Ipamorelin
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Features & Compatibility
Product Summary – Ipamorelin benefits – GHSR-1a Agonist
| Field | Details |
| Product Name | Ipamorelin Benefits |
| Category | Synthetic pentapeptide; selective growth hormone secretagogue (GHS) and ghrelin receptor agonist (GHS-R1a) |
| Length | 5 amino acids |
| Amino Acid Sequence | Aib-His-D-2-Nal-D-Phe-Lys-NH₂
(Aib = 2-aminoisobutyric acid; 2-Nal = 2-naphthylalanine) |
| Molecular Formula | C₃₈H₄₉N₉O₅ |
| Molecular Weight | ≈ 711.9 Da |
| Form & Purity | Lyophilised powder; ≥95% purity (HPLC, vendor spec). Supplied for research use; not an FDA-approved drug. |
| Storage | Store at −20 °C in a dry, dark environment. Reconstituted solution should be used promptly; avoid repeated freeze–thaw cycles. |
| Typical Research Dose (non-clinical) | Commonly studied in the 0.5–1.0 µg/kg range SC or IV in trials; not approved for medical use. |
| Key Mechanisms | – Selective agonist of ghrelin (GHS-R1a) receptors → stimulates pituitary release of growth hormone (GH)
– Minimal effect on cortisol or prolactin (greater selectivity vs. GHRP-6 / GHRP-2) – Enhances IGF-1 indirectly via GH stimulation – Promotes anabolic and fat-metabolism effects without broad endocrine disruption |
| Research / Preclinical Use Cases | – Investigated for GH deficiency and age-related decline in the GH/IGF-1 axis
– Potential for bone health, muscle repair, and fat metabolism – Preclinical models: improved bone turnover, gut motility, and neuroprotection |
| Common AEs / Safety Signals (from trials) | – Generally well tolerated in early-phase human studies
– Mild headache, flushing, or transient injection-site reactions – Unlike other GHRPs, minimal cortisol and prolactin stimulation |
| Contraindications / Warnings | – Not FDA/EMA approved; distributed for research use only
– Long-term safety unknown; theoretical concerns include tumor promotion (via chronic GH/IGF-1 elevation) |
| Regulatory / Compliance | – Not approved for clinical use; available only as a research chemical
– Any medical use is restricted to controlled trials/protocols |
Mechanism of Action | Ipamorelin benefits
Selective Agonist of Ghrelin Receptor
Ipamorelin Benefits targets the GHS-R1a receptors present in the hypothalamus and pituitary loci to act as a dose-dependent facilitation of GH secretory bursts. “Ipamorelin causes rapid, pulsatile GH secretion when administered systemically due to the receptor’s capacity for peptide recognition and biased signalling, involving constitutive activity and ligand-dependent engagement of G proteins and β-arrestin. [1]
Minimal Effect on Cortisol & Prolactin
Ipamorelin Benefits induces a selective release of GH with minimal to no stimulation of ACTH, cortisol, or prolactin, even at doses sufficient to elicit robust GH secretion. In contrast, clinical comparative studies show that earlier GHRPs such as GHRP-6 and GHRP-2 often trigger significant increases in ACTH, cortisol, and prolactin.
The selectivity of Ipamorelin Benefits is dose- and species-dependent due to its receptor engagement, tissue penetration, and off-target receptor interactions.
Insulin-like Growth Factor-1 (IGF-1) Production
Acute and repeated peptide-induced GH pulses cause the IGF-1 release from the liver. Although the single doses secrete the rapid GH peaks, measurable rises of IGF-1 in serum require sustained and repeated dosing. [3]
Anabolic & Fat-Metabolism Effects
In preclinical and limited clinical contexts, ipamorelin was found to cause increased markers of anabolism and attenuated glucocorticoid-induced catabolism in rodent bones. Ipamorelin also modulates the energy balance by increasing the appetite, promoting adipogenesis, and limiting the lipolysis through the ghrelin receptor activation. [4]
Net body composition effects of ipamorelin are context-dependent. In cachectic or GH-deficient states, anabolic and lean-mass benefits are predominant, while in GH-intact systems, enhanced adiposity and attenuated fat distribution are prevailing. [5]
Tolerability and Safety Considerations of Ipamorelin benefits
- Generally well tolerated in human and animal studies.
- The most common adverse events can be injection site irritation, mild headache, and transient flushing.
- Selective GH secretagogue → minimal effects on cortisol or prolactin compared to earlier GHRPs.
- Long-term safety is not fully established; data is mostly from short-term trials and research use.
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