Background:
Focal segmental glomerulosclerosis (FSGS) is a disease that causes scarring in parts of the kidneys that filter waste. This can lead to protein loss in the urine, which can worsen kidney function. The kidneys may fail over time, and dialysis or a kidney transplant may be needed. Other treatments for this disease do not always work and often have adverse effects. Better treatments for FSGS are needed.
Objective:
To test a study drug (ManNAc) in people with FSGS.
Eligibility:
People aged 18 years and older with FSGS.
Design:
Participants will have 5 to 6 clinic visits over 14 weeks. Two of the visits will require overnight stays for 2 or 3 nights.
ManNAc is a white powder that comes in a sachet. It is dissolved in water and taken twice a day by mouth. Participants will take their first dose at the clinic. They will learn how to store ManNAc and prepare each dose. They will record their doses in a diary. They will also write down any adverse effects or troubles they have using the drug at home.
During clinic visits, participants will have physical exams with blood and urine tests. They will complete questionnaires about their health, sleep habits, and fatigue symptoms.
During overnight visits, participants will also have 24-hour urine collection.
A study team member will call participants 1 week after the first dose to check on their health. Follow-up phone calls will then be every 2 weeks after each clinic visit.
Participants may meet with a dietitian to discuss nutrition while taking the ManNAc.
Participants may choose to have genetic tests.

开始日期2026-04-21

申办/合作机构

National Human Genome Research Institute

ACTRN12623000609651

/ RecruitingN/AIIT

An open-label, randomised, three-arm crossover study to examine the comparative pharmacokinetics of ManNAc administered as an oral solution and as two novel oral tablet formulations in healthy adult males

开始日期2023-07-13

申办/合作机构

University of South Australia

ACTRN12622000394741

/ CompletedN/AIIT

An open-label, randomised, two-arm crossover study to determine the absolute oral bioavailability of ManNAc in healthy adult males

开始日期2022-11-17

申办/合作机构

University of South Australia

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100 项与 N-acetyl-D-mannosamine 相关的专利（医药）

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项与 N-acetyl-D-mannosamine 相关的文献（医药）

2026-03-01·Kidney International Reports

Phase 1 Study of Oral N-Acetylmannosamine in Primary Podocytopathies

Article

作者: Ganguli, Anirban ; Rossignol, Francis ; Bolaños, Jonathan ; Figg, William D ; Leoyklang, Petcharat ; Kopp, Jeffrey B ; Huizing, Marjan ; Gahl, William A ; Zeng, Yi ; Malicdan, May Christine V ; Wilkins, Kenneth J

Introduction:

Terminal sialic acid (SA) residues on glycoconjugates are essential for maintaining the glomerular filtration barrier's charge selectivity and podocyte ultrastructure. SA depletion affects key podocyte glycoproteins, contributing to podocytopathy and proteinuria. Glomerular hyposialylation is commonly seen in experimental podocytopathies and human renal biopsies. In nephrotic mouse models, oral administration of the metabolic SA precursor, N-acetylmannosamine (ManNAc) restored sialylation and reduced proteinuria, suggesting therapeutic potential.

Methods:

In this single-center, single-arm, ascending dose phase 1 trial, we evaluated safety and pharmacokinetics (PKs) of oral ManNAc in primary podocytopathies (ClinicalTrials.gov: NCT02639260). Eligible participants had urine protein-to-creatinine ratio (UPCR) > 1 g/g and estimated glomerular filtration rates (eGFR) > 15 ml/min per 1.73 m². Six subjects received a single 3g ManNAc dose followed by 5 days of 1.5 g twice-daily (BID) dosing. One subject received a single 6 g dose.

Results:

All enrolled participants had primary podocytopathy, with eGFR of 25 to 89 ml/min per 1.73 m² and UPCR of 1.1 to 9.21 g/g. ManNAc was well-tolerated without serious adverse events (AEs). Maximum plasma ManNAc concentration was reached within 2 to 4 hours postdose, with dose-dependent increases in plasma SA. Subjects with eGFR < 45 ml/min per 1.73 m² showed elevated maximum plasma ManNAc concentration and area under curve for both ManNAc and SA, reflecting reduced renal clearance. Proteinuria reduction of 12% to 52% (regression-adjusted mean 9.69%, P < 0.0001) was observed in subjects receiving ManNAc BID, correlating with glomerular hyposialylation in pre-study renal biopsies.

Conclusion:

Oral ManNAc demonstrated short-term safety and increased plasma SA levels in podocytopathy subjects. Early efficacy signals suggest that proteinuria reduction may correlate with glomerular hyposialylation, identifying a potential treatment biomarker. A phase 2 trial (NCT06664814) is underway to assess long-term outcomes.

2026-03-01·JOURNAL OF BIOLOGICAL CHEMISTRY

Profiling the pancreatic cancer secretome with metabolic glycoengineering

Article

作者: Aafreen, Safiya ; Dharharma, Vrinda ; Liu, Guanshu ; Dammen-Brower, Kris ; Yarema, Kevin J ; Saeui, Christopher T ; Li, Hui ; Zhu, Stanley ; Song, Jian ; Buettner, Matthew J ; Kwagala, Keith R ; Zhang, Hui ; Agatemor, Christian ; Katz, Howard E

Profiling the secretome for biomarkers offers an attractive, minimally invasive strategy to detect and monitor cancer. Several challenges, however, must be overcome, including the broad dynamic range of biomolecules in the secretome and the requirement for selective detection of tumor-associated markers. Here, we employed a metabolic glycoengineering (MGE) strategy, using 1,3,4-O-Bu₃ManNAz, an azido-tagged, bio-orthogonal metabolic precursor of sialic acid, to label the glycome of pancreatic near-normal and cancer cells to improve conventional LC-MS/MS proteomics-based biomarker discovery. By using this "MGE-LC-MS/MS" approach that incorporates MGE enrichment into conventional LC-MS/MS proteomics, we identified several unique proteins from the secretomes of cancer cells evaluated in vitro. In addition to proteins known to be secreted, we identified several putatively intracellular, non-N-glycosylated proteins, such as β-glucocerebrosidase and paladin, linked to pancreatic cancer (PC) as well as proteins associated with extracellular vesicles (EVs) in PC, such as dCTP pyrophosphatase 1. The identification of EV-associated proteins was consistent with our discovery that ManNAc analogs used in the MGE-LC-MS/MS workflow enhance EV production, creating a more complete secretome profile of PC cells. Pointing toward clinical relevance, we used MGE-LC-MS/MS to enrich PC-derived glycoproteins from plasma harvested from mice bearing xenografted human pancreatic tumors, unambiguously demonstrating that this approach can interrogate the secretomes of cancer cells for biomarker discovery. Finally, we discovered that MGE dramatically improved the production of EVs, which both aids in biomarker discovery (this study) and holds potential to facilitate biomanufacturing of these nascent drugs.

2026-02-01·BRITISH JOURNAL OF CLINICAL PHARMACOLOGY

Absolute bioavailability and intravenous pharmacokinetics of N‐acetyl‐D‐mannosamine in humans

Article

作者: Allan M. Evans ; Guy Ludbrook ; Gianfranco Fornasini ; Tahlia R. Meola ; Stephanie E. Reuter ; Olga Pavlova ; Sumit Jain

Aims:

N‐acetyl‐D‐mannosamine monohydrate (ManNAc) is a naturally occurring monosaccharide that has attracted considerable attention for its potential in treating GNE myopathy, a rare autosomal recessive muscle disorder. Despite its promise as an oral treatment, the absolute bioavailability of oral ManNAc has not been determined and there has been no evaluation of the ManNAc pharmacokinetics following intravenous administration in humans. The aim of this study was to investigate the pharmacokinetics of intravenous ManNAc and to characterize its absolute bioavailability following a single oral dose.

Methods:

In this single‐centre, open‐label, crossover study, six healthy adult males were administered ManNAc as a single oral dose (1000 mg) and intravenous dose (100 mg). Blood samples were collected over a 48 h period after dose administration for the quantification of plasma ManNAc concentrations. Non‐compartmental pharmacokinetic analysis was performed using baseline‐corrected plasma concentration–time data.

Results:

After intravenous dosing, the mean plasma clearance of ManNAc was 10.1 ± 1.94 L/h, volume of distribution was 24.1 ± 4.98 L and elimination half‐life was 1.67 ± 0.251 h. The mean absolute bioavailability of oral ManNAc at a dose of 1000 mg was 4.01 ± 1.82%. Deconvolution analysis revealed a zero‐order absorption rate of about 10 mg per hour in the initial 3 h after dosing.

Conclusions:

The low oral bioavailability of ManNAc is likely due to poor absorption (rather than first‐pass hepatic extraction) due to its high polarity. In addition, zero‐order absorption explains why the systemic exposure to ManNAc does not increase proportionally with dose.

项与 N-acetyl-D-mannosamine 相关的新闻（医药）

2026-01-14

·bilibili

3,4-二氟-6-氮杂糖衍生物：氟化糖类化合物在药物发现中的新型构建单元

2-乙酰氨基-6-氮杂-1-O-乙酰-2,3,4,6-四脱氧-3,4-二氟-D-吡喃葡萄糖是一种结构经过精心设计的氟化糖类衍生物。该分子将氟原子引入到糖环骨架的特定位置，同时以氮原子替代了经典的6位碳，构成了一个兼具糖类特征与氮杂环特性的杂化骨架。此类经过多重修饰的糖类似物，正日益成为现代药物化学，尤其是核苷类似物、糖基化抑制剂及新型抗生素研发中备受关注的高级中间体与核心结构单元。 [图片] 化学信息化学名称： 2-Acetamido-6-azdio-1-O-acetyl-2,3,4,6-tetradeoxy-3,4-di-Fluoro-D-Glucopyranose 通用名： 3,4-二氟-6-氮杂糖衍生物化学式： C10H14F2N4O4 分子量： 292.24 g/mol 分类： Fluorinated Compound 结构特点该化合物的结构融合了多项关键的合成修饰，赋予其独特的物理化学与潜在生物学特性：双重氟原子取代：在糖环的3位和4位碳原子上引入两个氟原子，是结构的核心特征。氟原子的强电负性与较小原子半径，能显著改变分子整体的电子分布、偶极矩以及构象偏好，同时增强C-F键的代谢稳定性，有效抵抗糖苷键的酶解。 6-氮杂修饰：以氮原子替换传统吡喃糖6位的CH2基团，将吡喃环转化为一个含氮杂环。这一改变不仅引入了额外的氢键结合位点（胺基或质子化铵离子），也可能显著影响分子的碱性与溶解性，并模拟天然糖胺或核苷酸中的部分结构特征。选择性保护基团：1位羟基被乙酰化（1-O-acetyl），可作为进一步糖基化反应的离去基团或修饰位点；2位的乙酰氨基（Acetamido）则提供了稳定的酰胺键和潜在的分子识别位点，常见于几丁质、唾液酸等天然氨基糖的结构中。脱氧骨架：2,3,4,6位均为脱氧状态，这使得分子骨架更具刚性，疏水性增强，同时减少了被糖代谢酶识别和降解的可能性，更倾向于模拟某些天然产物的活性片段或作为药物递送载体。主要应用与优势创新药物研发的关键中间体作为高度官能团化的氟化氮杂糖，该分子是构建各类生物活性分子的理想起点。其结构可被进一步衍生化，用于合成新型的氟化核苷类似物（作为抗病毒或抗肿瘤药物的候选前体）、糖基转移酶抑制剂（用于代谢性疾病或炎症研究）以及作为糖模拟物干扰病原体细胞壁合成（探索新型抗菌策略）。氟化学在药物设计中的价值体现引入的3,4-二氟模式是经典的“双氟效应”应用实例。相邻的两个氟原子可以产生独特的立体电子效应，稳定特定的糖环构象（如1C4椅式构象），从而精确模拟天然底物过渡态或高能中间体的结构。这种精确的分子模拟能力，对于开发高选择性、高亲和力的酶抑制剂至关重要。优化先导化合物性质的多功能工具在药物化学优化中，该结构提供的修饰“工具箱”价值显著：氟原子的引入可提高脂溶性和膜通透性，延长体内半衰期；氮杂原子的引入可调节pKa，改善溶解度或靶标结合特异性；脱氧结构则能增强代谢稳定性。这些特性使得以其为核心衍生的分子，有潜力在药代动力学和药效学方面得到系统性优化。化学生物学与机理研究的探针分子该化合物及其衍生物可作为化学探针，用于研究糖类加工酶（如糖苷酶、糖基转移酶）对氟化及氮杂修饰底物的识别与催化机制。其独特的结构有助于阐明酶活性中心的精确几何与静电要求，推动糖类酶学的基础研究。结语 2-乙酰氨基-6-氮杂-1-O-乙酰-2,3,4,6-四脱氧-3,4-二氟-D-吡喃葡萄糖代表了一类融合了氟化学、糖化学与杂环化学精妙设计的高级合成砌块。其结构所蕴含的多重修饰潜力，为探索新的药物作用机制、克服现有疗法的局限性提供了独特的分子骨架。从靶向特定酶的抑制剂设计，到开发具有新颖作用模式的治疗剂，这一氟化氮杂糖衍生物展现出作为下一代生物活性分子发现平台的重要价值。以上资料由凯森斯生物小编提供，仅用于科研相关推荐 N-Acetyl-D-mannosamine CAS: 7772-94-3 D-Mannosamine hydrochloride CAS: 5505-63-5 5-DEOXY-L-ARABINOSE CAS: 920-60-8 2-Acetamido-1,3,4,6-tetra-O-acetyl-2-deoxy-5-thio-a-D-glucopyranose CAS: 67561-97-1 O-(2-Acetamido-2-deoxy-3,4,6-tri-O-acetyl-β-D-glucopyranosyl)-N-FMoc-L-serine CAS: 67561-96-0 Fmoc-Asn(Ac₃AcNH-β-Glc)-OH CAS: 160067-63-0 Fmoc-Ser[α-D-GalNAc(Ac)3]-OH CAS: 131287-39-3 Tetra-O-acetyl-α-Mannosyl-Fmocserine CAS: 120173-57-1 Fmoc-Ser(Ac₃Fucα)-OH CAS: 118358-80-8 L-Serine, N-[(9H-fluoren-9-ylmethoxy)carbonyl]-O-(2,3,4-tri-O-acetyl-6-deoxy-β-L-galactopyranosyl)- CAS: 173935-46-1 L-Ser(Fmoc)-O-(2,3,4-tri-O-Ac-6-deoxy-β-L-Galp)-OH CAS: 118358-72-8 Fmoc-Thr(Ac₃Fucα)-OH CAS: 184851-26-1 N-[(9H-芴-9-基甲氧基)羰基]-O-(2,3,4-三-O-乙酰基-6-脱氧-β-D-半乳吡喃糖基)-L-苏氨酸 CAS: 174623-16-6 T Epitope, Serinyl CAS: 60280-57-1 L-Serine, N-[(9H-fluoren-9-ylmethoxy)carbonyl]-O-[O-2,3,4,6-tetra-O-acetyl-β-D-galactopyranosyl-(1→3)-O-[3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D- CAS: 1954673-83-6 Fmoc-Thr((Ac₄Galβ1-3)Ac₃GlcNAcβ1-6AcGalNAcα)-OH CAS: 1240252-34-9 L-Serine, O-[O-2-(acetylamino)-2-deoxy-β-D-glucopyranosyl-(1→6)-O-[β-D-galactopyranosyl-(1→3)]-2-(acetylamino)-2-deoxy-α-D- CAS: 110797-61-0 L-Serine, O-[4,6-di-O-acetyl-2-(acetylamino)-2-deoxy-3-O-[3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D-glucopyranosyl]-α-D-galactopyranosyl]-N-[(9H-fluoren-9-ylmethoxy)carbonyl]- CAS: 878483-09-1 L-Threonine, O-[4,6-di-O-acetyl-2-(acetylamino)-2-deoxy-3-O-[3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D-glucopyranosyl]-α-D-galactopyranosyl]-N-[(9H-fluoren-9-ylmethoxy)carbonyl]- CAS: 878483-13-7 GlcNAc beta(1-3)GalNAc-alpha-Thr CAS: 126740-76-9 GlcNAc beta(1-3)[GlcNAc beta(1-6)]GalNAc-alpha-Thr CAS: 1304646-00-1 N-[(1S,2R,3E)-2-hydroxy-1-[[[O-[N-(2-hydroxyacetyl)-α-neuraminosyl]-(2→3)-O-β-D-galactopyranosyl-(1→4)-β-D-glucopyranosyl]oxy]methyl]-3-heptadecen-1-yl]-Octadecanamide） CAS: 851608-39-4 N-硬脂酰基-D-赤型鞘氨醇-1-磷酸胆碱 CAS: 58909-84-5 BETA-D-GAL-[1->3]-D-GALNAC CAS: 20972-29-6 血液H组二糖 CAS: 146076-26-8 N-乙酰神经氨酰基-(2-3)-半乳糖 CAS: 83563-61-5 N-乙酰神经氨酰-(2-6)-半乳糖（钠盐） CAS: 35259-23-5 Globopentaose CAS: 71937-76-3 3'-(N-Glycolyl-a-neuraminosyl)lactose CAS: 81275-44-7 2-[(Azidoacetyl)amino]-2-deoxy-D-glucopyranose 1,3,4,6-tetraacetate CAS: 98924-81-3 N-叠氮乙酰半乳糖胺四酯化物 (Ac4GalNAz) CAS: 653600-56-7 2-[(2-叠氮乙酰基)氨基]-2-脱氧-D-吡喃甘露糖 1971934-97-0 1,3,4,6-四-O-乙酰基-N-叠氮乙酰基氨基甘露糖 CAS: 361154-30-5 [图片]

临床结果

2026-01-14

·知乎专栏

2-Acetamido-2,3,4-trideoxy-3,4-di-Fluoro-D-Glucopyranose—氟化糖化学中的关键合成砌块

2-Acetamido-2,3,4-trideoxy-3,4-di-Fluoro-D-Glucopyranose 是一种结构独特且经过精确设计的氟化单糖衍生物。作为氟化化合物（Fluorinated Compound）家族的重要成员，其在现代药物化学与糖生物学研究中扮演着日益关键的角色。氟原子的引入犹如为分子装上了精密的“化学开关”，能够深刻改变其物理化学性质及生物活性，使其成为开发新型治疗剂和探索生命过程的强大工具。化学信息化学名称： 2-Acetamido-2,3,4-trideoxy-3,4-di-Fluoro-D-Glucopyranose通用名： 2,3,4-三脱氧-3,4-二氟-N-乙酰氨基葡萄糖化学式： C8H13F2NO4分子量： 225.29 g/mol分类：Fluorinated Compound结构特点该分子以D-葡萄糖吡喃糖为基本骨架，经过精妙的化学修饰，呈现出以下几个核心结构特征：多重脱氧与氟取代：在糖环的2、3、4位进行了脱氧处理，同时于3位和4位引入了两个氟原子。这种设计显著降低了糖环的极性，并极大地增强了整个分子对酶降解和化学分解的代谢稳定性。关键乙酰氨基修饰：在2位连接有一个乙酰氨基基团。这一基团是许多生物活性糖类（如几丁质、某些糖胺聚糖的组成单元）中常见的结构模体，提供了重要的分子识别位点，可用于模拟天然糖类与蛋白质的相互作用。l立体化学控制：氟原子的引入不仅改变了电子分布，其强电负性和较小的原子半径（与氢原子相近）使其能够微妙地调整分子构象和立体电子效应，从而影响其与生物靶点的结合亲和力与特异性。主要应用与优势1.药物化学中的先进合成砌块在创新药物研发中，该化合物是构建具有改善药代动力学性质候选药物的宝贵中间体。氟原子的引入可以增强脂溶性，促进细胞膜渗透，提高口服生物利用度。其稳定的C-F键能有效阻断代谢位点，延长药物在体内的半衰期。特别在开发靶向糖苷酶、糖基转移酶或凝集素的抑制剂方面，其作为糖模拟物具有巨大潜力。2.糖类疫苗与糖类药物研发的潜在前体基于碳水化合物的疫苗（如抗细菌或抗肿瘤疫苗）是前沿研究方向。2-Acetamido-2,3,4-trideoxy-3,4-di-Fluoro-D-Glucopyranose 可作为合成非天然、代谢稳定的糖抗原或佐剂分子的核心单元。其独特的氟化结构可能有助于产生更具特异性和效力的免疫反应。3.化学生物学与机理研究的探针分子在基础研究领域，该分子是探索糖-蛋白相互作用、酶催化机制以及细胞信号传导通路的理想化学工具。氟原子可作为19F核磁共振（NMR）的敏感探针，用于实时、无背景干扰地监测分子在复杂生物体系中的行为、定位及代谢过程。此外，它也可用于合成稳定的糖肽或糖脂类似物，以研究糖基化修饰的功能。4.抗生素与抗病毒药物修饰的灵感来源许多天然抗生素和抗病毒药物含有糖基结构。将该氟化糖结构单元引入此类分子中，进行结构优化，有望克服现有药物的耐药性、提高其稳定性和疗效，为开发新一代抗感染药物提供新的思路。结语2-Acetamido-2,3,4-trideoxy-3,4-di-Fluoro-D-Glucopyranose 代表了合成有机化学与药物设计融合的精细成果。它不仅仅是一个氟化糖分子，更是一个功能强大的多功能平台，为跨越药物发现、疫苗开发和基础科学研究的多个领域提供了独特的化学空间与可能性。其价值在于赋能研究人员设计与构建下一代更具针对性、更稳定、更有效的生物活性分子。以上资料由凯森斯生物小编提供，仅用于科研相关推荐N-Acetyl-D-mannosamine CAS: 7772-94-3D-Mannosamine hydrochloride CAS: 5505-63-55-DEOXY-L-ARABINOSE CAS: 920-60-82-Acetamido-1,3,4,6-tetra-O-acetyl-2-deoxy-5-thio-a-D-glucopyranose CAS: 67561-97-1O-(2-Acetamido-2-deoxy-3,4,6-tri-O-acetyl-β-D-glucopyranosyl)-N-FMoc-L-serine CAS: 67561-96-0Fmoc-Asn(Ac₃AcNH-β-Glc)-OH CAS: 160067-63-0Fmoc-Ser[α-D-GalNAc(Ac)3]-OH CAS: 131287-39-3Tetra-O-acetyl-α-Mannosyl-Fmocserine CAS: 120173-57-1Fmoc-Ser(Ac₃Fucα)-OH CAS: 118358-80-8L-Serine, N-[(9H-fluoren-9-ylmethoxy)carbonyl]-O-(2,3,4-tri-O-acetyl-6-deoxy-β-L-galactopyranosyl)- CAS: 173935-46-1L-Ser(Fmoc)-O-(2,3,4-tri-O-Ac-6-deoxy-β-L-Galp)-OH CAS: 118358-72-8Fmoc-Thr(Ac₃Fucα)-OH CAS: 184851-26-1N-[(9H-芴-9-基甲氧基)羰基]-O-(2,3,4-三-O-乙酰基-6-脱氧-β-D-半乳吡喃糖基)-L-苏氨酸 CAS: 174623-16-6T Epitope, Serinyl CAS: 60280-57-1L-Serine, N-[(9H-fluoren-9-ylmethoxy)carbonyl]-O-[O-2,3,4,6-tetra-O-acetyl-β-D-galactopyranosyl-(1→3)-O-[3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D- CAS: 1954673-83-6Fmoc-Thr((Ac₄Galβ1-3)Ac₃GlcNAcβ1-6AcGalNAcα)-OH CAS: 1240252-34-9L-Serine, O-[O-2-(acetylamino)-2-deoxy-β-D-glucopyranosyl-(1→6)-O-[β-D-galactopyranosyl-(1→3)]-2-(acetylamino)-2-deoxy-α-D- CAS: 110797-61-0L-Serine, O-[4,6-di-O-acetyl-2-(acetylamino)-2-deoxy-3-O-[3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D-glucopyranosyl]-α-D-galactopyranosyl]-N-[(9H-fluoren-9-ylmethoxy)carbonyl]- CAS: 878483-09-1L-Threonine, O-[4,6-di-O-acetyl-2-(acetylamino)-2-deoxy-3-O-[3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D-glucopyranosyl]-α-D-galactopyranosyl]-N-[(9H-fluoren-9-ylmethoxy)carbonyl]- CAS: 878483-13-7GlcNAc beta(1-3)GalNAc-alpha-Thr CAS: 126740-76-9GlcNAc beta(1-3)[GlcNAc beta(1-6)]GalNAc-alpha-Thr CAS: 1304646-00-1N-[(1S,2R,3E)-2-hydroxy-1-[[[O-[N-(2-hydroxyacetyl)-α-neuraminosyl]-(2→3)-O-β-D-galactopyranosyl-(1→4)-β-D-glucopyranosyl]oxy]methyl]-3-heptadecen-1-yl]-Octadecanamide） CAS: 851608-39-4N-硬脂酰基-D-赤型鞘氨醇-1-磷酸胆碱 CAS: 58909-84-5BETA-D-GAL-[1->3]-D-GALNAC CAS: 20972-29-6血液H组二糖 CAS: 146076-26-8N-乙酰神经氨酰基-(2-3)-半乳糖 CAS: 83563-61-5N-乙酰神经氨酰-(2-6)-半乳糖（钠盐） CAS: 35259-23-5Globopentaose CAS: 71937-76-33'-(N-Glycolyl-a-neuraminosyl)lactose CAS: 81275-44-72-[(Azidoacetyl)amino]-2-deoxy-D-glucopyranose 1,3,4,6-tetraacetate CAS: 98924-81-3N-叠氮乙酰半乳糖胺四酯化物 (Ac4GalNAz) CAS: 653600-56-72-[(2-叠氮乙酰基)氨基]-2-脱氧-D-吡喃甘露糖 1971934-97-01,3,4,6-四-O-乙酰基-N-叠氮乙酰基氨基甘露糖 CAS: 361154-30-5

2026-01-14

·bilibili

氟化糖化学中的关键合成砌块

2-Acetamido-2,3,4-trideoxy-3,4-di-Fluoro-D-Glucopyranose 是一种结构独特且经过精确设计的氟化单糖衍生物。作为氟化化合物（Fluorinated Compound）家族的重要成员，其在现代药物化学与糖生物学研究中扮演着日益关键的角色。氟原子的引入犹如为分子装上了精密的“化学开关”，能够深刻改变其物理化学性质及生物活性，使其成为开发新型治疗剂和探索生命过程的强大工具。 [图片] 化学信息化学名称： 2-Acetamido-2,3,4-trideoxy-3,4-di-Fluoro-D-Glucopyranose 通用名： 2,3,4-三脱氧-3,4-二氟-N-乙酰氨基葡萄糖化学式： C8H13F2NO4 分子量： 225.29 g/mol 分类：Fluorinated Compound 结构特点该分子以D-葡萄糖吡喃糖为基本骨架，经过精妙的化学修饰，呈现出以下几个核心结构特征：多重脱氧与氟取代：在糖环的2、3、4位进行了脱氧处理，同时于3位和4位引入了两个氟原子。这种设计显著降低了糖环的极性，并极大地增强了整个分子对酶降解和化学分解的代谢稳定性。关键乙酰氨基修饰：在2位连接有一个乙酰氨基基团。这一基团是许多生物活性糖类（如几丁质、某些糖胺聚糖的组成单元）中常见的结构模体，提供了重要的分子识别位点，可用于模拟天然糖类与蛋白质的相互作用。 l立体化学控制：氟原子的引入不仅改变了电子分布，其强电负性和较小的原子半径（与氢原子相近）使其能够微妙地调整分子构象和立体电子效应，从而影响其与生物靶点的结合亲和力与特异性。主要应用与优势 1.药物化学中的先进合成砌块在创新药物研发中，该化合物是构建具有改善药代动力学性质候选药物的宝贵中间体。氟原子的引入可以增强脂溶性，促进细胞膜渗透，提高口服生物利用度。其稳定的C-F键能有效阻断代谢位点，延长药物在体内的半衰期。特别在开发靶向糖苷酶、糖基转移酶或凝集素的抑制剂方面，其作为糖模拟物具有巨大潜力。 2.糖类疫苗与糖类药物研发的潜在前体基于碳水化合物的疫苗（如抗细菌或抗肿瘤疫苗）是前沿研究方向。2-Acetamido-2,3,4-trideoxy-3,4-di-Fluoro-D-Glucopyranose 可作为合成非天然、代谢稳定的糖抗原或佐剂分子的核心单元。其独特的氟化结构可能有助于产生更具特异性和效力的免疫反应。 3.化学生物学与机理研究的探针分子在基础研究领域，该分子是探索糖-蛋白相互作用、酶催化机制以及细胞信号传导通路的理想化学工具。氟原子可作为19F核磁共振（NMR）的敏感探针，用于实时、无背景干扰地监测分子在复杂生物体系中的行为、定位及代谢过程。此外，它也可用于合成稳定的糖肽或糖脂类似物，以研究糖基化修饰的功能。 4.抗生素与抗病毒药物修饰的灵感来源许多天然抗生素和抗病毒药物含有糖基结构。将该氟化糖结构单元引入此类分子中，进行结构优化，有望克服现有药物的耐药性、提高其稳定性和疗效，为开发新一代抗感染药物提供新的思路。结语 2-Acetamido-2,3,4-trideoxy-3,4-di-Fluoro-D-Glucopyranose 代表了合成有机化学与药物设计融合的精细成果。它不仅仅是一个氟化糖分子，更是一个功能强大的多功能平台，为跨越药物发现、疫苗开发和基础科学研究的多个领域提供了独特的化学空间与可能性。其价值在于赋能研究人员设计与构建下一代更具针对性、更稳定、更有效的生物活性分子。以上资料由凯森斯生物小编提供，仅用于科研相关推荐 N-Acetyl-D-mannosamine CAS: 7772-94-3 D-Mannosamine hydrochloride CAS: 5505-63-5 5-DEOXY-L-ARABINOSE CAS: 920-60-8 2-Acetamido-1,3,4,6-tetra-O-acetyl-2-deoxy-5-thio-a-D-glucopyranose CAS: 67561-97-1 O-(2-Acetamido-2-deoxy-3,4,6-tri-O-acetyl-β-D-glucopyranosyl)-N-FMoc-L-serine CAS: 67561-96-0 Fmoc-Asn(Ac₃AcNH-β-Glc)-OH CAS: 160067-63-0 Fmoc-Ser[α-D-GalNAc(Ac)3]-OH CAS: 131287-39-3 Tetra-O-acetyl-α-Mannosyl-Fmocserine CAS: 120173-57-1 Fmoc-Ser(Ac₃Fucα)-OH CAS: 118358-80-8 L-Serine, N-[(9H-fluoren-9-ylmethoxy)carbonyl]-O-(2,3,4-tri-O-acetyl-6-deoxy-β-L-galactopyranosyl)- CAS: 173935-46-1 L-Ser(Fmoc)-O-(2,3,4-tri-O-Ac-6-deoxy-β-L-Galp)-OH CAS: 118358-72-8 Fmoc-Thr(Ac₃Fucα)-OH CAS: 184851-26-1 N-[(9H-芴-9-基甲氧基)羰基]-O-(2,3,4-三-O-乙酰基-6-脱氧-β-D-半乳吡喃糖基)-L-苏氨酸 CAS: 174623-16-6 T Epitope, Serinyl CAS: 60280-57-1 L-Serine, N-[(9H-fluoren-9-ylmethoxy)carbonyl]-O-[O-2,3,4,6-tetra-O-acetyl-β-D-galactopyranosyl-(1→3)-O-[3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D- CAS: 1954673-83-6 Fmoc-Thr((Ac₄Galβ1-3)Ac₃GlcNAcβ1-6AcGalNAcα)-OH CAS: 1240252-34-9 L-Serine, O-[O-2-(acetylamino)-2-deoxy-β-D-glucopyranosyl-(1→6)-O-[β-D-galactopyranosyl-(1→3)]-2-(acetylamino)-2-deoxy-α-D- CAS: 110797-61-0 L-Serine, O-[4,6-di-O-acetyl-2-(acetylamino)-2-deoxy-3-O-[3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D-glucopyranosyl]-α-D-galactopyranosyl]-N-[(9H-fluoren-9-ylmethoxy)carbonyl]- CAS: 878483-09-1 L-Threonine, O-[4,6-di-O-acetyl-2-(acetylamino)-2-deoxy-3-O-[3,4,6-tri-O-acetyl-2-(acetylamino)-2-deoxy-β-D-glucopyranosyl]-α-D-galactopyranosyl]-N-[(9H-fluoren-9-ylmethoxy)carbonyl]- CAS: 878483-13-7 GlcNAc beta(1-3)GalNAc-alpha-Thr CAS: 126740-76-9 GlcNAc beta(1-3)[GlcNAc beta(1-6)]GalNAc-alpha-Thr CAS: 1304646-00-1 N-[(1S,2R,3E)-2-hydroxy-1-[[[O-[N-(2-hydroxyacetyl)-α-neuraminosyl]-(2→3)-O-β-D-galactopyranosyl-(1→4)-β-D-glucopyranosyl]oxy]methyl]-3-heptadecen-1-yl]-Octadecanamide） CAS: 851608-39-4 N-硬脂酰基-D-赤型鞘氨醇-1-磷酸胆碱 CAS: 58909-84-5 BETA-D-GAL-[1->3]-D-GALNAC CAS: 20972-29-6 血液H组二糖 CAS: 146076-26-8 N-乙酰神经氨酰基-(2-3)-半乳糖 CAS: 83563-61-5 N-乙酰神经氨酰-(2-6)-半乳糖（钠盐） CAS: 35259-23-5 Globopentaose CAS: 71937-76-3 3'-(N-Glycolyl-a-neuraminosyl)lactose CAS: 81275-44-7 2-[(Azidoacetyl)amino]-2-deoxy-D-glucopyranose 1,3,4,6-tetraacetate CAS: 98924-81-3 N-叠氮乙酰半乳糖胺四酯化物 (Ac4GalNAz) CAS: 653600-56-7 2-[(2-叠氮乙酰基)氨基]-2-脱氧-D-吡喃甘露糖 1971934-97-0 1,3,4,6-四-O-乙酰基-N-叠氮乙酰基氨基甘露糖 CAS: 361154-30-5 [图片]

100 项与 N-acetyl-D-mannosamine 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
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研发状态

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适应症	最高研发状态	国家/地区	公司	日期
局灶性节段性肾小球硬化症	临床2期	美国	National Human Genome Research Institute	2026-04-21
遗传性包涵体肌病	临床2期	美国	National Human Genome Research Institute	2015-02-05
膜性肾小球肾炎	临床1期	美国	National Institute of Diabetes & Digestive & Kidney Diseases	2016-07-07
微小病变性肾病	临床1期	美国	National Institute of Diabetes & Digestive & Kidney Diseases	2016-07-07

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02346461 (Pubmed \| Genet Med) 人工标引	临床2期	遗传性包涵体肌病	12	ManNAc	糧壓築醖遞鹽廠鹹衊獵(糧糧衊夢願淵簾網襯簾) = 憲鏇餘餘齋餘鏇醖壓鏇繭鹹淵衊繭築築廠醖範 (網窪構簾願窪網願鹽網 )	积极	2021-11-01
NCT02639260 (Phase 1 Study of N-Acetylmannosamine (ManNAc) for Glomerular Disease, ASN2020)	临床1期	肾小球疾病	7	ManNAc 3g single dose	憲繭鏇遞顧築範獵窪選(簾鑰構憲繭觸範窪積鑰) = There were no serious adverse events. Most subjects (5 of 6) that received ManNAc twice daily showed a marked reduction in urine PCR (26-54%), which correlated with the degree of glomerular hyposialylation 鬱鑰淵壓積積窪獵遞鹹 (膚膚顧齋網顧醖願繭艱 ) 更多	积极	2020-10-19
NCT02346461 (CTgov)	临床2期	遗传性包涵体肌病	12	ManNAc (ManNAc: Cohort A)	鑰鏇鏇鏇餘鬱製窪衊窪(遞淵鑰衊積蓋夢齋衊製) = 夢願鹽蓋繭廠選淵衊觸簾艱廠鑰顧膚鏇顧糧蓋 (鑰鏇網網鬱糧壓膚選選, 1776) 更多	-	2019-04-16
NCT02346461 (CTgov)	临床2期	遗传性包涵体肌病	12	ManNAc (ManNAc: Cohort B)	鑰鏇鏇鏇餘鬱製窪衊窪(遞淵鑰衊積蓋夢齋衊製) = 範鏇製餘鏇簾築顧廠衊簾艱廠鑰顧膚鏇顧糧蓋 (鑰鏇網網鬱糧壓膚選選, 2710) 更多	-	2019-04-16