Micafungin sodium
(Synonyms: 米卡芬净钠; FK 463 sodium) 目录号 : GC17507
Micafungin sodium是一种棘白菌素类抗真菌药，能够抑制白色念珠菌中的1，3-β-D-葡聚糖合成。Micafungin sodium是Micafungin（货号：GC32244）的钠盐形式，Micafungin能够用于治疗多种真菌感染，包括念珠菌病和曲霉病。
Cas No.:208538-73-2
Sample solution is provided at 25 µL, 10mM.
Micafungin sodium is an echinocandin antifungal that inhibits 1,3-β-D-glucan synthesis in Candida albicans[1]. Micafungin sodium is the sodium salt form of Micafungin (Cat. No. GC32244), which is used to treat a variety of fungal infections, including candidiasis and aspergillosis[2]. Micafungin can inhibit dengue virus infection by disrupting viral binding, entry, and stability[3]. Micafungin has the ability to stimulate phagocytes and promote immune responses, thereby inhibiting microbial infection[4]. Micafungin is a promising inhibitor of ubiquitin-conjugating enzyme E2M (UBE2M) and can inhibit cancer cell growth[5].
In vitro, treatment of erythrocytes with Micafungin (10-25µg/mL) for 48h significantly increased the percentage of hemolyzed and annexin V-bound cells and significantly reduced forward scatter[6].
In vivo, Micafungin (1mg/kg) was injected intraperitoneally to treat mice with mucormycosis and significantly improved the survival rate of mice, but it did not exert a synergistic effect when used in combination with Isavuconazonium sulphate[7]. Treatment of mice with doxorubicin-induced cardiotoxicity with Micafungin (10, 20mg/kg) improved cardiac function and inhibited oxidative stress, mitochondrial dysfunction, and cell death in a dose-dependent manner[8].
References:
[1] Vehreschild J J, Cornely O A. Micafungin sodium, the second of the echinocandin class of antifungals: theory and practice[J]. Future Microbiology, 2006, 1(2): 161-170.
[2] Carver P L. Micafungin[J]. Annals of Pharmacotherapy, 2004, 38(10): 1707-1721.
[3] Chen Y C, Lu J W, Yeh C T, et al. Micafungin inhibits dengue virus infection through the disruption of virus binding, entry, and stability[J]. Pharmaceuticals, 2021, 14(4): 338.
[4] Fuchs B B, Li Y, Li D, et al. Micafungin elicits an immunomodulatory effect in Galleria mellonella and mice[J]. Mycopathologia, 2016, 181: 17-25.
[5] Mamun M A A, Liu S, Zhao L, et al. Micafungin: a promising inhibitor of UBE2M in cancer cell growth suppression[J]. European Journal of Medicinal Chemistry, 2023, 260: 115732.
[6] Peter T, Bissinger R, Signoretto E, et al. Micafungin-induced suicidal erythrocyte death[J]. Cellular Physiology and Biochemistry, 2016, 39(2): 584-595.
[7] Gebremariam T, Wiederhold N P, Alqarihi A, et al. Monotherapy or combination therapy of isavuconazole and micafungin for treating murine mucormycosis[J]. Journal of Antimicrobial Chemotherapy, 2016: dkw433.
[8] Lu L Q, Li M R, Huang L L, et al. Micafungin protects mouse heart against doxorubicin-induced oxidative injury via suppressing MALT1-dependent k48-linked ubiquitination of Nrf2[J]. Chemico-Biological Interactions, 2024, 400: 111179.
Micafungin sodium是一种棘白菌素类抗真菌药，能够抑制白色念珠菌中的1，3-β-D-葡聚糖合成[1]。Micafungin sodium是Micafungin（货号：GC32244）的钠盐形式，Micafungin能够用于治疗多种真菌感染，包括念珠菌病和曲霉病[2]。Micafungin能够通过破坏病毒结合、进入和稳定性来抑制登革热病毒感染[3]。Micafungin具有刺激吞噬细胞和促进免疫反应的能力，从而抑制微生物感染[4]。Micafungin是一种有前景的泛素结合酶E2M（UBE2M）抑制剂，可抑制癌细胞生长[5]。
在体外，Micafungin（10-25µg/mL）处理红细胞48h，显著增加了溶血和膜联蛋白V结合细胞的百分比，并显著减少前向散射[6]。
在体内，Micafungin（1mg/kg）通过腹腔注射治疗毛霉菌病小鼠，显著提高了小鼠的存活率，但与硫酸艾沙康唑（Isavuconazonium sulphate）联合使用并不能发挥协同作用[7]。Micafungin（10, 20mg/kg）治疗阿霉素诱导的心脏毒性模型小鼠，改善了心脏功能，以剂量依赖性方式抑制了氧化应激、线粒体功能障碍和细胞死亡[8]。
| Cell experiment [1]: | |
Cell lines | Erythrocytes |
Preparation Method | Erythrocytes were incubated for 48h in Ringer's solution without or with Micafungin (10-25µg/mL). Phosphatidylserine exposing erythrocytes were identified utilizing annexin-V-binding, as determined by flow cytometry. |
Reaction Conditions | 10-25µg/mL; 48h |
Applications | Micafungin significantly increased the percentage of annexin-V-binding cells. |
| Animal experiment [2]: | |
Animal models | Neutropenic mice |
Preparation Method | Neutropenic mice were intratracheally infected with 2.5×105 spores in 25mL PBS of M. circinelloides f. jenssenii or R. delemar 99-880 using a gelloading tip after sedation with isoflurane gas. Following inoculationthree mice were sacrificed and their lungs harvested for quantification the delivered fungal inoculum by quantitative culturing on potato dextrose agar+0.1% triton X-100. Treatment with Isavuconazonium sulphate (110 or 215mg/kg three times daily given orally), Micafungin (1mg/kg once daily, i.p.) or combination of Isavuconazonium sulphate+Micafungin started 16h postinfection and continued through day 4. Mice treated with a high dose of liposomal amphotericin B (LAmB) (15mg/kg once daily, i.v.) was included as a positive control. The primary and secondary endpoints were time to moribundity of mice infected and tissue fungal burden in lungs and brains (primary and secondary target organs) determined using quantitative PCR, respectively. |
Dosage form | 1mg/kg/day for 4 days; i.p. |
Applications | All monotherapy arms resulted in a comparable significant enhancement of 40%-60% survival when compared with placebo-treated mice. Although mice treated with Isavuconazole+Micafungin had significantly enhanced survival compared with placebo-treated mice, the combination therapy was not better than treatment with monotherapy. |
References: | |
| Cas No. | 208538-73-2 | SDF | |
| 别名 | 米卡芬净钠; FK 463 sodium | ||
| Canonical SMILES | CCCCCOC1=CC=C(C=C1)C2=CC(=NO2)C3=CC=C(C=C3)C(=O)NC4CC(C(NC(=O)C5C(C(CN5C(=O)C(NC(=O)C(NC(=O)C6CC(CN6C(=O)C(NC4=O)C(C)O)O)C(C(C7=CC(=C(C=C7)O)OS(=O)(=O)[O-])O)O)C(CC(=O)N)O)C)O)O)O.[Na+] | ||
| 分子式 | C56H70N9NaO23S | 分子量 | 1292.26 |
| 溶解度 | ≥ 64.66 mg/mL in DMSO, ≥ 17.5 mg/mL in Water with ultrasonic and warming | 储存条件 | 4°C, protect from light |
| 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 | 0.7738 mL | 3.8692 mL | 7.7384 mL |
| 5 mM | 0.1548 mL | 0.7738 mL | 1.5477 mL |
| 10 mM | 0.0774 mL | 0.3869 mL | 0.7738 mL |
| 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。
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Quality Control & SDS
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- Purity: >98.00%
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