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Selective Ghrelin Receptor Agonist
Ipamorelin
5MG per vial
Ipamorelin is a synthetic pentapeptide growth hormone secretagogue, Aib-His-D-2-Nal-D-Phe-Lys-NH2, derived from GHRP-1, in which three of the five positions are non-proteinogenic — α-aminoisobutyric acid, D-2-naphthylalanine and D-phenylalanine — and the C-terminus is amidated, a design that leaves it poorly recognised by peptidases. It is an agonist at growth hormone secretagogue receptor type 1a (GHS-R1a), the ghrelin receptor, a Gq/11-coupled GPCR expressed on anterior pituitary somatotrophs and in hypothalamic and enteric neurons, where occupancy drives phospholipase C activation, IP3 generation and intracellular calcium release. It shares that receptor with ghrelin while bearing no structural resemblance to it, and it lacks ghrelin's octanoylated serine entirely.
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Research use only. Supplied for in vitro laboratory research. Not a drug, supplement, cosmetic or medical device, not approved by the TGA, and not for administration to humans or animals. See our research use conditions.
Compound signature
From confirmed structure
711.9g/mol
Molar mass
52atoms
Heavy atoms
Atomic composition
C38H49N9O5
- C38
- H49
- N9
- O5
Characterised targets
- GHS-R1a (ghrelin receptor)
Sequence
Aib-His-D-2-Nal-D-Phe-Lys-NH2
Research applications
Ipamorelin was introduced by Raun and colleagues at Novo Nordisk in 1998, and it is known for a selectivity result rather than a potency one: in conscious swine, GHRP-2 and GHRP-6 raised plasma ACTH and cortisol whereas ipamorelin did not release either at levels significantly different from those following GHRH stimulation, a separation the authors reported held at doses more than 200-fold above its ED50 for GH release. In the same swine work none of the secretagogues tested altered plasma FSH, LH, prolactin or TSH, and the authors characterised ipamorelin as the first GHRP-receptor agonist with a selectivity for GH release comparable to that of GHRH — which is why it is frequently chosen as the comparator when investigators want to interrogate GHS-R1a in isolation from the corticotroph axis. It has since been used in rat pituitary cell preparations to characterise GHS-R1a coupling and in rodent studies examining GH-axis contributions to bone and body-composition endpoints, while GHS-R1a agonism more broadly has been investigated in gastrointestinal motility models.
Formulation and handling
A small chemically synthesised peptide supplied lyophilised; the C-terminal amide together with the D-amino acid and Aib substitutions make it comparatively robust in solution relative to all-L peptides. The lysine side chain gives it basic character and it dissolves readily in water or bacteriostatic diluent without acid or organic co-solvent.
Intended use
Ipamorelin is supplied exclusively for in vitro and non-clinical scientific research. It is not approved for human or animal therapeutic, diagnostic or medicinal use. All handling and experimentation must be carried out by trained personnel in an appropriately controlled laboratory.
Specification
- Presentation
- Vial
- Labelled strength
- 5MG
- Molecular formula
- C38H49N9O5
- Molar mass
- 711.9 g/mol
- CAS number
- 170851-70-4
- Molecular targets
- GHS-R1a (ghrelin receptor)
- Appearance
- Lyophilised powder
- Storage
- 2–8 °C sealed, −20 °C long term
Values describe the compound as supplied. Analytical figures for the material in your vial are on that lot’s certificate, not here.
Certificates of analysis
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