Growth Hormone - Releasing Hormone CJC by KEIFEI® PHARMA

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Growth Hormone - Releasing Hormone CJC by KEIFEI® PHARMA

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Releasing Hormone CJC-1295

Regular Price: €200.00

Special Price €180.00

   

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Delivery: 1 box   10vial



Presentation: Each 2ml multidose vial contains 2 mg/vial. Orange colour cap with KeiFei wording stamp on it.
CJC-1295 is a Long-acting growth-hormone-releasing hormone (GHRH) analog. Because of the long half-life
and stability of the CJC-1295 analog, it appears to become more and more popular.


CJC-1295 is a Long acting GHRH analog. Growth-hormone-releasing hormone (GHRH), also known as
growth-hormone-releasing factor (GRF or GHRF) or somatocrinin, is a 44-amino acid peptide hormone
produced in the hypothalamus by the arcuate nucleus. GHRH stimulates growth hormone (GH) secretion
from the pituitary. GHRH is released in a pulsatile manner, stimulating pulsatile release of GH respectively.
In addition, GHRH also promotes slow-wave sleep. The active portion of this GRF or GHRH 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.
CJC-1295 is a synthetic modification of growth hormone releasing factor (GRF) 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. By applying the Drug Affinity Complex (DAC) technology to GRF, the peptide
selectively and covalently binds to circulating albumin after subcutaneous (SC) administration, thus prolonging
its half-life. 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.