If you have been reading about IGF-1 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 2026-07-11. Numbers and descriptions here follow the published literature rather than marketing material.
The native hormone is produced in the hypothalamus and acts on the anterior pituitary. Binding of GHRH to its receptor stimulates synthesis and release of growth hormone into circulation. Because the analogue retains the receptor-binding region of the parent sequence, it engages the same receptor and triggers the same downstream signaling. The result is increased growth hormone secretion from pituitary cells, which in turn influences hepatic production of insulin-like growth factor 1. This axis is the basis for the compound's measured biological effects.
Interest in this peptide developed because native GHRH has a short circulating lifetime. The N-terminal modification slows cleavage by dipeptidyl peptidase IV, an enzyme that removes the first two residues of many peptides and terminates their activity. Slower degradation means a longer window of receptor stimulation per administration. This design logic parallels other modified peptide hormones, where a small chemical change at a vulnerable site yields a more durable molecule without altering the core mechanism of action.
特沙莫瑞林是一种合成肽,其序列与人生长激素释放激素的 44 个氨基酸形式相关。它在 N 端带有反式-3-己烯酰基修饰,这一改动可减缓二肽基肽酶 IV 的降解。该化合物属于生长激素释放激素受体激动剂,可刺激垂体释放生长激素。研究文献通常将其归入合成肽类药物,而非小分子化合物。
监管记录显示,特沙莫瑞林于 2010 年在美国首次获得批准,用于人类免疫缺陷病毒感染相关的脂肪营养不良患者。批准依据来自降低内脏脂肪的临床试验,而非体重或瘦体重的普遍改善。后续出现了不同制剂版本,但其核心适应症保持一致。关于长期心血管结局和死亡率影响,现有证据仍不充分。
| Property | Value | Notes |
|---|---|---|
| Molecular formula | C221H366N72O67S | Reflects a 44-residue peptide with one N-terminal modification |
| Approximate molecular weight | 5136 Da | Sequence length and single acyl group determine the mass |
| Appearance | White to off-white lyophilized powder | Typical form of a purified synthetic peptide |
| Solubility class | Soluble in water and aqueous buffer | Peptide backbone favors aqueous dissolution |
| Common synonyms | GHRH(1-44) analogue; Egrifta | Descriptive name and approved brand name |
Tesamorelin is a synthetic peptide that belongs to the growth hormone-releasing hormone family and contains the same forty-four amino acid sequence as endogenous GHRH, extended at the amino terminus by a trans-3-hexenoyl group. That small fatty acid modification protects the peptide from rapid cleavage by dipeptidyl peptidase-4, the enzyme that shortens the half-life of native GHRH to only a few minutes. Chemically the compound is produced by solid-phase peptide synthesis, purified by chromatography, and supplied as a sterile lyophilized powder for reconstitution.
Regulatory approval in the United States came in 2010, when the Food and Drug Administration cleared the peptide for the reduction of excess abdominal fat in adults with HIV infection and associated lipodystrophy. The decision rested mainly on two randomized phase 3 trials that enrolled roughly eight hundred patients and ran for twenty-six weeks. Participants receiving active drug showed substantially greater declines in visceral adipose tissue than those receiving placebo, while total body weight changed comparatively little. A reformulated presentation was later approved, and the product has remained a niche therapy rather than a general weight-loss agent.
Tesamorelin occupies a narrow position among agents that act on the growth hormone axis. Unlike growth hormone itself, which is given as replacement, it stimulates the pituitary to release the hormone in pulses, so the downstream increase in insulin-like growth factor 1 depends on intact somatotroph function. Other peptides in the same family include shorter GHRH fragments and synthetic secretagogues with different stability profiles. Several points remain unresolved, including whether the reduction in visceral fat translates into fewer cardiovascular events, what happens to metabolic markers after long-term use, and how the drug compares with lifestyle or surgical approaches.
Tesamorelin is a synthetic peptide analog of growth hormone-releasing hormone, composed of 44 amino acids. It was designed to retain the biological activity of the native hormone while resisting rapid enzymatic degradation. The compound is classified as a growth hormone secretagogue and belongs to the broader family of hypothalamic releasing factors. In research and clinical settings, it is studied for its ability to stimulate pituitary growth hormone release. Its structure includes a modification at the N-terminus that contributes to an extended half-life relative to native growth hormone-releasing hormone.
Tesamorelin binds to growth hormone-releasing hormone receptors on the surface of pituitary somatotroph cells. This binding activates adenylate cyclase, raising intracellular cyclic AMP levels and triggering the release of growth hormone into circulation. The elevated growth hormone then stimulates hepatic production of insulin-like growth factor 1. Because the effect is mediated through the endogenous axis, secretion remains subject to feedback regulation. This distinguishes it from direct growth hormone administration, which bypasses pituitary control entirely.
Tesamorelin is a synthetic peptide of forty-four amino acids whose sequence reproduces human growth hormone-releasing hormone. Its distinguishing feature sits at the amino terminus, where a trans-3-hexenoyl group replaces the free amine. That acylation slows cleavage by dipeptidyl peptidase IV, an enzyme that otherwise removes the first two residues and inactivates the natural hormone quickly. The modified peptide therefore persists longer in circulation while keeping the same receptor target. It is handled as a lyophilized solid and dissolved shortly before use.
Signaling begins at the GHRH receptor, a class B G protein-coupled receptor displayed on somatotroph cells of the anterior pituitary. Receptor occupancy activates Gs proteins, which raise adenylyl cyclase activity and intracellular cyclic AMP, in turn driving protein kinase A dependent pathways. The downstream output is synthesis and pulsatile secretion of growth hormone into the bloodstream. Hepatic tissue and peripheral sites respond by increasing insulin-like growth factor 1 production. Somatostatin and IGF-1 itself supply negative feedback that caps the size and duration of each secretory burst.
After the expression of the gene product, it may be necessary to purify the expressed protein; however, separating the protein of interest from the great majority of proteins of the host cell can be a protracted process. To make this purification process easier, a purification tag may be added to the cloned gene. This tag could be histidine (His) tag, other marker peptides, or a fusion partners such as glutathione S-transferase or maltose-binding protein. Some of these fusion partners may also help to increase the solubility of some expressed proteins. Other fusion proteins such as green fluorescent protein may act as a reporter gene for the identification of successful cloned genes, or they may be used to study protein expression in cellular imaging.
=== High-resolution mass spectrometry (MS) and high-performance liquid chromatography (HPLC) === The most commonly applied methods are MS and HPLC, in which the glycan part is cleaved either enzymatically or chemically from the target and subjected to analysis. In case of glycolipids, they can be analyzed directly without separation of the lipid component. N-glycans from glycoproteins are analyzed routinely by high-performance-liquid-chromatography (reversed phase, normal phase and ion exchange HPLC) after tagging the reducing end of the sugars with a fluorescent compound (reductive labeling). A large variety of different labels were introduced in the recent years, where 2-aminobenzamide (AB), anthranilic acid (AA), 2-aminopyridin (PA), 2-aminoacridone (AMAC) and 3-(acetylamino)-6-aminoacridine (AA-Ac) are just a few of them. O-glycans are usually analysed without any tags, due to the chemical release conditions preventing them to be labeled. Fractionated glycans from high-performance liquid chromatography (HPLC) instruments can be further analyzed by MALDI-TOF-MS(MS) to get further information about structure and purity. Sometimes glycan pools are analyzed directly by mass spectrometry without prefractionation, although a discrimination between isobaric glycan structures is more challenging or even not always possible. Anyway, direct MALDI-TOF-MS analysis can lead to a fast and straightforward illustration of the glycan pool. In recent years, high performance liquid chromatography online coupled to mass spectrometry became very popular.
The chelate effect increases as the number of chelate rings increases. For example, the complex [Ni(dien)2)]2+ is more stable than the complex [Ni(en)3)]2+; both complexes are octahedral with six nitrogen atoms around the nickel ion, but dien (diethylenetriamine, 1,4,7-triazaheptane) is a tridentate ligand and en is bidentate. The number of chelate rings is one less than the number of donor atoms in the ligand. EDTA (ethylenediaminetetracetic acid) has six donor atoms so it forms very strong complexes with five chelate rings. Ligands such as DTPA, which have eight donor atoms are used to form complexes with large metal ions such as lanthanide or actinide ions which usually form 8- or 9-coordinate complexes. 5-membered and 6-membered chelate rings give the most stable complexes. 4-membered rings are subject to internal strain because of the small inter-bond angle is the ring. The chelate effect is also reduced with 7- and 8- membered rings, because the larger rings are less rigid, so less entropy is lost in forming them.
Sources: en.wikipedia.org
== Deaths == 1 January – Frank McGarvey, Scottish footballer (St Mirren, Celtic, national team) (b. 1956) 18 March – Robert Lindsay, 29th Earl of Crawford, Scottish peer, MP (1955–1974) and Minister of State for Defence (1970–1972) (b. 1927) 21 March Willie Bell, Scottish footballer (Leeds United, national team) and manager (Birmingham City) (b. 1937) John Smith, Baron Kirkhill, Scottish peer, Lord Provost of Aberdeen (1971–1975) and Minister of State for Scotland (1975–1978) (b. 1930) 1 April – Ken Buchanan, professional boxer who became undisputed world lightweight champion in 1971 (b. 1945) 8 April – Bob Heatlie, Scottish songwriter ("Japanese Boy", "Cry Just a Little Bit", "Merry Christmas Everyone") and record producer (b. 1946). 30 April – Elizabeth Scott, Duchess of Buccleuch, wife of Richard Scott, 10th Duke of Buccleuch (b. 1954) 10 May – Hugo Burge, internet entrepreneur and owner of Marchmont House (b. 1972) 15 June – Gordon McQueen, Scottish footballer (Leeds United, Manchester United, national team) and manager. (b. 1953) 21 June – Winnie Ewing, Scottish politician (MP (1967–1979), MEP (1979–1999), MSP (1999–2003), President of the Scottish National Party (1987–2005)) (b. 1929) 26 June Craig Brown, Scottish professional footballer and football manager. (b. 1940) David Ogilvy, 13th Earl of Airlie, Scottish peer and Lord Chamberlain (1984–1997) (b. 1926) 2 July – Greig Oliver, 58, rugby union player. 6 September – John Cairney, Scottish actor (A Night to Remember, Cleopatra, Jason and the Argonauts), author and painter. (b.
k¢ is the capacity factor of the solute KSW is the partition coefficient of the solute between the stationary phase and the water KMW is the partition coefficient of the solute between the micelles and the water f is the phase volume ratio (stationary phase volume/mobile phase volume) n is the molar volume of the surfactant CM is the concentration of the micelle in the mobile phase (total surfactant concentration - critical micelle concentration) A plot of 1/k¢ verses CM gives a straight line in which KSW can be calculated from the intercept and KMW can be obtained from the ratio of the slope to the intercept. Finally, KSM can be obtained from the ratio of the other two partition coefficients:
Sonography (ultrasound diagnostics) is a versatile and widely used imaging modality in medical diagnostics. Ultrasound is also used in therapy. However, it uses mechanical waves and no ionizing or non-ionizing radiation. Patient safety is ensured if the recommended limits for avoiding cavitation and overheating are observed, see also Safety Aspects of Sonography. Even devices that use alternating magnetic fields in the radiofrequency range, such as magnetic resonance imaging (MRI), do not use ionizing radiation. MRI was developed as an imaging technique in 1973 by Paul Christian Lauterbur (1929-2007) with significant contributions from Sir Peter Mansfield (1933-2017). Jewelry or piercings can become very hot; on the other hand, a high tensile force is exerted on the jewelry, which in the worst case can cause it to be torn out. To avoid pain and injury, jewelry containing ferromagnetic metals should be removed beforehand. Pacemakers, defibrillator systems, and large tattoos in the examination area that contain metallic color pigments may heat up or cause second-degree burns or malfunction of the implants.
Sources: en.wikipedia.org
It shares the 44-residue sequence of human GHRH but carries an added trans-3-hexenoyl group at its N-terminus. That addition does not occur in the natural hormone and serves mainly to resist enzymatic breakdown. The receptor target and signaling pathway remain the same.
It binds the growth hormone-releasing hormone receptor on anterior pituitary cells. Activation of that receptor promotes synthesis and release of growth hormone. The effect propagates through the growth hormone and insulin-like growth factor 1 axis.
Native GHRH is cleared quickly by peptidases, which limits how long it can stimulate its receptor. The added group hinders one of the primary cleavage enzymes. The practical consequence is a longer period of receptor activity per dose.
特沙莫瑞林是国际非专利名称,指一种经过 N 端修饰的生长激素释放激素类似物。它被归类为合成肽,序列与 GHRH(1-44) 密切相关。该名称不指代任何特定品牌或剂型。