Anidulafungin
(Synonyms: 阿尼芬净; LY303366) 目录号 : GC12754
Anidulafungin是一种棘白菌素类抗真菌药物。
Cas No.:166663-25-8
Sample solution is provided at 25 µL, 10mM.
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Anidulafungin is an echinocandin antifungal drug [1]. Anidulafungin inhibits the synthesis of β-(1,3)-D-glucan in the fungal cell wall, thereby disrupting the integrity of the cell wall and causing cell lysis and death [2]. Anidulafungin is primarily used to treat invasive candida infections, including candidemia and other deep candidiasis, and is particularly suitable for patients who cannot tolerate or are resistant to azoles such as fluconazole [3-4].
In erythrocytes, Anidulafungin (1.5-6µg/mL; 48h) can cause morphological changes in red blood cells, manifested as cell shrinkage, decreased forward scattering, and increased hemolysis rate, suggesting that it may affect red blood cell integrity by destroying cell membrane stability [5]. In BV2 microglial cells, Anidulafungin (10nM–5μM, 24h) selectively blocks the primary nucleation of Aβ aggregation, significantly delays fibril formation, and confers potential neuroprotective effects by reducing oligomeric Aβ-induced cytotoxicity [6].
In invasive Candidiasis mice model, signs of improved infection in the kidneys of mice treated with Anidulafungin (0.3mg/kg; iv; 6d) included a reduction in the area of inflammatory cells and the number of fungal hyphae surrounding tubules and glomeruli [7]. In neutropenic murine disseminated Candidiasis model, Anidulafungin (1.25–320mg/kg; ip; 96h) exhibits potent efficacy against multiple Candida species (including C. albicans, C. tropicalis, and C. glabrata), with its activity primarily determined by the C_max/MIC and AUC/MIC ratios, maintaining prolonged antifungal effects even when blood concentrations fall below the MIC, thereby demonstrating sustained activity and favorable pharmacokinetic properties [8].
References:
[1]. Raasch R H. Anidulafungin: review of a new echinocandin antifungal agent[J]. Expert review of anti-infective therapy, 2004, 2(4): 499-508.
[2]. Aderiye B I, Oluwole O A. Antifungal agents that target fungal cell wall components: a review[J]. Agri Biol Sci, 2015, 1: 206-216.
[3]. Vazquez J A, Sobel J D. Anidulafungin: a novel echinocandin[J]. Clinical infectious diseases, 2006, 43(2): 215-222.
[4]. Mayr A, Aigner M, Lass‐Flörl C. Anidulafungin for the treatment of invasive candidiasis[J]. Clinical Microbiology and Infection, 2011, 17: 1-12.
[5]. Peter T, Bissinger R, Liu G, et al. Anidulafungin-induced suicidal erythrocyte death[J]. Cellular Physiology and Biochemistry, 2016, 38(6): 2272-2284.
[6]. Xie S, Liang Y, Song Y, et al. Repurposing Anidulafungin for Alzheimer’s Disease via Fragment-Based Drug Discovery[J]. ACS Chemical Neuroscience, 2024, 15(16): 2995-3008.
[7]. Zhang Y, Liu Y C, Chen S M, et al. Evaluation of the in vitro activity and in vivo efficacy of anidulafungin-loaded human serum albumin nanoparticles against Candida albicans[J]. Frontiers in Microbiology, 2021, 12: 788442.
[8]. Andes D, Diekema DJ, Pfaller MA, et al. In vivo pharmacodynamic characterization of anidulafungin in a neutropenic murine candidiasis model. Antimicrob Agents Chemother. 2008 Feb;52(2):539-50.
Anidulafungin是一种棘白菌素类抗真菌药物 [1]。Anidulafungin抑制真菌细胞壁中β-(1,3)-D-葡聚糖的合成，从而破坏细胞壁的完整性，导致细胞裂解和死亡 [2]。Anidulafungin主要用于治疗侵袭性念珠菌感染，包括念珠菌血症和其他深部念珠菌病，尤其适用于对fluconazole等唑类药物无法耐受或耐药的患者 [3-4]。
在红细胞中，Anidulafungin（1.5-6µg/mL；48h）可引起红细胞形态学改变，表现为细胞皱缩、前向散射降低和溶血率增加，提示其可能通过破坏细胞膜稳定性来影响红细胞完整性 [5]。在BV2小胶质细胞中，Anidulafungin（10nM-5μM，24h）选择性阻断Aβ聚集的初级成核，显著延缓纤维形成，并通过降低寡聚Aβ诱导的细胞毒性发挥潜在的神经保护作用 [6]。
在侵袭性念珠菌病小鼠模型中，经Anidulafungin（0.3mg/kg；iv；6d）治疗的小鼠肾脏感染改善的迹象包括炎症细胞面积减少以及肾小管和肾小球周围真菌菌丝数量的减少 [7]。在中性粒细胞减少性小鼠播散性念珠菌病模型中，Anidulafungin（1.25-320mg/kg；ip；96h）对多种念珠菌（包括白色念珠菌、热带念珠菌和光滑念珠菌）表现出强效疗效，其活性主要由C_max/MIC和AUC/MIC比率决定，即使血液浓度低于MIC也能维持长时间的抗真菌作用，从而表现出持续的活性和良好的药代动力学特性 [8]。
| Cell experiment [1]: | |
Cell lines | Erythrocytes |
Preparation Method | The blood was centrifuged at 120g for 20min at 21℃ and the platelets and leukocytes-containing supernatant was disposed. Erythrocytes were incubated in vitro at a hematocrit of 0.4% in Ringer solution containing 125mM NaCl, 5mM KCl, 1mM MgSO4, 32 N-2-hydroxyethylpiperazine-N-2-ethanesulfonic acid (HEPES; pH 7.4), 5mM glucose, 1mM CaCl2, at 37℃ for 48 hours. To test for an involvement of oxidative stress, erythrocytes were exposed for 48 hours to a combination of Anidulafungin and the antioxidant N-acetylcysteine. |
Reaction Conditions | 1.5-6µg/mL; 48h |
Applications | Anidulafungin can cause morphological changes in red blood cells, manifested as cell shrinkage, decreased forward scattering, and increased hemolysis rate, suggesting that it may affect red blood cell integrity by destroying cell membrane stability. |
| Animal experiment [2]: | |
Animal models | Invasive candidiasis mice model |
Preparation Method | This study evaluated the in vivo antifungal efficacy of Anidulafungin and its Anidulafungin nanoparticles. Immunocompetent female C57BL/6 mice, 7–8 weeks old and weighing 18–20g, were randomly divided into groups based on body weight and injected via the lateral tail vein with 1×106 CFU of candida albicans SC5314 to establish an infection model. For survival experiments, a single dose of antifungal therapy was initiated 2 hours after fungal inoculation. Treatment groups included a PBS control group, a 0.3mg/kg Anidulafungin group, and a 0.3mg/kg Anidulafungin nanoparticles group. |
Dosage form | 0.3mg/kg; iv; 6d |
Applications | Signs of improved infection in the kidneys of mice treated with Anidulafungin included a reduction in the area of inflammatory cells and the number of fungal hyphae surrounding tubules and glomeruli. |
References: | |
| Cas No. | 166663-25-8 | SDF | |
| 别名 | 阿尼芬净; LY303366 | ||
| Canonical SMILES | O[C@H]1[C@H](C)CN(C([C@H]([C@H](C)O)NC([C@H]([C@@H]([C@@H](C(C=C2)=CC=C2O)O)O)NC([C@H](C3)N(C([C@H]([C@H](C)O)NC4=O)=O)C[C@@H]3O)=O)=O)=O)[C@@H]1C(N[C@H]([C@@H](C[C@@H]4NC(C5=CC=C(C6=CC=C(C(C=C7)=CC=C7OCCCCC)C=C6)C=C5)=O)O)O)=O | ||
| 分子式 | C58H73N7O17 | 分子量 | 1140.24 |
| 溶解度 | ≥ 30 mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 877 μL | 4.385 mL | 8.7701 mL |
| 5 mM | 175.4 μL | 877 μL | 1.754 mL |
| 10 mM | 87.7 μL | 438.5 μL | 877 μL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet