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Free U.S. shipping on orders over $150Ipamorelin is a synthetic pentapeptide that stimulates the pituitary to release growth hormone (GH). Since its discovery in 1998, it has gained a lot of attention as the first selective GH secretagogue.
It stimulates GH release without affecting other pituitary hormones such as adrenocorticotropic hormone, follicle-stimulating hormone, luteinizing hormone, thyroid-stimulating hormone, and prolactin.
Ipamorelin has primarily been researched preclinically for muscle gain and weight loss, as well as for counteracting corticosteroid side effects and postoperative complications [1].
Ipamorelin has an intriguing mechanism of action that mimics some aspects of ghrelin (hunger hormone). It’s a selective agonist, which activates the ghrelin receptor pathway [2]. This interaction activates GH release from the pituitary gland, essentially initiating anabolic processes, including:
In rodents, ipamorelin increases appetite, hunger, and caloric intake, suggesting that it may be helpful in patients with cachexia or other conditions where weight gain is beneficial [3]. However, in humans, its effect on appetite appears to vary between individuals.
Ipamorelin-induced GH may act on muscles through insulin-like growth factor-1 (IGF-1) to increase muscle protein synthesis, inhibit protein degradation, stimulate satellite cell activity, and counteract myostatin signals [4].
In rats treated with glucocorticoid (GC), ipamorelin significantly increased maximum muscle tension and the rate of periosteal bone formation by fourfold [5].
These findings suggest that ipamorelin may mitigate the decline in muscle strength and bone formation typically observed in GC-treated rats.
In young rats, chronic administration of ipamorelin does not lead to desensitization of the GH response, helping to increase body weight.
However, chronic administration of ipamorelin on pituitary cell culture did lead to a dampened GH response over time, suggesting a desensitization response [6].
GH is essential for linear body growth during childhood, bone remodeling throughout life, and bone preservation in aging adults. GH and its downstream effector IGF-1 are central to skeletal growth and homeostasis. They activate osteoblasts and increase calcium storage and bone collagen.
In adult rats, 12 weeks of continuously administered ipamorelin significantly increased body weight, bone mineral content, and femur and vertebra L6 bone volume [6].
Another rat study found that ipamorelin increased linear growth rate and body weight in a dose-dependent manner. However, the ipamorelin treatment did not alter levels of IGF-1, IGFBPs, or serum markers of bone formation or resorption [7].
The effect of ipamorelin on weight has been paradoxical. Although GH is a crucial hormone for weight loss, most rodent studies found that ipamorelin assists with weight and body fat gain.
Ipamorelin has been shown to exert effects beyond muscle mass regulation. Experimental studies demonstrated that it significantly increased insulin secretion (p < 0.04) from the pancreas in both normal and diabetic rats.
These findings suggest that ipamorelin may influence glucose metabolism and insulin-dependent anabolic processes [8].
Ipamorelin demonstrated gastrointestinal effects that are mediated through activating ghrelin receptors. In a rodent model of postoperative ileus, a painful bowel paralysis after surgery, ipamorelin was shown to accelerate gastric emptying by enhancing gastric contractility [9].
A clinical trial on 114 patients who had undergone bowel resection surgery compared twice-daily ipamorelin administration with placebo to assess its effects on shortening the time to the first solid meal.
Although there was no statistically significant difference between ipamorelin and the placebo, no safety concerns were observed [10].
In a Phase 2 placebo-controlled trial, ipamorelin had lower but nonsignificant differences in incidents of side effects than placebo (87.5% in the ipamorelin group vs. 94.8% in the placebo group) [10].
Adverse effects observed in this trial included headache, gastrointestinal symptoms, and injection site reactions. The study did not report severe side effects specific to ipamorelin. The one report of risk for immunogenicity was linked to a production-related impurity in an IV administration [11].
Research Use Only. All findings described above are derived from preclinical studies (animal models and in vitro experiments). Ipamorelin is not approved by the FDA for any diagnostic or therapeutic use in humans. Genesis Peptides makes no claims regarding human clinical efficacy. This product is sold exclusively for laboratory research.
Every lot undergoes six independent assays before release. Results are published in the lot-specific Certificate of Analysis.
Ipamorelin is a growth hormone secretagogue (GHS) from the peptidomimetic GHS family. In animal research, ipamorelin is described as a peripherally restricted ghrelin mimetic. The authors of that animal study suggested it may offer a novel approach for treating acute visceral and somatic pain. In a separate study, ipamorelin was one of the peptidomimetic GHS families from which the authors derived 4-fluorobenzoylated compounds for PET imaging of the ghrelin receptor.
In animal studies, ipamorelin is described as a peripherally restricted ghrelin mimetic and a selective ghrelin receptor agonist. In rats, ipamorelin was given intravenously to study visceral and somatic nociception. In animals, the anti-nociceptive effects of ipamorelin and HM01 were blocked by the ghrelin receptor antagonist H0900, indicating a ghrelin receptor-mediated mechanism. In the animal study, the authors suggest that this peripherally restricted ghrelin mimetic may offer a novel approach for treating acute visceral and somatic pain.
The provided facts do not mention FDA approval for ipamorelin. A review describes ipamorelin, a growth hormone axis secretagogue, as investigational, with uncertain safety profiles, product quality concerns, and widespread antidoping restrictions. The same review's conclusion calls peptides such as ipamorelin experimental substances with poorly defined long-term risks. Growth hormone releasing peptides, the class ipamorelin belongs to, are listed on the World Anti-Doping Agency Prohibited List.
A review describes Ipamorelin, a growth hormone axis secretagogue, as investigational, with an uncertain safety profile and product quality concerns. The same review concludes that peptides such as Ipamorelin remain experimental substances with poorly defined long-term risks, and that their use should be considered high-risk until longitudinal data are available. The review also notes that the largely unregulated supply chain for peptides such as Ipamorelin means products are often mislabeled or contaminated.
In a fish study, ipamorelin (IPA) at 5 or 30 µg significantly elevated serum luteinizing hormone (LH) and 11-ketotestosterone (11-KT) compared with controls. The available findings concern 11-ketotestosterone, so they do not directly show a rise in testosterone. Fish treated with 30 µg of IPA also showed a significant elevation in androgen receptor protein expression.
In ferrets, ipamorelin was given intraperitoneally at 1-3 mg/kg 30 s before cisplatin (5 mg/kg, i.p.), with subsequent doses every 24 h, and behaviour was recorded for up to 72 h. In these ferret experiments, intraperitoneally administered ipamorelin had no effect on cisplatin-induced acute or delayed emesis. Ipamorelin inhibited cisplatin-induced weight loss on the last day of the delayed phase (48-72 h) by approximately 24 % in ferrets. The authors concluded that intraperitoneally administered ipamorelin had beneficial effects in alleviating cisplatin-induced weight loss during the delayed phase in ferrets.
In rats with acetic acid-induced visceral hypersensitivity, ipamorelin significantly attenuated colonic hypersensitivity and somatic allodynia compared with vehicle controls. The anti-nociceptive effects of ipamorelin were blocked by the ghrelin receptor antagonist H0900, which indicates a ghrelin receptor-mediated mechanism in these rats. The authors describe ipamorelin as a peripherally restricted ghrelin mimetic and suggest it may offer a novel approach for treating acute visceral and somatic pain.
In a study in the tilapia Oreochromis mossambicus, Ipamorelin acetate (IPA), a ghrelin agonist, was given at 5 or 30 µg for 21 days. Both doses were reported to cause a significant, dose-dependent rise in food intake, along with significant increases in primary spermatocytes, secondary spermatocytes, and early spermatids compared with controls. Fish given 30 µg of IPA also showed a significant rise in late spermatids and in the areas of the lobule and lumen compared with the control group. The percentage of gonadotropin-releasing hormone (GnRH)-immunoreactive fibres in the hypothalamus and anterior pituitary gland did not differ significantly between groups.
The paper describes a method that detects Ipamorelin in urine by direct urine injection into a liquid chromatograph, followed by ion-mobility time-of-flight mass spectrometry. The authors describe this method as a facile, specific and sensitive assay for the peptidic compounds it covers, including Ipamorelin. In a human clinical trial, Ipamorelin (1-4) free acid was detected in urine samples after complete withdrawal of the parent substances. In human urine after nasal administration, Ipamorelin was metabolized intensively and excreted as a set of parent compounds with metabolites.
Gly-Ipamorelin is ipamorelin extended by an N-terminal glycine residue. Gly-Ipamorelin was identified as one of three analogues of growth hormone releasing peptides (GHRPs) found in black market products. The structure of Gly-Ipamorelin was characterised by high resolution (tandem) mass spectrometry, and its identity was additionally confirmed by custom synthesis.
FOR RESEARCH USE ONLY — Products are sold exclusively for in vitro and preclinical laboratory research. Not for human consumption or administration. Not intended for diagnostic or therapeutic use. These statements have not been evaluated by the FDA.