If you have been reading about GHS-R1a and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.
Updated 2026-06-04. Numbers and descriptions here follow the published literature rather than marketing material.
从用途定位看，ipamorelin 目前主要以研究用肽的身份被讨论，未见主要药品监管机构将其批准为治疗药物。市售材料通常标注仅供研究使用，不得用于人体或诊断程序。文献中它常与生长激素促分泌素、GHS-R1a 激动剂、胃饥饿素拟似物等表述并列出现。既有研究的样本量普遍偏小，因此对其效应强度与一致性的描述应保持谨慎。
Ipamorelin 是一种合成五肽，序列为 Aib-His-D-2-Nal-D-Phe-Lys-NH2，分子式 C38H49N9O5，游离碱分子量约 711.85 g/mol。它属于生长激素促分泌素（GHS）家族，作用靶点是胃饥饿素受体 GHS-R1a。该化合物由诺和诺德的研究团队在二十世纪九十年代末报道，设计目标是提高对生长激素释放的选择性。C 端酰胺化与 N 端 Aib 残基是两个用于抵抗肽酶降解的结构特征。
在 GHS 家族中，早期肽类如 GHRP-6 与 GHRP-2 会同时促进生长激素、皮质醇与催乳素的释放，并明显增加食欲。Ipamorelin 在动物与早期人体研究中表现出对生长激素释放的相对选择性，对上述其他激素的影响较小。这种差异通常归因于受体结合模式与下游信号偏向的不同，而完整的分子解释仍有待补充。需要区分的是，选择性是研究观察中的相对程度，并非绝对界限。
At the cellular level, ipamorelin binds the growth hormone secretagogue receptor, also called the ghrelin receptor. Activation of this receptor on pituitary somatotroph cells triggers a signaling cascade that leads to release of growth hormone into circulation. Because release follows a pulsatile pattern, studies often report peak concentration and total area under the curve rather than a single time point. Selectivity for this receptor is the property most frequently discussed in comparative work.
Compared with older secretagogues such as hexarelin or GHRP-6, ipamorelin shows weaker stimulation of cortisol, prolactin, and appetite in the animal models used for early characterization. Whether that selectivity is preserved across longer human exposures remains an open question, because published clinical data are limited in size and duration. Reported effects on food intake are generally described as modest. The compound is therefore treated in the literature as a relatively selective research tool rather than a fully characterized therapeutic agent.
| Property | Value | Notes |
|---|---|---|
| 分子式 | C38H49N9O5 | 五肽，C 端酰胺化 |
| 分子量 | 约 711.85 g/mol | 游离碱形式 |
| 外观 | 白色至类白色冻干粉 | 研究用材料的常见形态 |
| 溶解性 | 溶于水及 DMSO 等极性溶剂 | 建议现配现用 |
| 储存温度 | -20 °C 或更低 | 干燥、避光、限制冻融次数 |
Research peptides such as ipamorelin are commonly supplied as lyophilized powder and characterized by analytical certificates. Reversed-phase high-performance liquid chromatography is used to estimate purity by ultraviolet absorbance, while mass spectrometry confirms molecular identity and detects sequence-related impurities. Counterion content, water content, and residual synthesis reagents can affect the reported mass balance. A certificate of analysis may list a purity percentage, but that number depends on the analytical method and the definition of impurity peaks. Independent verification is often recommended because research supply chains vary in quality control practices.
Storage recommendations for ipamorelin usually focus on temperature, moisture, and light. Lyophilized powder is typically held at or below minus twenty degrees Celsius in a desiccated container protected from light. Reconstituted solutions are often aliquoted and stored at minus eighty degrees Celsius to reduce repeated freeze-thaw cycles, which can promote aggregation or degradation. The optimal buffer and pH depend on the specific assay, and no single condition applies to every experimental context. Peptide stability should be assessed with time-point measurements rather than assumed from general handling rules.
Purity assessment for this peptide relies mainly on reversed-phase high-performance liquid chromatography. A C18 column with a water-acetonitrile gradient containing trifluoroacetic acid separates the target from truncated sequences and oxidation products. Detection near 214 nm exploits the amide backbone, while the aromatic side chains allow additional monitoring close to 280 nm. Reported purity values depend on the method, so a certificate of analysis carries weight only when gradient, column and integration parameters are given.
Mass spectrometry confirms identity and reveals structural deviations that chromatography alone can miss. Positive-mode electrospray ionisation generally yields multiply charged ions whose deconvoluted mass is checked against the theoretical value. Amino acid analysis, and enzymatic digestion with subsequent fragment mapping, provide independent confirmation of sequence and of the terminal amide. Analysts take care to separate the target from deletion sequences, which may differ by one residue and therefore by only a small mass increment.
The lyophilised solid is normally held at -20 °C or colder, shielded from light and moisture. Stability in that state is measured in years, although shelf life depends on residual water content and the container seal. Once dissolved, the peptide is more fragile: aqueous solutions are commonly kept at 2-8 °C and used within days to weeks, and repeated freeze-thaw cycling is avoided. Strongly acidic or basic conditions accelerate hydrolysis, and prolonged exposure to them can strip the terminal amide.
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A Hahn echo decay experiment can be used to measure the dephasing time, as shown in the animation. The size of the echo is recorded for different spacings of the two pulses. This reveals the decoherence that is not refocused by the 180° pulse. In simple cases, an exponential decay is measured which is described by the T2 time.
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Sources: en.wikipedia.org
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Inhibitors of OATP1B1 may increase circulating levels of elagolix, and elagolix is considered to be contraindicated in combination with strong OATP1B1 inhibitors. Elagolix is a substrate of P-glycoprotein, but the effect of inhibitors and inducers of P-glycoprotein on the pharmacokinetics of elagolix is unknown. Elagolix itself is an inhibitor of P-glycoprotein.
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Sources: en.wikipedia.org
== Occurrence == More than 100 naturally occurring nitriles were known as early as the 1990s, and several hundred have since been identified. These compounds occur in bacteria, fungi, plants, and arthropods and sponges. The biosynthesis of naturally occurring nitriles frequently begins with amino acids. Their N-hydroxylation followed by decarboxylation (cleavage of the carboxylic acid group as carbon dioxide) yields oximes, which serve as the direct precursors of nitriles.
=== Non-volatile chlorogenic acids === Chlorogenic acids belong to a group of compounds known as phenolic acids. The content of chlorogenic acids in dried arabica green coffee beans is 65 mg/g, and in robusta 140 mg/g, depending on the time of harvest. At roasting temperature, more than 70% of chlorogenic acids are destroyed. Chlorogenic acids are homologous compounds comprising caffeic acid, ferulic acid and 3,4-dimethoxycinnamic acid, which are connected by an ester bond to the hydroxyl groups of quinic acid. Chlorogenic acids have a bitter taste in low concentrations such as 50 mg/L water. At higher concentrations of 1 g/L water, they have a sour taste. Chlorogenic acids increase the solubility of caffeine, and are important modulators of taste.
== Background/History == Izon Science Limited is a company incorporated as Australo Ltd. on January 10, 2005, by four New Zealand-based scientists. In 2007, Hans van der Voorn became CEO, and on November 17, 2008, the company was renamed Izon Science Limited. Initially focused on developing tunable resistive pulse sensing instruments for nanoparticle characterization, the company later expanded into developing tools for isolating exosomes and other extracellular vesicles from biological fluids. Presently, Izon Science develops and manufactures tools for nanoparticle characterization and separation, catering to academic researchers and diagnostics companies working with extracellular vesicles, as well as those involved in nanomedicine, viruses, and virus-like particles. The Exoid is one of Izon's latest tunable resistive pulse sensing instruments, succeeding the qViro-X, qMicro, and qNano. In June 2021, Izon Science relocated its headquarters from Burnside (Christchurch) to a larger facility on Show Place, Addington (Christchurch). The company currently employs approximately 70 individuals. Izon has received investment funds from Bolton Equities, a privately funded investor group based in New Zealand. Research partnerships include the University Medical Center Utrecht and the VU University Medical Center in the Netherlands, the Mayo Clinic, the National Institutes of Health, and Massachusetts General Hospital.
Sources: en.wikipedia.org
两者都是 GHS-R1a 激动剂，但 ipamorelin 在研究中显示出更高的生长激素释放选择性。早期资料显示它对皮质醇、催乳素与食欲的刺激弱于 GHRP-6。这些差异是相对程度，而非绝对区分。
公开资料中它主要以研究用肽的形式出现，未获主要监管机构批准用于治疗。可得材料通常标注仅供研究使用。任何临床用途的宣称都缺少监管依据。
序列中的 Aib 与 D-2-Nal 等非天然残基可提高对肽酶的抵抗能力，并影响受体结合的构象。这类修饰在合成肽设计中较为常见。它们也使常规氨基酸分析需要额外步骤才能确认序列。
Aib 即 α-氨基异丁酸，是一种非蛋白质源氨基酸，其侧链为两个甲基。它在肽链中倾向于诱导螺旋构象并限制骨架的柔性。这种刚性被认为有助于抵抗蛋白酶切割。