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What are GHRP-2 Benefits

The research peptide GHRP-2 was originally discovered by Zettler. It has been used in clinical practice for the treatment of short stature caused by growth hormone deficiency. The research GHRP-2 is used in a single-dose oral (PO) formulation and a multidose subcutaneous (SC) formulation.

GHRP-2 is generally used in children and adults under 3.5 to 5 years of age for treatment of short stature due to growth hormone deficiency. It is also used to increase the lean body mass and bone mineral density in chronic renal failure and elderly patients in the United States. GHRP-2 is also under investigation for the treatment of wasting, obesity, sarcopenia, Alzheimer’s disease, and cancers.

What is GHRP used for?

GHRP-2 is a synthetic analog of met-enkephalin, a naturally occurring opioid peptide that has been studied for years as a pain killer. The met-enkephalin molecule is made up of eleven amino acids. The GHRP-2 is similar, containing 11 amino acids with a sequence of RLLR-NH2 at the carboxy-terminal end. GHRP-2 does not contain opioid or opiate receptors in humans but has been shown to bind to the GHSR in rat brains. It’s a secretagogue and stimulates the release of growth hormone and insulin-like growth factor-1 from the pituitary.

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A single dose of GHRP-2 will increase insulin-like growth factor-1 concentrations in serum by about 1.5 fold. It also stimulates the metabolism of carbohydrates and fat, which increases oxygen consumption and carbon dioxide output.

How Does GHRP-2 Dosage Work?

GHRP-2, like other peptide hormones, acts by binding to GHS receptors (GHSR) to activate G proteins, which stimulate G proteins. A diagram of this process is shown in the figure below.

GHRP-2 causes these events by interacting with GHSR, which is a part of a G protein-coupled receptor. The GHS receptor activates the G-protein complex. The G-protein complex then activates its own proteins which stimulate phospholipase C (PLC). This leads to the breakdown of phosphatidylinositol, thus producing inositol triphosphate (IP3). IP3 opens the calcium channel in the sarcoplasmic reticulum (SR), which causes the release of calcium ions from the SR into the cytoplasm. When this happens, adenosine triphosphate (ATP) is released into the cytoplasm, and in turn, the Ca2+ ATPase pump removes it.

How long does it take for GHRP-2 to work?

The above process causes an increase in cytoplasmic free calcium ion levels. Calcium binds to calmodulin, activating protein kinase C. Protein kinase C, in turn, phosphorylates phospholipase A2 (PLA2), which then activates PLA2, thus initiating the arachidonic acid cascade. Arachidonic acid is converted by 5-lipoxygenase to leukotrienes and 5-hydroperoxy eicosatetraenoic acid (5-HpETE) by peroxidases. 5-HpETE activates protein kinase C, leading to activation of PLA2 by calcium. This process is the basic mechanism for the production of inflammatory mediators. GHRP-2, by stimulation of phospholipase A2, also leads to the release of eicosanoids, such as arachidonic acid and leukotrienes, as well as prostaglandins.

What are the possible GHRP-2 side effects?

The FDA has stated in its package insert that the risks of GHRP-2 can vary greatly from patient to patient. The table below is a summary of some of the adverse events of GHRP-2 reported by the manufacturer.

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