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�Œ–学性质与分析表征 — Research Overview

By Editorial Desk · published 2025-11-08 · last reviewed 2025-12-15 · Info

Everything below concerns peptidase cleavage. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Updated 2025-12-15. Numbers and descriptions here follow the published literature rather than marketing material.

化学性质与分析表征

从分子层面看,Semax 是线性七肽,没有二硫键、糖基或脂链修饰,N 端为游离氨基,C 端为游离羧基。分子含组氨酸与谷氨酸侧链,因此在水和甲醇等极性溶剂中溶解良好,在非极性溶剂中溶解有限。计算分子量约为 814 Da,与其质子化离子的质荷比吻合,可用于质谱确认。

稳定性主要由水解与氧化两条路径支配。肽键在中性或弱酸性条件下相对稳定,遇到强碱或长时间高温则明显断裂;甲硫氨酸侧链容易被氧化成亚砜,使主峰前移并拉低实际含量。金属离子、光照和反复冻融会进一步促进降解或聚集。冻干粉在低温避光条件下可存放较长时间,配制后的水溶液通常需要冷藏并尽快用完。

纯度评估以反相高效液相色谱为主,通过主峰面积百分比给出粗略结果,再配合电喷雾质谱核对分子量。氨基酸分析可验证组成比例,手性色谱或毛细管电泳用于检查残基构型。常见杂质包括缺失序列的短肽、氧化产物与二聚体。由于多数市售品不附带完整检验报告,独立第三方检测常被用来核实标称值。

Semax Background and Molecular Structure

The C-terminal Pro-Gly-Pro extension is not incidental. Proline-rich tails are known to resist several common peptidases, and the published literature attributes the longer half-life of Semax, relative to unmodified ACTH fragments, to this feature. The modification also removes the melanocyte-stimulating and corticosteroidogenic activity that characterizes longer ACTH-derived sequences. Because the molecule is small and hydrophilic, it is typically formulated as an aqueous solution for intranasal or parenteral delivery. Acetylation or amidation at the termini appears in closely related research peptides and shifts the mass by a fixed increment.

Reported pharmacological work centers on neurotrophic signaling, including changes in BDNF and NGF expression in hippocampal tissue in animal models. Human data come largely from studies conducted in Russia, and how well those results generalize to other populations remains an open question. Regulatory status differs sharply by jurisdiction: Semax is a registered prescription medicine in Russia, while it holds no approved marketing status in the United States or the European Union. Outside such jurisdictions it is generally handled as a research chemical, which affects both documentation and quality expectations.

Semax is a synthetic heptapeptide whose sequence is Met-Glu-His-Phe-Pro-Gly-Pro. It was developed as a fragment analog of adrenocorticotropic hormone, modeled specifically on the ACTH(4-10) region. The first four residues reproduce that fragment, while a Pro-Gly-Pro tripeptide is appended at the C-terminus. Work on the compound originated in Russia, where it entered clinical use as an intranasal preparation. Its sequence places it among short regulatory peptides studied for effects on the central nervous system rather than on the adrenal axis.

Semax at a glance

PropertyValueNotes
分子式C37H51N9O10S游离碱形式
等电点约 6.5估算值,随缓冲体系变化
主要降解途径水解与氧化侧链氧化最为常见
溶液储存2 至 8 摄氏度避光避免反复冻融
常规分析手段反相色谱与质谱联用氨基酸分析辅助核对

Mechanism and Research Context

The mechanisms attributed to semax are inferred from animal and cell studies rather than traced to one confirmed target. The most frequently cited pathway involves increased expression of brain-derived neurotrophic factor and nerve growth factor in hippocampal and cortical tissue. Some work points to engagement of melanocortin receptors, particularly MC4, which the parent ACTH fragment can activate. Effects on dopaminergic and serotonergic signalling have also been reported. No single account explains all observed results, and the relative weight of each pathway remains unsettled.

Published studies examine a fairly narrow set of endpoints. Rodent experiments commonly measure maze learning, infarct volume after induced ischemia, and tissue levels of neurotrophic factors. Clinical reports from Russian centres describe attention, memory and recovery scores in patients after stroke or transient ischemic attack. Most of those human studies are small and few have been repeated by independent groups. Outcome measures differ between studies, which limits direct comparison.

Circulation time for the peptide is short because peptidases cleave it readily. The Pro-Gly-Pro tail is thought to slow breakdown compared with the bare ACTH fragment, but the gain appears modest. Absorption after intranasal dosing is limited, and only a fraction of a dose is expected to reach the central nervous system. Laboratory concentrations therefore sit well above levels achieved systemically, a gap that complicates translation from bench findings to clinical claims.

Related pages on this site

Semax Background and Chemistry

Semax is a synthetic heptapeptide with the sequence Met-Glu-His-Phe-Pro-Gly-Pro. It corresponds to the ACTH(4-7) fragment extended at the C-terminus by a Pro-Gly-Pro tripeptide, an addition intended to slow enzymatic breakdown. The molecular formula is C37H51N9O10S and the molecular mass is approximately 814 daltons. In the literature it is often described as an ACTH(4-10) analog, although that label reflects a naming convention as much as a precise structural relationship. The compound was developed in Russia and remains most closely associated with that research tradition.

Laboratory descriptions of the material are consistent across suppliers. It appears as a white to off-white lyophilized powder that dissolves readily in water and in polar organic solvents such as dimethyl sulfoxide. Aqueous solutions are clear and colorless at low concentrations. Because the peptide contains methionine, oxidation at the sulfur atom is a recognized degradation pathway, and handling notes usually call for protected, desiccated storage. Reported purity for research-grade lots is generally above 95 percent as measured by reversed-phase high-performance liquid chromatography.

The compound is registered in Russia as a pharmaceutical product, most commonly formulated as a nasal solution, and has been used in that setting since the 1990s. Outside that jurisdiction it is generally handled as a research chemical rather than an approved medicine. Regulatory status therefore differs sharply between countries, and material sold internationally may not correspond to the Russian pharmaceutical formulation. Documentation with commercial samples is typically limited to a certificate of analysis covering purity and identity, not clinical status or local legal classification.

Further detail

Other adverse events included spinal epidural hematoma (in the cervical, thoracic and lumbar spine), chylothorax, injuries of abdominal organs and tissues, injuries in the neck region, injuries to the eyes, including orbital hemorrhage, traumatic cataract, injury of the oculomotor nerve and retinal puncture, hemorrhage to the cheeks and the hypoglottis, peripheral motor-nerve injuries and subsequent motor dysfunction, local allergic reactions to metal needles, stroke, and cerebral hemorrhage after acupuncture. A causal link between acupuncture and the adverse events cardiac arrest, pyknolepsy, shock, fever, cough, thirst, aphonia, leg numbness, and sexual dysfunction remains uncertain. The same review concluded that acupuncture can be considered inherently safe when practiced by properly trained practitioners, but the review also stated there is a need to find effective strategies to minimize the health risks. Between 1999 and 2010, the Korean-language literature contained reports of 1104 adverse events. Between the 1980s and 2002, the Japanese-language literature contained reports of 150 adverse events.

=== Miscellaneous === Urine drug screen — screen for usage of recreational drugs Urine cytology — cytopathological examination of cells in the urine, used to screen for cancer Urine protein electrophoresis — classification and measurement of different proteins in the urine; used to help diagnose monoclonal gammopathies Urine organic acids, urine amino acids — used to test for some inborn errors of metabolism

== Ice hockey scandals == Operation Slapshot (2006) – investigation into a gambling ring allegedly operated by National Hockey League assistant coach Rick Tocchet. Chicago Blackhawks Sexual Assault Scandal (2010) - Kyle Beach, former NHL player, was sexually assaulted by then assistant coach Brad Aldrich during the 2009-10 Chicago Blackhawks season. Even though the incident was known by the front office, no actions were taken to provide Beach with a proper care and recovery. The scandal was under the radar for almost a decade when Beach decided to formally expose the incident.

=== Discontinued === Acebilustat (CTX-4430; EP-501) – leukotriene A4 (LTA4H) hydrolase inhibitor Afamelanotide (CUV-1647; EPT-1647; Melanotan I; Melanotan; Prenumbra; Scenesse) – melanocortin receptor agonist BBI-3000 – retinoid X receptor agonist BMX-010 (MnTE-2-PyP) – reactive oxygen species (ROS) scavenger and radioprotector Botulinum toxin A liquid (AI-09) – acetylcholine release inhibitor and neuromuscular blocking agent Botulinum toxin A topical (ANT-1207) – acetylcholine release inhibitor and neuromuscular blocking agent Cioteronel (CPC-10997; Cyoctol; X-Andron) – antiandrogen (androgen receptor antagonist) Diroleuton (DGLA; DHLA; DS-107; RO-12-1989) – omega-6 fatty acid and anti-inflammatory DMVT-503 (RVT-503) – undefined mechanism of action DX-0385 – retinoic acid metabolism modulator Encapsulated tretinoin cream – retinoid (retinoic acid receptor agonist) Epristeride (Aipuliete; ONO-9302; SKF-105657) – 5α-reductase inhibitor Falecalcitriol (DSC-103; F6VD3; flocalcitriol; Fulstan; hexafluorocalcitriol; hexafluorovitamin D3; Hornel; SM-8000; ST-630) – vitamin D/calcitriol analogue Gevokizumab (S-78989; VPM-087; XMA-005.2) – monoclonal antibody against interleukin-1β Hypochlorous acid (PR-013; PR-022) – disinfectant and other actions Imsidolimab (ANB-019) – monoclonal antibody against the interleukin-36 receptor Incyclinide (chemically modified tetracycline 3; CMT-3; COL-3; Metastat) – chemically modified tetracycline and matrix metalloproteinase inhibitor (no antibiotic activity) Ingenol disoxate (LEO-43204) – undefined mechanism of action JNJ-10229570 – melanocortin MC5 receptor antagonist MDI-301 – undefined mechanism of action MK-434 (MK-0434) – 5α-reductase inhibitor MTCH-24 (Zilex; Zorex) – undefined mechanism of action PF-06423264 – acetyl-CoA carboxylase inhibitor PSK-3841 (HMR-3841; RU-58841) – antiandrogen (androgen receptor antagonist) Research programme: acne therapeutics - Praxis – undefined mechanism of action Research programme: tetracycline derivatives - Paratek Pharmaceuticals (P-004292) – tetracycline derivatives Rose bengal sodium (PH-10; Provecta; PV-10; rose bengal; Xantryl) – immunomodulator and other actions Santalum album ointment (albuterpenoid; East Indian sandalwood oil) – undefined mechanism of action Talarozole (R115866; Rambazole) – retinoic acid metabolism modulator Thykamine (PCT-233; PUR-0110) – undefined mechanism of action (anti-inflammatory) Valproic acid topical (Avugane; Baceca; G2M-777) – histone deacetylase inhibitor and other actions XEN-801 (XEN801) – stearoyl-CoA desaturase inhibitor XOMA-629 (XMP-629) – endotoxin inhibitor Zileuton (A-64077; Abbott-64077; ABT-077; CRTX-073; CTI-02; Zyflo) – 5-lipoxygenase inhibitor

Sources: en.wikipedia.org

Background from the literature

In number theory and combinatorics, the rank of an integer partition is a certain integer associated with the partition. Dyson introduced the concept in a paper published in the journal Eureka. It was presented in the context of a study of certain congruence properties of the partition function discovered by the mathematician Srinivasa Ramanujan.

=== Inkjet printing === A promising physical technique is inkjet printing, which allows for conductive materials to be deposited in a precise and reproducible fashion onto paper. As a proof-of-concept, Ko et al. developed a paper-based electrical chip using a home office printer, an ink made of carbon nanotubes, and magazine paper. Similarly, silver nanoparticles were printed into microfluidic channels to sense changes in the permittivity of fluids, revealing information about concentration and mixing ratios. Research groups have found, however, that these nanoparticle containing inks can self-aggregate on the paper due to uneven drying, which leads to non-uniform coverage and non-linear responses. A promising physical technique is inkjet printing, which allows for conductive materials to be deposited in a precise and reproducible fashion onto paper. In this regards, the controlled growth of nanoparticles can help to improve conductivity and sensing performances. As the seeds clusters grow and interconnect inside of the paper fibers, there properties and structure of the final material can be controlled through the process and chemical conditions. A typical growth process conditions consist dissolved metal ions in a reductive chemical environment. Once the nanoparticles have grown, they can be functionalized with recognition biomolecules to increase the specificity and sensitivity of the microfluidic devices. Inkjet printing is compatible with a wide variety of materials.

== Applications == Ammonium sulfate is the traditional kosmotropic salt for the salting out of protein from an aqueous solution. Kosmotropes are used to induce protein aggregation in pharmaceutical preparation and at various stages of protein extraction and purification.

Sources: en.wikipedia.org

Frequently asked questions

用什么方法确认分子量?

电喷雾或基质辅助激光解吸电离质谱是常用手段,测得的质子化离子质荷比可换算为分子量。结果与理论值落在合理误差内,才支持结构一致的判断。

为什么甲硫氨酸容易出问题?

甲硫氨酸侧链含硫醚,在氧气、光照或金属离子存在时容易被氧化。氧化产物极性略增,常在色谱图上表现为主峰之前的肩峰或前伸峰。

溶液配制后如何保存?

通常建议冷藏避光,并在较短时间内使用。不存在适用于所有配方的统一期限,具体取决于浓度、缓冲体系与容器材质。

What is the amino acid sequence of Semax?

The sequence is Met-Glu-His-Phe-Pro-Gly-Pro, a seven-residue peptide. The first four residues correspond to the ACTH(4-10) fragment, and Pro-Gly-Pro is added at the C-terminus. N-acetylated versions also appear in the literature and differ in mass.

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