. Therefore using CJC 1295- NON-DAC daily (between 6-8pm) provides a more effective GH spike at 1:00am.
Tesamorelin
Tesamorelin is a growth hormone releasing hormone analog that has been shown to increase IGF-1 levels in men by an average of 181 micrograms/liter. It binds and stimulates human GHRH receptors with similar potency as endogenous GHRH. It has a host of other benefits including nootropic effects and reducing triglycerides. Tesamorelin has subsequently been shown to decrease carotid intima media thickness (cIMT), visceral adipose tissue (VAT), and C-reactive proteins (CRP) in a recent study. It has not been shown to significantly affect otherpituitary hormones and their respective mechanisms in the body. Additionally, it has been shown to improve cognitive function for healthy older adults and also for people with mild cognitive impairment who are at an increased risk of progressing to Alzheimer’s disease.
Ipamorelin
Ipamorelin, a synthetic peptide derived from GHRP-1, is made up of five amino acids. Ipamorelin is a powerful growth hormone releasing peptide and is capable of causing potent growth hormone release. Ipamorelin stimulates the release of growth hormone by activating the ghrelin receptor found in the brain. Activating this receptor and increasing the levels of growth hormone within the body can modulate food intake and energy metabolism and also influences glucose and fat metabolism. Growth hormone secretion also increases appetite and causes increased lean muscle growth. Ipamorelin has been demonstrated to be a highly specific growth hormone stimulator since it does not lead to increases in prolactin, follicle-stimulating hormone, luteinizing hormone, or thyroid-stimulating hormone. Furthermore, the peptide does not cause adrenocorticotropic
hormone or cortisol stimulation. Therefore, compared to other growth hormone stimulators, such as GHRP-2 and GHRP-6, ipamorelin is a more specific growth hormone stimulator. This means that ipamorelin does not possess lipogenic properties and it does not promote hunger. Furthermore, it is at least as potent as GHRP-6 and almost as potent as GHRP-2. Animal studies have shown that ipamorelin can counteract a reduction in bone and muscle strength [5]. In human trials, ipamorelin was shown to induce substantial and dose dependent growth hormone release in healthy males. Another human study also determined that ipamorelin strongly induces growth hormone release over a range of doses and that the half-life of the peptide is two hours. In summary, ipamorelin is a potent growth hormone stimulator that does not broadly affect additional biochemical pathways like some other GHRPs. The optimal way to use ipamorelin is to stack it with low doses of other growth hormone releasing peptides, such as GHRP-2, GHRP-6 or hexarelin. Combining a low dose of ipamorelin with an additional GHRP will increase the pulse of human growth hormone. Ipamorelin should be reconstituted in BAC water and injected subcutaneously or intramuscularly at a dosage of 200 mcg. Ipamorelin can be dosed once or twice daily and dosages should be spread out over the course of 24 hours. Ipamorelin has been acutely administered to humans at 100 mcg/kg with no adverse effects reported. The peptide has also been administered at 30 mcg/kg twice daily for up to 7 days and was well tolerated [8]. The highly specific actions of ipamorelin give it a positive safety profile and side effects when using ipamorelin at the recommended dose are generally minimal, although headaches have been reported.
IGF-1 LR3
IGF-1 LR3, also known as LR3-IGF-1, is an elongated and modified version of naturally occurring IGF-1. The naturally occurring 70-amino acid form of activated IGF-1 is essential for normal human growth and development and acts via IGF-1 receptors to exert an anabolic effect to build muscle, which is why IGF-1 is important in bodybuilding. Low IGF-1 peptide levels are linked to poor growth and a number of metabolic disorders. Multiple tissues inside the body produce IGF-1 and its site of synthesis affects its function. The majority of IGF-1 is made by the liver and is transported to other tissues in the bloodstream, acting as an endocrine hormone. Importantly, IGF-1 is a central growth hormone that controls the anabolic growth promoting effect of growth hormone. It also has a growth hormone independent growth-stimulating effect, which is optimized when combined with human growth hormone (HGH). In comparison to IGF-1, IGF-1 LR3 contains 13 extra amino acids and has the amino acid arginine substituted in position 3. These additional amino acids increase the potency of IGF-1 LR3 to three times that of IGF-1 since it has around 1% affinity for IGF-binding proteins, which act to block the growth-promoting effects of IGF-1. The modified IGF-1 LR3 peptide also has improved metabolic stability and remains active in the body for longer than IGF-1. The reduced protein binding and longer half-life means that the peptide is free to promote muscle and bone growth and repair and smooth muscle survival. IGF-I LR3 has been shown to stimulate muscle growth and increase muscle mass by up to 50%. Additionally, IGF’s also modulate how the body utilizes glucose via insulin signaling and can stimulate free fatty acid utilization and fat loss.
IGF-1 LR3 has an extended half-life of between 20 and 30 hours, which is around twice that of unmodified IGF-1. The long half-life means that IGF-1 LR3 only needs to be dosed once per day, either subcutaneously or intramuscularly and will increase lean muscle growth and promote fat reduction and weight loss throughout the whole body. Up to 100 mcg can be dosed each day. A standard IGF-1 LR3 cycle should last four weeks and should be stacked with an anabolic androgenic steroid for optimal results. Side effects of IGF-1 LR3 may include headaches and nausea since the peptide can induce a hypoglycemic state. High levels of this hormone have also been shown to promote organ enlargement, so never exceed the recommended dose of 100 mcg per day. Ibutamoren (MK-677) Ibutamoren is a potent, long-acting,orally active, selective agonist of the ghrelin receptor and a growth hormone secretagogue, mimicking the growth hormone (GH)-stimulating action of the endogenous hormone ghrelin. It has been shown to increase the secretion of several hormones including GH and insulin-like growth factor 1 (IGF-1) and produces sustained increases in the plasma levels of these hormones without affecting cortisol levels.
Ibutamoren has been shown to sustain activation of the GH–IGF-1 axis and to increase lean body mass with no change in total fat mass or visceral fat. It is under investigation as a potential treatment for reduced levels of these hormones, such as in children or elderly adults with growth hormone deficiency, and human studies have shown it to increase both muscle mass and bone mineral density, making it a promising potential therapy for the treatment of frailty in the elderly.
Tesofensine
Tesofensine is a serotonin.noradrenaline/dopamine reuptake inhibitor. It acts in the brain to decrease appetite and therefore triggers weight loss. Tesofensine has been proven very effective in the treatment of obesity. Patients in clinical studies have shown lost an average of 12.8kg (i.e. about 10% of body weight) in 6 months, showing tesofensine as one of the most effective weight loss molecules.
PEG-MGF
PEG MGF refers to pegylated mechano growth factor. This is a spliced variant of the IGF gene that is used by animals to increase their stem cell count within the muscle tissue while encouraging muscle fibers to mature and fuse.
This system is largely used to produce adult muscle as rats mature. The natural version of this peptide is developed where needed and does not travel through the bloodstream; synthetic versions of this chemical have been altered so they may remain stable in the bloodstream for a few minutes. Pegylation refers to the chemical’s ability to attract polyethylene glycol from larger molecules. In this case, the peptide is specifically designed to fuel the breakdown of MGF. PEG molecules can act as a protective coating for the portion of MGF they attract. In theory this would allow MGF to be carried through the bloodstream without being broken down so it can reach its destination more successfully.