Manufacturer: Generic GENSCI
Substance: 98% purity GHRH Analog
Pack: 1 vial
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. Over 98% purity
CJC-1295: 1mg/vial or 2mg/vial
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. 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.
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