What Is TESAMORELIN 5MG?
Tesamorelin is a man-made analog of growth hormone-releasing hormone (GHRH). It is composed of 44 amino acids, and its N-terminus is chemically modified by the addition of a trans-3-hexenoic acid group. This minor difference makes it resistant to cleavage by dipeptidyl aminopeptidase, thus making it more stable and extending its half-life.
Tesamorelin was approved by the FDA for the treatment of HIV-related lipodystrophy in 2010. Further, this synthetic peptide has been researched for its applications in cardiovascular diseases and dementia. At Pinnacle Peptides, tesamorelin for sale is exclusively available for research and educational institutions.
Structure Of TESAMORELIN 5MG
Molecular Formula: C216H360N72O63S
Molecular Weight: 5006 g/mol
CAS number: 218949-48-5
PubChem CID: 56928011
Mechanism Of TESAMORELIN 5MG
As a GHRH analog, it binds to growth hormone releasing-hormone receptors in the anterior pituitary glands. This, in turn, activates the series of intracellular signaling, leading to the production and release of growth hormone. GH is a powerful anabolic hormone involved in many processes, including building muscle mass and repair. It acts on different cells, including liver cells, and stimulates the release of insulin-like growth factor-1 (IGF-1).
1. HIV-related Lipodystrophy
The use of highly active antiretroviral therapy among AIDS patients has been associated with the development of lipodystrophy. Lipodystrophy is characterized by the abnormal distribution of fat in the body, such as the accumulation of visceral adipose tissue in the abdomen. This can increase the risk of cardiovascular diseases and insulin resistance.
The use of recombinant human growth hormone has been approved by the FDA for the treatment of lipodystrophy. However, it requires large doses and might cause side effects, such as peripheral edema and carpal tunnel syndrome [1[. On the other hand, tesamorelin proved a safe and effective option for the treatment of HIV-associated lipodystrophy.
Research suggests it is four times more effective than all the other treatment options combined . A phase III clinical trial was conducted to check the long-term safety and efficacy of tesamorelin. AIDS patients with lipodystrophy were randomized to receive either 2mg tesamorelin or placebo subcutaneously for 26 weeks. After that, patients originally on tesamorelin were switched to placebo and vice versa. The study concluded that tesamorelin was generally well-tolerated and effective. The decrease in visceral adipose tissue was sustained over 52 weeks. However, fat was reaccumulated upon the discontinuation of treatment .
2. Insulin Resistance
The use of recombinant growth hormone is associated with insulin resistance. One study was conducted to determine if tesamorelin also alters insulin sensitivity. 53 patients with type 2 diabetes were randomized to receive either tesamorelin (1mg, 2mg) or placebo for 12 weeks. The results didn’t find any significant difference between the two groups relative to insulin response throughout the study .
3. Cardiovascular Diseases
HIV patients on antiretroviral therapy are at higher risk of heart disease due to the accumulation of fat in the abdomen area. Along with HAART, the prevention of cardiovascular diseases is an important intervention for the long-term safety of patients. Research suggests that tesamorelin effectively reduces triglyceride, total cholesterol and LDL-C levels. 2mg of tesamorelin for 26 weeks has been shown to decrease 15% of the visceral adipose tissue which is equivalent to a 50mg reduction in triglyceride levels [5, 6].
Research suggests that tesamorelin may help elderly patients suffering from dementia. One randomized double-blind placebo-controlled study found that GHRH analogs, including tesamorelin, increase the concentration of GABA (gamma-aminobutyric acid) and decrease myoinositol levels .
GABA is a neurotransmitter involved in regulating neuronal signalling in the hippocampus, a brain part responsible for episodic memory . On the other hand, an increased concentration of myo-inositol is associated with an increased risk of dementia .
5. Peripheral Nerve Damage
Damage to peripheral nerves can occur as a consequence of uncontrolled diabetes, surgical procedures and injury. This might often affect a person's ability to move and perform daily tasks. Currently, there is no treatment to reverse the damage as nerve cells are difficult to regenerate. However, research suggests that growth hormone-based therapies, including tesamorelin, might improve the condition and boost the rate of healing .
Tesamorelin is a synthetic peptide that mimics the activity of GHRH. It is chemically modified to extend its half-life and duration of action. Research shows that it might improve peripheral nerve damage, prevent cardiovascular diseases and alleviate dementia. However, its FDA approval is limited to the treatment of HIV-associated lipodystrophy. We don’t support its unwarranted use and offer the option to purchase tesamorelin exclusively for research and experimentation. Only buy tesamorelin if you are a qualified researcher.
- Bedimo, R., Growth hormone and tesamorelin in the management of HIV-associated lipodystrophy. HIV AIDS (Auckl), 2011. 3: p. 69-79.
- Mangili, A., et al., Predictors of Treatment Response to Tesamorelin, a Growth Hormone-Releasing Factor Analog, in HIV-Infected Patients with Excess Abdominal Fat. PLoS One, 2015. 10(10): p. e0140358.
- Falutz, J., et al., Long-term safety and effects of tesamorelin, a growth hormone-releasing factor analogue, in HIV patients with abdominal fat accumulation. Aids, 2008. 22(14): p. 1719-28.
- Clemmons, D.R., S. Miller, and J.C. Mamputu, Safety and metabolic effects of tesamorelin, a growth hormone-releasing factor analogue, in patients with type 2 diabetes: A randomized, placebo-controlled trial. PLoS One, 2017. 12(6): p. e0179538.
- Falutz, J., et al., Metabolic Effects of a Growth Hormone–Releasing Factor in Patients with HIV. New England Journal of Medicine, 2007. 357(23): p. 2359-2370.
- Stanley, T.L., et al., Reduction in visceral adiposity is associated with an improved metabolic profile in HIV-infected patients receiving tesamorelin. Clinical infectious diseases, 2012. 54(11): p. 1642-1651..
- Friedman, S.D., et al., Growth Hormone–Releasing Hormone effects on brain γ-Aminobutyric acid levels in mild cognitive impairment and healthy aging. JAMA neurology, 2013. 70(7): p. 883-890.
- Jiménez-Balado, J. and T.S. Eich, GABAergic dysfunction, neural network hyperactivity and memory impairments in human aging and Alzheimer's disease. Semin Cell Dev Biol, 2021. 116: p. 146-159.
- Beacher, F., et al., Hippocampal Myo-inositol and Cognitive Ability in Adults With Down Syndrome: An In Vivo Proton Magnetic Resonance Spectroscopy Study. Archives of General Psychiatry, 2005. 62(12): p. 1360-1365.
- Tuffaha, S.H., et al., Therapeutic augmentation of the growth hormone axis to improve outcomes following peripheral nerve injury. Expert Opinion on Therapeutic Targets, 2016. 20(10): p. 1259-1265.
High Performance Liquid Chromatography (HPLC)
Mass Spectrometry (MS)
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