Caspofungin Acetate
(Synonyms: 二醋酸卡泊芬净; MK-0991 diacetate; L-743872 diacetate) 目录号 : GC10303
Caspofungin Acetate是棘白菌素（echinocandins）成员，是一种通过抑制真菌细胞壁β(1,3)- d -葡聚糖合成酶而靶向曲霉和念珠菌的脂肽类抗真菌化合物。
Cas No.:179463-17-3
Sample solution is provided at 25 µL, 10mM.
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Caspofungin Acetate, a member of echinocandins, is a lipopeptide anti-fungal compound targeting Aspergillus and Candida by inhibiting β(1,3)-D-Glucan synthase of the fungal cell wall[1]. Caspofungin Acetate has both fungistatic and fungicidal effects by inhibiting the synthesis of β(1,3)-D-glucan in a non-competitive manner, suppressing the proliferation of fungus and causing cell destruction[2]. Caspofungin Acetate has been approved as an anti-fungal drug named Cancidas by the FDA(2001, USA), EMA(2001, EU), and PMDA (2012, Japan)[2].
In vitro, Caspofungin Acetate kills growing cells of Aspergillus fumigatus (0.2 μg/ml; 15h)[1], and against Candida auris planktonic cells and biofilms (0.03 to 2mg/L; 48h)[3]. Caspofungin Acetate-induced β(1,3)-glucan exposure in Candida albicans is driven by increased chitin levels (46.9ng/mL; 30min)[4]. Caspofungin Acetate is also widely tested combined with other compounds such as voriconazole (0.03-4μg/ml)[5] and fluconazole(0.25 or 0.5MIC)[6].
In vivo, the Caspofungin Acetate activity against Candida glabrata biofilms (10mg/kg; i.p) is tested by bioluminescence imaging in BALB/c mice[7], and in vivo efficiency of Caspofungin Acetat is also tested (3mg/kg; i.p) in a neutropenic mouse bloodstream infection model[8].
References:
[1] Bowman, J C et al. “The antifungal echinocandin caspofungin acetate kills growing cells of Aspergillus fumigatus in vitro.” *Antimicrobial agents and chemotherapy* vol. 46,9 (2002): 3001-12. doi:10.1128/AAC.46.9.3001-3012.2002
[2] Hashemian SM, Farhadi T, Velayati AA. Caspofungin: a review of its characteristics, activity, and use in intensive care units. Expert Rev Anti Infect Ther. 2020 Dec;18(12):1213-1220. doi: 10.1080/14787210.2020.1794817. Epub 2020 Jul 23. PMID: 32662712.
[3] Nagy, Fruzsina et al. “In vitro and in vivo interaction of caspofungin with isavuconazole against Candida auris planktonic cells and biofilms.” *Medical mycology*vol. 59,10 (2021): 1015-1023. doi:10.1093/mmy/myab032
[4] Wagner, Andrew S et al. “Caspofungin-induced β(1,3)-glucan exposure in *Candida albicans* is driven by increased chitin levels.” *mBio* vol. 14,4 (2023): e0007423. doi:10.1128/mbio.00074-23
[5] Perea, Sofia et al. “In vitro interaction of caspofungin acetate with voriconazole against clinical isolates of Aspergillus spp.” *Antimicrobial agents and chemotherapy* vol. 46,9 (2002): 3039-41. doi:10.1128/AAC.46.9.3039-3041.2002
[6] Pesee, Siripen et al. “In vitro activity of Caspofungin combined with Fluconazole on mixed Candida albicans and Candida glabrata biofilm.” *Medical mycology* vol. 54,4 (2016): 384-93. doi:10.1093/mmy/myv108
[7] Persyn, Aranka et al. “Monitoring of Fluconazole and Caspofungin Activity against *In Vivo* Candida glabrata Biofilms by Bioluminescence Imaging.” *Antimicrobial agents and chemotherapy* vol. 63,2 e01555-18. 29 Jan. 2019, doi:10.1128/AAC.01555-18
Balázsi, Dávid et al. “In Vivo Efficacy of Rezafungin, Anidulafungin, Caspofungin, and Micafungin against Four *Candida auris* Clades in a Neutropenic Mouse Bloodstream Infection Model.” *Journal of fungi (Basel, Switzerland)* vol. 10,9 617. 29 Aug. 2024, doi:10.3390/jof10090617
Caspofungin Acetate是棘白菌素（echinocandins）成员，是一种通过抑制真菌细胞壁β(1,3)- d -葡聚糖合成酶而靶向曲霉和念珠菌的脂肽类抗真菌化合物[1]。Caspofungin Acetate通过非竞争方式抑制β(1,3)- d -葡聚糖的合成，抑制真菌的增殖并引起细胞破坏，具有抑菌和杀真菌双重作用[2]。Caspofungin Acetate（商品名Cancidas）已被FDA（2001年，美国）、EMA（2001年，欧盟）和PMDA（2012年，日本）批准为抗真菌药物[2]。
体外实验中，Caspofungin Acetate对Aspergillus fumigatus（0.2μg/ml; 15h）具有杀伤作用[1]，对Candida auris细胞和生物膜（0.03~2 mg/L; 48h）具有杀伤作用[3]。Caspofungin Acetate诱导的β(1,3)-葡聚糖暴露在白色念珠菌中是由几丁质水平升高（46.9 ng/mL; 30min）引起的[4]。Caspofungin Acetate也广泛与伏立康唑（0.03~4μg/ml）[5]和氟康唑（0.25~0.5MIC）[6]等其它化合物联合试验。
在体内实验中，通过生物发光成像检测Caspofungin Acetate对光念珠菌生物膜（10 mg/kg; i.p）的活性[7]，并在中性粒细胞减少小鼠血流感染模型中检测Caspofungin Acetate（3mg/kg; i.p）的体内效率[8]。
| in vitro experiment [1]: | |
Targets | Aspergillus fumigatus and C. albicans |
Preparation Method | Several colonies of C. albicans strain MY1055 were inoculated from YPAD plates into 20ml of buffered RPMI 1640 medium and grown to saturation (ca. 40h) at 37°C with shaking (220rpm). The cells were subcultured to an initial A600 of 0.002 in 65 ml of fresh medium, and incubation was continued until the cultures reached a density of 1×106 to 2×106 cells/ml (determined by counting with a hemocytometer; ca. 9h). Aliquots were removed, serially diluted in buffered RPMI 1640 medium, and spread onto SDA plates (BBL) to determine the number of CFU per milliliter. Caspofungin Acetate（AMB, or FLC) or vehicle was added, and incubation was continued for 15h. |
Reaction Conditions | 0.2μg/ml; 15h |
Applications | The dye-staining patterns illustrate that the cells at the active centers for new cell wall synthesis within A. fumigatus hyphae are killed when they are exposed to caspofungin. |
| Animal experiment [2]: | |
Animal models | BALB/c male mice (23–25g) |
Preparation Method | The mice (groups of 10mice/isolate) were intravenously infected through the lateral tail vein (day0). The infectious dose was 107 colony-forming units (CFU)/mouse, administered in volumes of 0.2mL. Beginning at 24h post-infection, the mice received once-daily treatment for 6days with 3mg/kg of Caspofungin Acetate. |
Dosage form | 3mg/kg; i.p |
Applications | Histopathological examination performed on day 7 showed no fungal cells in the heart and kidneys of rezafungin-treated mice and to a lesser extent, Caspofungin Acetate-treated mice, regardless of the clinical isolate. All echinocandin-treated mice showed medium and/or large foci of fungal cells in their cerebrum or cerebellum. |
References: | |
| Cas No. | 179463-17-3 | SDF | |
| 别名 | 二醋酸卡泊芬净; MK-0991 diacetate; L-743872 diacetate | ||
| 化学名 | acetic acid compound with (Z)-N-((2R,6S,7Z,9S,11R,12S,13E,14aS,15S,20S,21Z,23S,24Z,25aS)-20-((R)-3-amino-1-hydroxypropyl)-12-((2-aminoethyl)amino)-23-((1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl)-2,8,11,14,15,22,25-heptahydroxy-6-((R)-1-hydroxyethyl)-5 | ||
| Canonical SMILES | CCC(C)CC(C)CCCCCCCCC(=O)NC1CC(C(NC(=O)C2C(CCN2C(=O)C(NC(=O)C(NC(=O)C3CC(CN3C(=O)C(NC1=O)C(C)O)O)C(C(C4=CC=C(C=C4)O)O)O)C(CCN)O)O)NCCN)O.CC(=O)O.CC(=O)O | ||
| 分子式 | C56H96N10O19 | 分子量 | 1213.42 |
| 溶解度 | ≥ 60.671mg/mL in DMSO | 储存条件 | Store at -20°C, sealed storage, away from moisture and 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 | 0.8241 mL | 4.1206 mL | 8.2412 mL |
| 5 mM | 0.1648 mL | 0.8241 mL | 1.6482 mL |
| 10 mM | 0.0824 mL | 0.4121 mL | 0.8241 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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- Purity: >98.00%
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