Overview
CJC-1295 + Ipamorelin is a two-peptide research blend supplied in a single vial: CJC-1295, a long-acting analogue of growth hormone-releasing factor (GRF, also GHRH), and ipamorelin, a selective growth hormone secretagogue acting at the ghrelin (GHRP) receptor. The two constituents act at different receptors on the growth hormone axis1,4.
Each constituent has its own published literature, mostly from rodent and swine models. CJC-1295 was identified in 2005 as a tetrasubstituted hGRF(1-29) analogue with an extended plasma half-life1, and ipamorelin was described in 1998 as the first GHRP-receptor agonist with a selectivity for growth hormone release similar to that of GHRH4. No published study has examined the combination itself; the sections below summarise each constituent separately.
Mechanism of action
As described in the research literature
As described in the research literature, CJC-1295 is a tetrasubstituted form of hGRF(1-29) with an added maleimidopropionamide-modified lysine at the C terminus, designed to bind covalently to serum albumin. In the originating study it showed enhanced in vitro stability against dipeptidylpeptidase-IV, was active in a growth hormone secretion assay in cultured rat anterior pituitary cells, and was detected bound to albumin in rat plasma1.
Ipamorelin is a pentapeptide (Aib-His-D-2-Nal-D-Phe-Lys-NH2) identified within a series of compounds lacking the central Ala-Trp dipeptide of GHRP-1. Pharmacological profiling with GHRP and GHRH antagonists indicated that it releases growth hormone via a GHRP-like receptor. In swine, it did not raise FSH, LH, prolactin or TSH, and, unlike GHRP-6 and GHRP-2, did not raise ACTH or cortisol above the levels seen with GHRH4.
Research areas
What published studies have examined
CJC-1295: GRF receptor pharmacology
Three maleimido derivatives of hGRF(1-29) were synthesised, bioconjugated to human serum albumin and compared for stability, pituitary cell activity and growth hormone release in rats; CJC-1295 was selected for pharmacokinetic evaluation1.
Sources [1]
CJC-1295: growth in GHRH knockout mice
A study in mice lacking the GHRH gene examined body weight and length, femur and tibia length, body composition, pituitary GH mRNA and somatotroph proliferation across different study protocols2.
Sources [2]
CJC-1295: registered clinical studies
Two randomised, placebo-controlled, double-blind phase 1 trials in healthy adults were designed to examine the pharmacokinetics, pharmacodynamics and safety of CJC-1295, with peak concentration and area under the curve of GH and IGF-I as the main outcome measures3.
Sources [3]
Ipamorelin: selectivity and pituitary pharmacology
Growth hormone release was compared with GHRP-6 and GHRP-2 in primary rat pituitary cells, anaesthetised rats and conscious swine, alongside measurement of ACTH, cortisol and other pituitary hormones4.
Sources [4]
Ipamorelin: bone and gastrointestinal models
Studies in female rats examined longitudinal bone growth by tetracycline labelling5 and bone mineral content by DXA and peripheral quantitative CT6. A rat model of postoperative ileus examined colonic transit, faecal output, food intake and body weight after laparotomy and intestinal manipulation7.
Sources [5] [6] [7]
Specifications
- Constituents
- CJC-1295 and ipamorelin, in equal amounts: 5 mg + 5 mg or 10 mg + 10 mg per vial
- CJC-1295
- Tetrasubstituted analogue of hGRF(1-29), the first 29 residues of growth hormone-releasing factor
- Ipamorelin sequence
- Aib-His-D-2-Nal-D-Phe-Lys-NH2
- Ipamorelin formula and weight
- C38H49N9O5, 711.9 g/mol
- Ipamorelin CAS number
- 170851-70-4
- Form
- White to off-white lyophilised powder in a sealed vial (5 mg + 5 mg or 10 mg + 10 mg)
- Storage
- Store lyophilised powder at -20 °C, protected from light and moisture. Once reconstituted, keep refrigerated at 2 to 8 °C and protect from light.
- Solubility and reconstitution
- Reconstitute with bacteriostatic water. Add the diluent slowly down the inside wall of the vial and swirl gently until clear; do not shake.
References
- 1
Human growth hormone-releasing factor (hGRF)1-29-albumin bioconjugates activate the GRF receptor on the anterior pituitary in rats: identification of CJC-1295 as a long-lasting GRF analog.
Jetté L, Léger R, Thibaudeau K, et al. Endocrinology, 2005.
PubMed 15817669 ↗DOI 10.1210/en.2004-1286 ↗
- 2
Once-daily administration of CJC-1295, a long-acting growth hormone-releasing hormone (GHRH) analog, normalizes growth in the GHRH knockout mouse.
Alba M, Fintini D, Sagazio A, et al. American Journal of Physiology. Endocrinology and Metabolism, 2006.
PubMed 16822960 ↗DOI 10.1152/ajpendo.00201.2006 ↗
- 3
Prolonged stimulation of growth hormone (GH) and insulin-like growth factor I secretion by CJC-1295, a long-acting analog of GH-releasing hormone, in healthy adults.
Teichman SL, Neale A, Lawrence B, et al. The Journal of Clinical Endocrinology and Metabolism, 2006.
PubMed 16352683 ↗DOI 10.1210/jc.2005-1536 ↗
- 4
- 5
- 6
The GH secretagogues ipamorelin and GH-releasing peptide-6 increase bone mineral content in adult female rats.
Svensson J, Lall S, Dickson SL, et al. The Journal of Endocrinology, 2000.
PubMed 10828840 ↗DOI 10.1677/joe.0.1650569 ↗
- 7
Efficacy of ipamorelin, a novel ghrelin mimetic, in a rodent model of postoperative ileus.
Venkova K, Mann W, Nelson R, et al. The Journal of Pharmacology and Experimental Therapeutics, 2009.
PubMed 19289567 ↗DOI 10.1124/jpet.108.149211 ↗