New long lasting peptide
- 10-14-2006, 01:19 PM
New long lasting peptide
Long-Acting GHRH Analog (CJC-1295) Stimulates GH and IGF-1 Secretion in Normal Adults for Up to Two Weeks After a Single Injection. CJC will keep a steady increase of HGH and IGF-1 for with no increase in prolactin
GHRH1-44, also known as Growth Hormone Releasing Hormone (other synonyms are GRF and GHRF), is a peptide that is produced in the hypothalamus and secreted to stimulate the release of human growth hormone (hGH). It consists of a 44 amino acid long sequence and is released in a pulsatile fashion similar to the pulsatile release of hGH. The active portion of this peptide can be found as a 29 amino acid long peptide and is appropriately named GHRH1-29. This pulsatile release of various peptides is due to the negative feedback loop that is part of the hGH axis and controls the amount of hGH that your body produces to keep it in a homeostatic environment. Despite the effectiveness of GHRH to stimulate growth hormone release there are a number of problems associated with using it in vivo. The most noteworthy problem is the half life of the peptide, which has been shown to be ~7 minutes using advanced HPLC technologies that have proven to be very accurate. The reason for this relatively short half life is due to an enzyme called dipeptidylaminopeptidase IV (DPP-IV), which has a high affinity for the amino acids Ala and Pro and in the case of GHRH it cleaves the 1 and 2 positions that consist of Tyr-Ala, creating GHRH3-29, an inactive form of the peptide. To prevent the problems associated with natural GHRH, pharmaceutical companies looked at new ways to increase the half life and bioavailability of these smaller peptides with technologies that work far different than other technologies, such as PEGylation.
This brings us to the introduction of a far more stable form of GHRH called CJC-1295. CJC-1295 is a tetrasubstituted peptide analogue of GHRH with D-Ala, Gln, Ala, and Leu substitutions at positions 2, 8, 15, and 27 respectively. These substitutions create a much more stable peptide with the substitution at position 2 to prevent DPP-IV cleavage, position 8 to reduce asparagine rearrangement or amide hydrolysis to aspartic acid, position 15 to enhance bioactivity, and position 27 to prevent methionine oxidation. These substitutions are key in increasing the overall half life of CJC-1295 but there lies an even greater reason as to why the half life has been extended from ~7 minutes to greater than 7 days! Bioconjugation is a relatively newer technology that takes a reactive group and attaches it to a peptide, which in turn reacts with a nucleophilic (usually a partially negative molecule) entity found in the blood to form a more stable bond. Albumin, one of the most abundant substances in the human body is chosen as the nucelophile by this particular peptide thanks to a Cys34 thiol group that attracts it. By combining the tetrasubstituted GHRH analogue with maleimodoproprionic acid using a Lys linker, you create a GHRH peptide with a high binding affinity for albumin. Once the CJC-1295 molecule has attached itself to albumin, it is given an extended half life and bioavailability thanks to the albumin preventing enzymatic degredation and kidney excretion. In fact, bioconjugation is so effective that there was less than 1% of CJC-1295 left unreacted in vivo and over 90% was stabilized after subcutaneous injection. This means that you get more of what you paid for working for you. There was no DPP-IV degredation observed on CJC-1295 in any of the various experiments conducted.
Due to the extremely long half life of CJC-1295 it is plausible to use this peptide once per week with outstanding results. Much like compounds such as testosterone enanthate, however, it would be wiser to use ½ dosages twice per week to keep serum levels high and to get maximal GH release and limit the pulsatile fashion of hGH. Various experiments have been conducted to test the effectiveness of CJC-1295 in vivo and the Journal of Clinical Endocrinology & Metabolism has reported dose-dependent increases in mean plasma GH concentrations by 2-10 fold for more than 6 days and increased IGF-1 concentrations 1.5-3 fold for 9-11 days after a single injection! Not only that but they proved the mean half life to be 5.8-8.1 days and after multiple doses showed mean IGF-1 levels remained above baseline for up to 28 days following! No serious adverse reactions were reported in any group. The graphs below show that this peptide has the ability to stimulate growth hormone very significantly and is much more cost effective than illegally buying hGH.
Another very positive benefit of CJC-1295 is its ability to promote slow wave sleep. Slow wave sleep is also known as deep sleep and is the portion of sleep responsible for the highest level of muscle growth and memory retention. SWS is decreased significantly in older adults and also with people who tend to exercise later in the evening.
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