Hexarelin (Examorelin) 2mg

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Hexarelin Acetate, Hexarelin 2mg

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  • Hexarelin HPLC
  • Hexarelin MS


 

Hexarelin (Examorelin)

Hexarelin is a synthetic growth hormone secretagogue. It is derived from GHRP-6 and has effects similar to ghrelin. The primary function of hexarelin, as shown in animal research models, is to increase plasma levels of growth hormone and promote the development of lean body mass.

Indirectly, hexarelin has been shown to improve cardiac function, lower lipid levels, and protect against the effects of certain chemotherapeutic agents. The peptide is currently under investigation for its ability to mitigate the effects of certain metabolic diseases, such as diabetes.

 

Hexarelin Peptide

Molecular Formula: C47H58N12O6

Molecular Mass: 887.04022

Amino Acid Sequence: His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys

 

Hexarelin Research Applications

There are several active areas of hexarelin research, with the most prominent involving metabolic conditions like diabetes. Hexarelin has recently been shown to activate CD36-PPARγ[1]. PPARs (Peroxisome proliferator-activated receptors) are the target of many pharmaceuticals (e.g. thiazolidinediones) that improve insulin resistance. Improving insulin resistance helps to lower blood sugar levels in type 2 diabetes and regulate lipid metabolism.

 

Closely linked to research in metabolic disease is research investigating the cardiac protective effects of hexarelin[2]. The peptide can improve cardiac function in the setting of chronic heart failure, protect heart muscle following heart attack, and reduce the formation of atherosclerotic plaques. Recently, studies designed to test the magnitude of hexarelin’s effect on the health of cardiomyoctes has revealed that the peptide is able to reduce scar formation following heart attack. In fact, mice given hexarelin following cardiac ischemia show significant improvement in several cardiac parameters after just 14 days. Long-term remodeling is also favorably influence, reducing the severity of the lifelong complications that often follow after heart attack[3], [4].

 

What Is Hexarelin?

Hexarelin (also called examorelin) is a synthetic ghrelin/growth hormone secretagogue similar to and derived from GHRP-6. The hexapeptide consists of His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys, making it similar to GHRP-6 with the exception of the methyl-tryptophan at the second position.

 

What Does Hexarelin Do?

Like GHRP-6, hexarelin causes substantial, dose-dependent increases in growth hormone. In fact, hexarelin causes more substantial increases in growth hormone than naturally secreted growth hormone releasing hormone dose[5].

 

Unlike GHRP-6, hexarelin does not produce substantial changes in prolactin, adrenocorticotropic hormone, or cortisol. It has no effect on glucose levels, luteinizing hormone, follicle stimulating hormone, or thyroid stimulating hormone.

 

Hexarelin Metabolic Research

The primarily applications for hexarelin research effects on metabolism revolve around insulin resistance and lipid metabolism. Hexarelin has been shown to substantially improve insulin resistance in diabetic rats through activation of PPARγ and beta cells of the pancreas. Research has suggested that hexarelin not only improves the functioning of existing beta cells, but actually helps the pancreas to recover and regenerate beta cells[2].

 

Lipid metabolism is the second area of metabolic research involving hexarelin. Abnormal lipid metabolism is an independent risk factor for diabetes. Even in non-obese individuals, abnormal lipid metabolism can lead to the development of type 2 diabetes. Studies in non-obese mice with dysfunctional fat metabolism has revealed that hexarelin significantly improves plasma glucose levels, which in turn reduces insulin secretion from the pancreas and long-term risk for the development of diabetes[6].

 

Hexarelin Cardiac Research

There is a great deal of research focusing on the cardiac effects of hexarelin. The peptide has strong cardioprotective benefits, particularly in cases of cardiac injury. In fact, hexarelin has been shown to inhibit apoptosis following myocardial infarction. This, in turn, reduces the amount of damage done to the heart (infarct size) in the short term. A reduction in short-term damage leads to a reduction in scar formation and thus long-term complications. Mice treated with hexarelin following cardiac ischemia demonstrated improved ejection fraction, reduced vascular resistance, and improved outcomes compared to controls. What is more, hexarelin has been shown to reduce atherosclerotic deposits in arteries, improving vascular health and reducing the risk of heart attack and stroke[3], [7]–[10].

 

Hexarelin Protective Benefits

Hexarelin protects skeletal muscle in mouse models by preventing apoptosis and muscle wasting. This is particularly true in models of muscle wasting conditions (e.g. chemotherapy treatment). Research suggests that hexarelin protects muscle tissue by regulating calcium homeostasis[11]. This effect is particularly important during episodes of muscle ischemia, in certain disease states, and during traumatic injury to muscle.

 

Hexarelin and Chemotherapy

As noted above, hexarelin protects several different types of muscle tissue, particularly during ischemic or low-nutrient states. For this reason, hexarelin has been of intense interest as a potential adjunct treatment for cancer. While there is some evidence to indicate that hexarelin directly affects cancer cells, the primary interest among scientists is in the ability of hexarelin to protect muscle tissue against the damaging effects of chemotherapy. Heart damage, in particular, is a frequent side effect of chemotherapeutics, particularly the platinum-based drugs. By limiting muscle wasting, hexarelin may be beneficial in improving long-term survival and even rates of remission in cancer by allowing higher doses of otherwise toxic drugs to be used[12].

 

Resources

[1]          L. Maréchal et al., “The CD36-PPARγ Pathway in Metabolic Disorders,” Int. J. Mol. Sci., vol. 19, no. 5, May 2018.

[2]          R. M. H. Mosa, Z. Zhang, R. Shao, C. Deng, J. Chen, and C. Chen, “Implications of ghrelin and hexarelin in diabetes and diabetes-associated heart diseases,” Endocrine, vol. 49, no. 2, pp. 307–323, Jun. 2015.

[3]          H. McDonald et al., “Hexarelin treatment preserves myocardial function and reduces cardiac fibrosis in a mouse model of acute myocardial infarction,” Physiol. Rep., vol. 6, no. 9, p. e13699, May 2018.

[4]          X. Zhang, L. Qu, L. Chen, and C. Chen, “Improvement of cardiomyocyte function by in vivo hexarelin treatment in streptozotocin-induced diabetic rats,” Physiol. Rep., vol. 6, no. 4, Feb. 2018.

[5]          M. Maccario et al., “Metabolic modulation of the growth hormone-releasing activity of hexarelin in man,” Metab. - Clin. Exp., vol. 44, no. 1, pp. 134–138, Jan. 1995.

[6]          R. Mosa et al., “Hexarelin, a Growth Hormone Secretagogue, Improves Lipid Metabolic Aberrations in Nonobese Insulin-Resistant Male MKR Mice,” Endocrinology, vol. 158, no. 10, pp. 3174–3187, Oct. 2017.

[7]          Y. Mao, T. Tokudome, and I. Kishimoto, “The cardiovascular action of hexarelin,” J. Geriatr. Cardiol. JGC, vol. 11, no. 3, pp. 253–258, Sep. 2014.

[8]          X. Xu et al., “Chronic administration of hexarelin attenuates cardiac fibrosis in the spontaneously hypertensive rat,” Am. J. Physiol. Heart Circ. Physiol., vol. 303, no. 6, pp. H703-711, Sep. 2012.

[9]          Y. Ma, L. Zhang, B. S. Launikonis, and C. Chen, “Growth hormone secretagogues preserve the electrophysiological properties of mouse cardiomyocytes isolated from in vitro ischemia/reperfusion heart,” Endocrinology, vol. 153, no. 11, pp. 5480–5490, Nov. 2012.

[10]        Y. Ma, L. Zhang, J. N. Edwards, B. S. Launikonis, and C. Chen, “Growth hormone secretagogues protect mouse cardiomyocytes from in vitro ischemia/reperfusion injury through regulation of intracellular calcium,” PloS One, vol. 7, no. 4, p. e35265, 2012.

[11]        A. Liantonio et al., “Growth hormone secretagogues exert differential effects on skeletal muscle calcium homeostasis in male rats depending on the peptidyl/nonpeptidyl structure,” Endocrinology, vol. 154, no. 10, pp. 3764–3775, Oct. 2013.

[12]        G. Sirago et al., “Growth hormone secretagogues hexarelin and JMV2894 protect skeletal muscle from mitochondrial damages in a rat model of cisplatin-induced cachexia,” Sci. Rep., vol. 7, no. 1, p. 13017, Oct. 2017.

 

 

Hexarelin

Hexarelin Acetate

Sequence: His-D-2-methyl-Trp-Ala-Trp-D-Phe-Lys-NH2
Molecular formula: C47H58N12O6
Molar Mass: 887.04022
CAS number: 140703-51-1
PubChem: CID 5464109
Synonyms: Hexarelin Acetate, HEX, Examorelin

Hexarelin Acetate