描述
Caspofungin Acetate 醋酸卡泊芬净
(1,3-β-D-葡聚糖合成抑制剂)
产品关键词
Caspofungin Acetate 醋酸卡泊芬净；Anidulafungin 阿尼芬净;Micafungin Sodium 米卡芬净钠；echinocandin antifungal agents 抗真菌剂；1,3-β-D-葡聚糖合成抑制剂；CAS NO.166663-25-8；
产品信息
|
产品名称
|
产品编号 |
CAS NO. |
规格 |
价格（元） |
|
Caspofungin Acetate醋酸卡泊芬净
|
MS0087-5MG |
179463-17-3 |
5mg |
680 |
| Caspofungin Acetate醋酸卡泊芬净 |
MS0087-10MG |
179463-17-3 |
10mg |
1180
|
| Caspofungin Acetate醋酸卡泊芬净 |
MS0087-100MG |
179463-17-3 |
100mg |
3980
|
产品描述
醋酸卡泊芬净（Caspofungin Acetate），CAS NO.179463-17-3，最早分离自G. lozoyensis的一种棘白菌素类抗真菌剂，是纽莫康定 B0（Pneumocandin B0，Cat#：MS0112）的衍生物[1]。卡泊芬净有效作用于3959株临床分离的念珠菌（MIC90= 1 µg/ml），包括耐氟康唑或伊曲康唑的分离物；以及38株临床分离的曲霉，包括黄曲霉（A. flavus）、烟曲霉（A. fumigatus）、黑曲霉（A. niger）和土曲霉（A. Terreus）（MICs = <0.25-64 µg/ml）[2-3]。卡泊芬净抑制1,3-β-D-葡聚糖合成酶的活性（白色念珠菌膜制备物的IC50=0.6nM）[4]。播散性念珠菌病或曲霉菌病小鼠模型中，卡泊芬净提高存活率[5]。
产品特性
| 化学名：1-[(4R,5S)-5-[(2-aminoethyl)amino]-N2-[(10R,12S)-10,12-dimethyl-1-oxotetradecyl]-4-hydroxy-L- ornithine]-5-[(3R)-3-hydroxy-lornithine]-pneumocandin B0 acetate (1:2) |
| 同义名：Caspofungin diacetate; L-743,872;L-743872; MK 0991Acetate;卡泊芬净醋酸盐；醋酸卡铂芬净； |
| CAS NO：179463-17-3 |
分子式：C52H88N10O15·2(C2H4O2) |
| 分子量：1213.42 |
外观：固体 |
| 纯度：≥99% |
溶解性：溶于DMSO（≥25mg/ml）、H2O（≥10mg/ml）、不溶于乙醇 |
| 化学结构式： |
保存与运输方法
保存：-20ºC避光密封干燥保存，至少2年有效。
运输：常温运输。
注意事项
1） 为了让化合物更好的溶解，可通过37℃加热或（和）超声波水浴中震动片刻来处理。若实验所需浓度过大甚至达产品溶解极限，请添加助溶剂助溶或自行调整浓度。
2） 本品仅用作科研用途，不得用作临床诊断或治疗，不得用于食品或药品，绝对禁止用在人身上。
3） 为了您的安全和健康，请穿实验服并戴一次性手套操作。
储存液制备
| 质量
溶剂体积
浓度 |
1mg |
5mg |
10mg |
| 1mM |
0.8241 mL |
4.1206 mL |
8.2412 mL |
| 5mM |
0.1648 mL |
0.8241 mL |
1.6482 mL |
| 10mM |
0.0824 mL |
0.4121 mL |
0.8241 mL |
【温馨提示】：请根据实验需求选择合适的溶剂来配制储存液，一旦配成储存液，请分装保存，避免由于反复冻融造成的产品失效。储存液建议保存和周期如下：-80℃避光密封干燥保存，6个月内使用；-20℃，1个月内使用。
参考文献
[1] Letscher-Bru, V., and Herbrecht, R. Caspofungin: The first representative of a new antifungal class. J. Antimicrob. Chemother. 51(3), 513-521 (2003).
[2] Pfaller, M.A., Diekema, D.J., Messer, S.A., et al. In vitro activities of caspofungin compared with those of fluconazole and itraconazole against 3,959 clinical isolates of Candida spp., including 157 fluconazole-resistant isolate. Antimicrob. Agents Chemother. 47(3), 1068-1071 (2003).
[3] Perea, S., Gonzalez, G., Fothergill, A.W., et al. In vitro interaction of caspofungin acetate with voriconazole against clinical isolates of Aspergillus spp. Antimicrob. Agents Chemother. 46(9), 3039-3041 (2002).
[4] Deresinski, S.C., and Stevens, D.A. Caspofungin. Clin. Infect. Dis. 36(11), 1445-1457 (2003).
[5] Abruzzo, G.K., Flattery, A.M., Gill, C.J., et al. Evaluation of the echinocandin antifungal MK-0991 (L-743,872): Efficacies in mouse models of disseminated aspergillosis, candidiasis, and cryptococcosis. Antimicrob. Agents Chemother. 41(11), 2333-2338 (1997).
使用方法【源自文献，仅作参考】
| 文献1，Sumiyoshi, M., Miyazaki, T., Makau, J.N. et al. Novel and potent antimicrobial effects of caspofungin on drug-resistant Candida and bacteria. Sci Rep 10, 17745 (2020). https://doi.org/10.1038/s41598-020-74749-8
体外研究（细胞水平）：
细胞类型（Cell Type）：C. albicans and C. auris biofilm cells
配制方法（Formulation）：Caspofungin dissolved in 5% glucose water
实验方法（Assay）：For antifungal treatment, 100 μL of antifungal solutions (caspofungin, micafungin, and amphotericin B dissolved in 5% glucose water, 0.9% NaCl, and RPMI-1640, respectively) were added to each well and incubated at 37 °C for 5 min, 30 min, or 60 min. A maximum concentration was selected for each drug according to the clinical dose indicated for fungal infections: 500 mg/L for caspofungin (50 mg/body weight diluted with 100 mL or 250 mL solution); |
| 文献2，Flattery AM, Hickey E, Gill CJ, Powles MA, Misura AS, Galgoci AM, Ellis JD, Zhang R, Sandhu P, Ronan J, Abruzzo GK. Efficacy of caspofungin in a juvenile mouse model of central nervous system candidiasis. Antimicrob Agents Chemother. 2011 Jul;55(7):3491-7.Epub 2011 Apr 25. PMID: 21518846;
体内研究（动物模型）：
动物模型（Animal Model）：Juvenile DBA/2N mice infected with Candida albicans MY1055
配制方法（Formulation）：Caspofungin acetate was solubilized and serially diluted in sterile distilled water.
实验方法（Assay）：Antifungal therapy was initiated at 30 h after infectious challenge andwas given by intraperitoneal (i.p.) injection once daily for 7 days. Mice were treated with caspofungin at 1, 2, 4, or 8 mg/kg/day, amphotericin B at 1 mg/kg/day, or vehicle control (VC; sterile distilled water). |
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