CJC-1295: ~8 day half life, GH and IGF-1 Stimulator
- 08-10-2006, 11:36 PM
CJC-1295: ~8 day half life, GH and IGF-1 Stimulator
This is an extremely interesting peptide guys. Bioconjugation is absolutely amazing. Works better than PEGylation if it is a smaller peptide and can be conjugated, not all of them can and still function properly. The half-life of this stuff proves the technology though. In fact, this isn't me guessing on half life like with PEG-MGF, the study conducted said 5.8-8.1 days.
A new company will be offering it soon although I cannot release details for obvious reasons. There is no source posting on AM.
(written by LakeMountD)
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. This peptide has a benefit to side effect ratio that exceeds all others currently being legally sold and would make a great addition to ones training regimen or post cycle therapy.
Last edited by LakeMountD; 08-15-2006 at 01:55 PM.PharmD
- 08-11-2006, 12:03 AM
Originally Posted by jomi822PharmD
- 08-11-2006, 12:05 AM
08-11-2006, 06:51 AM
08-11-2006, 09:09 AM
Please tell me that the 'tropins aren't going away!!!! But Congrats on your new endeavors! I'm salivating for the new peps!!!Originally Posted by LakeMountD
08-11-2006, 10:44 AM
The tropins are part of IBE's line not Innovative Research, don't you worry, they will still be thereOriginally Posted by Bionic
08-11-2006, 01:12 PM
08-15-2006, 01:54 PM
10-20-2006, 03:57 PM
There has been some issues during the CJC clinical trails resulting in what appears to be a temporary hault in the trail. It seems very likely that the trail will be resumed but Innovative Research has decided to hold off on distributing this product for the time being.
Here is the news direct from the pharmaceutical company’s (ConjuChem) press release after the incident
Lipodystrophy study halted after patient death
A Phase II study of a lipodystrophy treatment developed by Canadian
biotech company, ConjuChem, has been halted after the death of a study
participant. The cause of death and its relationship to the study drug -
CJC-1295, a chemically modified version of growth hormone releasing
factor (GRF) also known as DAC:GRF - is currently being investigated.
However, a Phase III study of another Canadian-developed GRF-based
lipodystrophy treatment, Theratechnologies' TH-9507, is continuing.
The multicentre, randomised, placebo-controlled, double-blind Phase II
study of CJC-1295 had only completed enrolling a total of 192
participants with HIV-related visceral obesity at various sites in North
and South America last month. Participants were randomised to receive
once-weekly injections of either a three-week escalating low dose of
CJC-1295 (at 60, 90, 120mcg/kg); a three-week escalating high dose (at
60, 120, 240mcg/kg); or a placebo, and then continue for a further nine
The only information released so far by ConjuChem, which stopped the
study on July 17th, is that the participant who died was attending a
study site in Argentina. An unconfirmed, anecdotal report from a trial
participant at a Canadian study site, suggests that the individual
concerned was a man who died a few hours after receiving his eleventh
Here is the results of the investigation regarding the death of the man participating in the trail.
ConjuChem provides findings of DAC(TM):GRF HIV Lipodystrophy trial investigation
ConjuChem Biotechnologies Inc. provided findings of its investigation into the death of a patient that occurred in its Phase II clinical trial of DAC(TM):GRF in HIV Lipodystrophy.
MONTREAL, Canada | Aug 08, 2006 | ConjuChem Biotechnologies Inc. (TSX:CJB) provided findings of its investigation into the death of a patient that occurred in its Phase II clinical trial of DAC(TM):GRF in HIV Lipodystrophy. The Company had previously reported on July 14 that a death occurred of a patient in the trial at a clinical site in Argentina. The trial was an international multi-center, randomized, placebo-controlled, double-blind study which had completed enrollment with 192 patients.
Patients were to be administered once-weekly dosing of DAC(TM):GRF for 12 weeks followed by a 6-week follow-up. The deceased patient received the 11th weekly dose on July 13 and approximately two hours later, the patient complained of chest discomfort and an ECG confirmed an acute myocardial infarction; death occurred approximately one hour later.
There is no evidence of any cardiotoxic effects of DAC(TM):GRF in previous preclinical or clinical studies. The attending physician stated that his most likely explanation for the event was the patient had asymptomatic coronary artery disease with plaque rupture and occlusion.
ConjuChem indicated it has terminated the Phase II study and is further evaluating the clinical development strategy of DAC(TM): GRF.
As you can see, it appears that the CJC-1295 peptide had nothing to do with death of the man in the trial. He was an obese AIDs patient as all the other participants. The autopsy showed positive ECG results for the heart attack and further investigation confirmed large amounts of plaque in the arteries as said above leading to the eventual heart attack. It happens everyday unfortunately, especially in the overweight population.
The CJC peptide and the GRF from which it is derived have shown no potential risk factors, and no cardio toxic effects. In fact a competing company was doing a similar study and has continued it trail right through the incident. That alone should show the confidence that this was a totally random, isolated and unrelated incident from the clinical trail of the CJC-1295 peptide. It is still however the wishes of Innovative Research to hold off on releasing the product at least for a short period of time.
10-20-2006, 04:10 PM
That right there makes it hard to diagnose when you're doing drug trials on the already health compromised types.He was an obese AIDs patient as all the other participants.
10-20-2006, 04:13 PM
You have to take that up with ConjuChem, but my guess is they were looking for an overal low risk improvemtn in quality of life for these types of patients. Unfortunantly the pharmeceutical industry isn't geared towards researching on bodybuilders... We just don't pay as well I guess.Originally Posted by Jayhawkk
10-20-2006, 04:14 PM
10-20-2006, 05:57 PM
10-20-2006, 06:20 PM
10-20-2006, 06:29 PM
Playing smartass?Originally Posted by TheGame46
No, it's just weird when a colleague of mine puts out a post that makes it look like he came up with the idea and all that. I personally konw the guy who discovered GRF 1-44 and started this whole analogue thing in the first place. I use to own stock in his company and was heavily implicated in the promotion of this R&D outfit.
And because I am probably the most familiar by far with this molecule and its development history, I find it a little surprising when a colleage starts posting about it.
But go ahead LMD you're doing a good job.
10-21-2006, 04:17 AM
is innovative research and ibe somehow affiliated? did innovative research splinter off from ibe or something? sorry bout the dumb question feels strange being back here after a year or so.Originally Posted by LakeMountD
10-21-2006, 04:18 AM
strange in a good way lol. i was here when there would be like 30-40 people on at a time during peek hours. ok ill shut up. peace
10-21-2006, 06:37 AM
10-21-2006, 11:39 AM
Tell that to Stryder and USP as I watch my available balance go steadily down.Originally Posted by TheGame46
01-01-2007, 03:29 PM
01-03-2007, 06:07 PM
01-05-2007, 03:53 PM
I have a question.
what would be more effective, a peptide that makes the body release GH and IGF or injecting straight HGH and IGF peptides?
difference? totally different? ...way off base possibly?
01-12-2007, 02:44 PM
01-12-2007, 02:57 PM
01-12-2007, 03:29 PM
Sweet! Back to the original question then, anyone run it with feedback to give?Originally Posted by IBE
01-12-2007, 05:20 PM
01-12-2007, 06:00 PM
01-30-2008, 08:42 PM
What's up everyone, my first post, been lurking for a while. I've been really interested in cjc-1295 as well. Found this for those interested...
Prolonged Stimulation of Growth Hormone and IGF-1 Secretion by CJC-1295, a Long-acting Analogue of Growth Hormone-Releasing Hormone, in Healthy Adults
Sam L. Teichman, Ann Neale, Betty Lawrence, Catherine Gagnon, Jean-Paul Castaigne, and Lawrence A. Frohman*
WinPharm Associates, San Ramon CA.; ConjuChem, Inc., Montréal, Québéc, Canada; Section of Endocrinology, Department of Medicine, University of Illinois at Chicago, Chicago IL
* To whom correspondence should be addressed. E-mail: [email protected].
Context: Therapeutic use of growth hormone-releasing hormone (GHRH) to enhance GH secretion is limited by its short duration of action.
Objective: To examine the pharmacokinetic profile, pharmacodynamic effects, and safety of CJC-1295, a long-acting GHRH analog.
Design: Two randomized, placebo-controlled, double-blind, ascending dose trials with durations of 28 and 49 days.
Setting: Two investigational sites.
Participants: Healthy subjects, ages 21 to 61 yr.
Interventions: sc administration of CJC-1295 or placebo in one of 4 ascending single doses in the first study and in 2 - 3 weekly or biweekly doses in the second study.
Main Outcome Measures: Peak concentrations and area under the curve (AUC) of GH and IGF-1; standard pharmacokinetic parameters for CJC-1295.
Results: After a single injection of CJC-1295, there were dose-dependent increases in mean plasma GH concentrations by 2-10 fold for 6 days and in mean plasma IGF-1 concentrations by 1.5- to 3-fold for 9 - 11 days. The estimated half-life of CJC-1295 was 5.8 - 8.1 days. After multiple CJC-1295 doses, mean IGF-1 levels remained above baseline for up to 28 days. No serious adverse reactions were reported.
Conclusions: sc administration of CJC-1295 resulted in sustained, dose-dependent increases in GH and IGF-1 levels in healthy adults and was safe and relatively well-tolerated, particularly at doses of 30 µg/kg or 60 µg/kg. There was evidence of a cumulative effect after multiple doses. These data support the potential utility of CJC-1295 as a therapeutic agent.
09-22-2008, 06:08 PM
09-22-2008, 06:14 PM
Seriously...have you not seen datbtrue's thread in this forum? It'll answer all of your questions regarding growth hormone secretagogues.
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