This is a working overview of pentapeptide, written for readers who want more than a one-paragraph summary but less than a textbook.
This page was last updated on 2025-07-22 and is reviewed periodically as new material appears.
Ipamorelin is a synthetic pentapeptide classified as a growth hormone secretagogue. Its sequence, Aib-His-D-2-Nal-D-Phe-Lys-NH2, combines three non-proteinogenic residues with a C-terminal amide. The N-terminal aminoisobutyric acid unit and the two aromatic D-amino acids distinguish it from peptides assembled only from standard L-amino acids. Its formula is C38H49N9O5, corresponding to an average mass near 711.9 Da. At neutral pH the molecule carries a net positive charge, a property that shapes its behaviour in chromatographic and electrophoretic systems.
The compound was developed at Novo Nordisk during the 1990s as part of a programme seeking secretagogues with improved selectivity. It was described in the peer-reviewed literature in 1998 alongside related pentapeptides from the same series. Investigators advanced it because it raised growth hormone output in animal models while leaving other pituitary hormones comparatively unaffected. The development code NNC 26-0161 appears in earlier reports, and ipamorelin later became the common designation in published work.
Ipamorelin 是一种合成五肽,在 20 世纪 90 年代被报道为生长激素促分泌剂。其结构基于胃饥饿素受体激动剂的设计思路,但并非天然激素。早期药理学研究显示,它可刺激垂体释放生长激素,而对应激激素轴的影响相对较小。该化合物常被用作研究生长激素调节通路的工具分子。
在机制层面,ipamorelin 与生长激素促分泌受体 1a 型结合,该受体也介导胃饥饿素的多种效应。受体激活后,细胞内信号促进生长激素从垂体前叶释放。由于对促肾上腺皮质激素和皮质醇的刺激较弱,它被视为选择性较高的促分泌剂。这种选择性在动物模型和少量人体研究中被观察到,但人体数据仍然有限。
| Property | Value | Notes |
|---|---|---|
| Molecular formula | C38H49N9O5 | Pentapeptide with C-terminal amide |
| Average mass | Approximately 711.9 Da | Value derived from the formula |
| Appearance | White to off-white powder | Typically supplied as a lyophilised solid |
| Solubility | Soluble in water and aqueous acetonitrile | Dissolution aided by acidic diluents |
| Common synonyms | Ipamorelin; NNC 26-0161 | Code name used in early reports |
Signal transduction begins when the peptide binds GHSR-1a on pituitary somatotrophs. The receptor couples to Gq/11 proteins, activating phospholipase C, which cleaves phosphatidylinositol bisphosphate into inositol trisphosphate and diacylglycerol. Inositol trisphosphate releases calcium from intracellular stores, and the resulting rise in cytosolic calcium drives growth hormone vesicle fusion. Concurrent Gs coupling and cyclic AMP elevation have also been reported, and the relative contribution of each arm to the overall secretory response is not fully settled.
Structural features distinguish the molecule from earlier secretagogues. An alpha-aminoisobutyric acid residue near the N-terminus and a D-naphthylalanine substitution increase receptor affinity, while C-terminal amidation improves resistance to exopeptidases. These modifications are associated with reduced stimulation of appetite and of the hypothalamic-pituitary-adrenal axis compared with hexarelin or growth hormone releasing peptide-6. Whether the same profile applies at every dose level studied is a matter of ongoing investigation rather than settled consensus.
Research quantities of ipamorelin are typically distributed as a white to off-white lyophilized powder. The solid dissolves readily in water and in aqueous buffers, and stock solutions are commonly prepared in sterile water or a mildly acidic diluent. Adsorption to plastic and glass surfaces can reduce the concentration of very dilute solutions, so containers and transfer steps deserve attention when accurate concentrations matter. Reconstituted material is generally used promptly rather than held for extended periods.
Storage recommendations for the dry solid center on low temperature and low moisture, most often -20 °C in a sealed, desiccated container protected from light. Solutions are less stable than the powder and are usually kept cold and used within a short window. Freeze-thaw cycling is a recognized source of loss, and aliquoting before freezing is a standard precaution. These practices derive from general peptide handling principles rather than from a single published stability trial, so exact shelf lives should be treated as approximate.
Analytical confirmation relies on reversed-phase high-performance liquid chromatography, often coupled to mass spectrometry for identity and purity assessment. Mass spectrometry distinguishes the intact molecule from truncation products and from oxidation or deamidation variants that share similar chromatographic retention. Immunoassays appear in some biological studies but can cross-react with related peptides, so they are weaker tools for identity work. Reported purity figures depend heavily on the gradient, detector, and integration method used, which complicates direct comparison between laboratories.
== Structure == ACTH receptors are the shortest of the melanocortin receptor family and are the smallest known G-coupled receptors. Both human and bovine ACTH receptors are synthesized as 297 residue long proteins with 81% sequence homology. There are currently no available protein X-ray crystallography structures for the ACTH receptor available in the Protein Data Bank; while the ACTH receptor and the β2 adrenergic receptor are relatively distantly-related with a sequence identity of approximately 26%, MC2R investigators such as David Fridmanis have assumed that the folded surfaces of both receptors that are responsible for binding Gαs should be very similar and use conserved motifs. The full length sequence of MC2R includes seven hydrophobic domains that are predicted as transmembrane segments. In the third intracellular loop of the receptor a protein kinase A and protein kinase c phosphorylation motifs have been detected. ACTH receptors also require the binding of melanocortin-2 receptor accessory protein-1 (MRAP1) without which ACTH receptors cannot bind ACTH. Without MRAP, the receptor is degraded in the endoplasmic reticulum, but with MRAP, the receptor is glycosylated and expressed on the cell plasma membrane.
=== Historical development === Milk is presently the most mature system to produce recombinant proteins from transgenic organisms. Blood, egg white, seminal plasma, and urine are other theoretically possible systems, but all have drawbacks. Blood, for instance, as of 2012 cannot store high levels of stable recombinant proteins, and biologically active proteins in blood may alter the health of the animals. Expression in the milk of a mammal, such as a cow, sheep, or goat, is a common application, as milk production is plentiful and purification from milk is relatively easy. Hamsters and rabbits have also been used in preliminary studies because of their faster breeding. One approach to this technology is the creation of a transgenic mammal that can produce the biopharmaceutical in its milk (or blood or urine). Once an animal is produced, typically using the pronuclear microinjection method, it becomes efficacious to use cloning technology to create additional offspring that carry the favorable modified genome. In February 2009 the US FDA granted marketing approval for the first drug to be produced in genetically modified livestock. The drug is called ATryn, which is antithrombin protein purified from the milk of genetically modified goats. Marketing permission was granted by the European Medicines Agency in August 2006.
Grain-based feeds such as corn and barley produce up to one third less methane gas in cattle than grass fed cattle. By impeding methane production, Asparagopsis increases the efficiency of ruminant digestion in livestock to improve productivity.
Sources: en.wikipedia.org
=== Blood === Drug-testing a blood sample measures whether or not a drug or a metabolite is in the body at a particular time. These types of tests are considered to be the most accurate way of telling if a person is intoxicated. Blood drug tests are not used very often because they need specialized equipment and medically trained administrators. Depending on how much marijuana was consumed, it can usually be detected in blood tests within six hours of consumption. After six hours has passed, the concentration of marijuana in the blood decreases significantly. It generally disappears completely within 30 days.
== Uses == Viral load monitoring is used by HIV-positive people to develop a plan for their personal treatment of HIV/AIDS. A count of the viral load is routine before the start of HIV treatment. If the treatment is not changed, then viral load is monitored with testing every 3–4 months to confirm a stable low viral load. Patients who are medically stable and who have low viral load for two years may get viral load counts every 6 months instead of 3. If a viral load count is not stable or sufficiently low, then that might be a reason to modify the HIV treatment. If HIV treatment is changed, then the viral load should be tested 2–8 weeks later.
Many pathways and signals lead to apoptosis, but these converge on a single mechanism that actually causes the death of the cell. After a cell receives stimulus, it undergoes organized degradation of cellular organelles by activated proteolytic caspases. In addition to the destruction of cellular organelles, mRNA is rapidly and globally degraded by a mechanism that is not yet fully characterized. mRNA decay is triggered very early in apoptosis. A cell undergoing apoptosis shows a series of characteristic morphological changes. Early alterations include:
In a normal thermal reactor, tin-121m has a very low fission product yield; thus, this isotope is not a significant contributor to nuclear waste. Fast fission or fission of some heavier actinides will produce 121mSn at higher yields. For example, its yield from U-235 is 0.0007% per thermal fission and 0.002% per fast fission.
Sources: en.wikipedia.org
It is a synthetic five-amino-acid peptide that acts as a growth hormone secretagogue. Three of its residues are non-standard amino acids, and the chain ends in an amide rather than a free acid. The molecule is small enough that it can be characterised by routine peptide analytical techniques.
It has not received marketing approval as a medicine in the United States or the European Union. Supplied material is generally described and handled as a research chemical. Regulatory treatment varies by jurisdiction, and some countries restrict growth hormone secretagogues under sports or medicines legislation.
Earlier secretagogues were associated with broader hormonal responses, including measurable changes in cortisol and prolactin. Reports on this peptide describe a narrower profile in which growth hormone release is the most prominent effect. The observation is influential because it shapes how the compound is compared with other members of the same receptor family.
不是。它属于人工合成的五肽,设计上模拟胃饥饿素受体的部分作用,但不存在于人体天然激素谱中。