CJC-1295 With DAC targets the growth hormone-releasing hormone receptor (GHRH-R), a G protein-coupled receptor expressed on somatotropic cells in the anterior pituitary gland. Upon binding to this receptor, it mimics the action of endogenous GHRH and stimulates the synthesis and pulsatile secretion of growth hormone (GH) from the pituitary. The DAC moiety does not alter receptor binding affinity but serves to prolong systemic exposure through reversible albumin association. This receptor-mediated mechanism activates intracellular signaling cascades including the cAMP/PKA pathway, ultimately leading to increased expression and release of GH and its downstream effector, insulin-like growth factor 1 (IGF-1).

In vitro studies demonstrate that CJC-1295 With DAC maintains potent and sustained activation of GHRH receptors in pituitary cell models, with the DAC modification not interfering with receptor binding or signaling efficacy. The peptide stimulates GH secretion from primary pituitary cell cultures in a concentration-dependent manner, with potency comparable to native GHRH. Immuno-polymerase chain reaction (I-PCR) assays using monoclonal antibodies raised against CJC-1295 With DAC can detect the peptide-protein conjugate at concentrations as low as 0.8 pg/mL, demonstrating high sensitivity for in vitro quantification. The compound also exhibits stability in serum-containing media, attributed to the protective effect of the DAC-albumin interaction.

CJC-1295 With DAC is a 30 amino acid peptide-based drug that stimulates the release of growth hormone (GH) from the pituitary gland. It is unique among performance-enhancing peptides due to the presence of a reactive maleimidopropionic acid group that covalently links the peptide to free thiols on the surface of plasma proteins. Once conjugated, CJC-1295 With DAC remains active in the bloodstream for significantly longer than non-conjugated peptide-based drugs that are rapidly excreted. Conjugation of CJC-1295 With DAC to plasma proteins prevents its detection by top-down mass-spectrometry-based peptide screening protocols as it effectively becomes a macromolecular protein with an undefined molecular weight. Using a pair of monoclonal antibodies raised against the CJC-1295 With DAC peptide, we present an immuno-polymerase chain reaction (I-PCR) assay that is capable of detecting the CJC-1295 With DAC-protein conjugate at concentrations down to 0.8 pg/mL. Detection of endogenous equine GHRH necessitated a screening threshold for CJC-1295 With DAC in equine plasma of 50 pg/mL. The effectiveness of the assay for controlling the illicit use of CJC-1295 With DAC was confirmed in equine blood samples after administration in thoroughbred race horses [1].

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In vivo, CJC-1295 With DAC exhibits significantly prolonged activity compared to unconjugated GHRH analogs due to its high-affinity binding to serum albumin via the DAC moiety. This albumin association creates a circulating reservoir that slowly releases active peptide, resulting in sustained stimulation of GH release over an extended period. Pharmacodynamic studies show that a single administration can elevate GH and IGF-1 levels for days rather than hours, a marked improvement over native GHRH which has a half-life of only a few minutes. This extended duration of action has made it a valuable research tool for studying chronic GHRH receptor activation and its metabolic consequences.

In vitro enzyme/receptor binding assays for CJC-1295 With DAC typically employ competition binding experiments using radiolabeled GHRH or fluorescently labeled peptide analogs on membrane preparations from cells overexpressing the human GHRH receptor. The DAC-conjugated peptide is incubated with varying concentrations of the receptor preparation, and bound versus free ligand is separated by filtration or centrifugation. Non-specific binding is determined in the presence of excess unlabeled GHRH. Binding affinity (Kd) and competitive inhibition constants (Ki) are calculated from saturation and displacement curves. Additionally, I-PCR-based immunoassays using monoclonal antibodies specific to the CJC-1295 DAC peptide can quantify peptide-protein conjugate formation as a surrogate for receptor engagement.

In vitro cellular assays for CJC-1295 With DAC utilize primary pituitary cell cultures or recombinant cell lines expressing the human GHRH receptor. Cells are treated with escalating concentrations of the peptide for defined time periods, typically 4-24 hours, and GH secretion into the culture medium is measured by enzyme-linked immunosorbent assay (ELISA) or radioimmunoassay (RIA). Intracellular signaling is assessed by quantifying cAMP accumulation using competitive immunoassays or by measuring downstream phosphorylation events via Western blot. The EC50 for GH stimulation and the kinetics of receptor desensitization or internalization can be determined. Assays are performed in serum-free or low-serum media to minimize interference from albumin binding.

In vivo animal studies with CJC-1295 With DAC are typically conducted in rodent models (rats or mice) to evaluate its pharmacokinetic and pharmacodynamic properties following subcutaneous or intravenous administration. Animals are dosed at various concentrations, and blood samples are collected at multiple time points post-administration to measure plasma levels of the peptide, GH, and IGF-1 by immunoassay. The extended half-life and sustained pharmacodynamic response are characterized by comparing AUC and peak concentration values against those of unconjugated GHRH analogs. Long-term studies may involve repeated dosing regimens to assess effects on body weight, tissue growth, and metabolic parameters in both healthy and disease-model animals.

CJC-1295 With DAC demonstrates profoundly altered pharmacokinetics compared to native GHRH or unconjugated synthetic analogs due to its reversible covalent binding to serum albumin via the DAC moiety. This albumin interaction creates a circulating depot that significantly prolongs the peptide's elimination half-life from minutes to several days in preclinical models. The peptide exhibits a slow release profile from the albumin complex, maintaining sustained plasma concentrations and continuous GHRH receptor occupancy. Bioavailability following subcutaneous administration is high, and the compound shows limited tissue distribution beyond the vascular compartment, consistent with its predominantly albumin-bound state in circulation.

Toxicological evaluation of CJC-1295 With DAC is limited in publicly available literature; however, its clinical development was reportedly discontinued after a fatality occurred in a trial subject. Preclinical safety studies in animal models would have assessed standard endpoints including acute and repeat-dose toxicity, genotoxicity, and local tolerance at injection sites. As a peptide hormone analog, potential toxicities are likely related to exaggerated pharmacology, including excessive GH and IGF-1 elevation leading to acromegaly-like effects, insulin resistance, fluid retention, and joint pain. Long-term exposure may also carry theoretical risks of neoplasia due to the mitogenic effects of sustained GH/IGF-1 signaling.

[1]. An immuno polymerase chain reaction screen for the detection of CJC-1295 With DAC and other growth-hormone-releasing hormone analogs in equine plasma. Drug Test Anal. 2019 Jun;11(6):804-812.

Background: Folk pharmacology circulating online fuels the desire for rapid muscle gain, fat loss, and youthful skin. Objective: This study uses internet ethnography to explore the use of synthetic growth hormone analogue CJC-1295 (including DAC) by women from the perspective of internet forum activities. Methods: A systematic internet search was conducted using "CJC-1295 (including DAC)" and its variants, combined with the term "forum." 96 results related to bodybuilding websites were retrieved, mentioning CJC-1295 (including DAC). Exclusion criteria were applied, limiting the search to female use and forum activity, ultimately retaining 9 websites. Internal searches were conducted on these websites to find content related to CJC-1295 (including DAC). Finally, 23 discussion posts related to female use of CJC-1295 (including DAC) were obtained and analyzed using empirical phenomenological psychology methods. Results: Forum users appeared to be very familiar with and experienced in the combined use of various supplements to enhance athletic performance and improve appearance. The primary reasons for choosing to use CJC-1295 in combination with DAC were weight loss, muscle enhancement, maintaining youthful skin, improving sleep, and promoting wound healing. Users also expressed concerns about female use of the drug, as gender differences in growth hormone pulses can affect dosage estimation, duration of use, and long-term consequences. Conclusion: Public health interventions should include women's self-use of synthetic growth hormone in the category of product supplements, taking into account the associated adverse health consequences. [Subst Use Misuse. 2016 Jan 2;51(1):73-84]

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CJC-1295 With DAC is a synthetic GHRH analog incorporating a drug affinity complex that binds serum albumin for extended half-life. Its mechanism of action involves prolonged GHRH receptor agonism leading to sustained GH secretion. While it advanced into clinical investigation for lipodystrophy and GH deficiency, development was halted following a subject death. The compound remains a research tool for studying long-acting peptide delivery and continuous GHRH receptor signaling. It is not FDA-approved for any indication and is available only for laboratory research purposes. No ongoing clinical trials have been identified in major registries.

C165H269N47O46

3647.28

3646.019

446262-90-4

91971820

Tyr-D-Ala-Asp-Ala-Ile-Phe-Thr-Gln-Ser-Tyr-Arg-Lys-Val-Leu-Ala-Gln-Leu-Ser-Ala-Arg- Lys-Leu-Leu-Gln-Asp-Ile-Leu-Ser-Arg-Lys(Maleimidopropionyl)-NH2

White powder

-11.7

54

52

128

258

8580

33

CC[C@H](C)[C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCNC(=O)CCN3C(=O)C=CC3=O)C(=O)N)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@H](CC4=CC=C(C=C4)O)N

ZUQGTWKGESAQCD-ZGFIGYLBSA-N

InChI=1S/C165H269N47O46/c1-22-87(15)130(209-137(233)92(20)185-148(244)116(76-127(225)226)196-136(232)89(17)183-138(234)99(168)73-95-44-48-97(217)49-45-95)160(256)204-115(74-94-36-25-24-26-37-94)154(250)211-132(93(21)216)162(258)195-108(54-57-123(171)221)145(241)205-120(80-215)158(254)200-114(75-96-46-50-98(218)51-47-96)153(249)192-105(43-35-66-182-165(177)178)141(237)191-102(40-28-31-62-167)146(242)208-129(86(13)14)159(255)202-109(68-81(3)4)147(243)184-90(18)135(231)189-106(52-55-121(169)219)143(239)198-112(71-84(9)10)151(247)206-118(78-213)156(252)186-91(19)134(230)188-103(41-33-64-180-163(173)174)140(236)190-101(39-27-30-61-166)142(238)197-111(70-83(7)8)150(246)199-110(69-82(5)6)149(245)194-107(53-56-122(170)220)144(240)201-117(77-128(227)228)155(251)210-131(88(16)23-2)161(257)203-113(72-85(11)12)152(248)207-119(79-214)157(253)193-104(42-34-65-181-164(175)176)139(235)187-100(133(172)229)38-29-32-63-179-124(222)60-67-212-125(223)58-59-126(212)224/h24-26,36-37,44-51,58-59,81-93,99-120,129-132,213-218H,22-23,27-35,38-43,52-57,60-80,166-168H2,1-21H3,(H2,169,219)(H2,170,220)(H2,171,221)(H2,172,229)(H,179,222)(H,183,234)(H,184,243)(H,185,244)(H,186,252)(H,187,235)(H,188,230)(H,189,231)(H,190,236)(H,191,237)(H,192,249)(H,193,253)(H,194,245)(H,195,258)(H,196,232)(H,197,238)(H,198,239)(H,199,246)(H,200,254)(H,201,240)(H,202,255)(H,203,257)(H,204,256)(H,205,241)(H,206,247)(H,207,248)(H,208,242)(H,209,233)(H,210,251)(H,211,250)(H,225,226)(H,227,228)(H4,173,174,180)(H4,175,176,181)(H4,177,178,182)/t87-,88-,89+,90-,91-,92-,93+,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,112-,113-,114-,115-,116-,117-,118-,119-,120-,129-,130-,131-,132-/m0/s1

(3S)-4-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-6-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-6-[3-(2,5-dioxopyrrol-1-yl)propanoylamino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxohexan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-4-oxobutanoic acid

CJC-1295 With DAC; CID 91971820

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

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Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).

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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline)

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Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).

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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

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Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

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 (Please use freshly prepared in vivo formulations for optimal results.)