Caspofungin Acetate
(Synonyms: 二醋酸卡泊芬净; MK-0991 diacetate; L-743872 diacetate) 目录号 : GC10303An echinocandin-type antifungal
Cas No.:179463-17-3
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1]: | |
Cell lines |
Aspergillus fumigates |
Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
32 μg/ml for 6 h; or 2 μg/ml for 12 h |
Applications |
Caspofungin suppressed the synthesis of cell wall β-1,3-glucan, which triggered a compensatory stimulation of chitin synthesis. Caspofungin induced morphological changes in Aspergillus fumigates. Moreover, Treatment with caspofungin induced ChsG-dependent upregulation of chitin synthesis and the formation of chitin-rich microcolonies in Aspergillus fumigates. |
References: 1Walker, L. A., Lee, K. K., Munro, C. A. and Gow, N. A. (2015) Caspofungin Treatment of Aspergillus fumigatus Results in ChsG-Dependent Upregulation of Chitin Synthesis and the Formation of Chitin-Rich Microcolonies. Antimicrob Agents Chemother. 59, 5932-5941 |
Caspofungin acetate(MK-0991), a new antifungal agent with minimal toxicity, inhibits synthesis of 1,3-β-D-glucan, an essential component of the fungal cell wall [1].
In vitro: Incubation ofA. fumigatuwith a single dose of caspofungin affected the same proportion of apical and subapical branching cells for up to 72 h.The cells at the active centers for new cell wall synthesis withinA. fumigateshyphae are killed when they are exposed to caspofungin [1]. Caspofungin acetate irreversibly inhibited the enzyme 1,3-β-D-glucan synthase, preventing the formation of glucan polymers and disrupting the integrity of the fungal cell wall. The elimination half-life of caspofungin acetate was 9-10 hours [2]. Caspofungin showed activity againstAspergillusspp. as well as a variety ofCandidaspp[3]. Growth kinetic studies of caspofungin acetate against Candida albicans and Candida tropicalis isolates showed that caspofungin acetate exhibited fungicidal activity (i.e., a 99% reduction in viability) within 3 to 7 h at concentrations ranging from 0.06 to 1 μg/ml (0.25 to 4 times the MIC)[4].The minimal inhibitory concentration for 90% inhibition of Candida species by caspofungin acetate were as follows:C. albicans 0.5 μg/mL (range, 0.25-0.5), C. glabrata 1.0 μg/mL (range, 0.25-2.0), C. tropicalis 1.0 μg/mL (range, 0.25-1.0), C. parapsilosis 0.5 μg/mL (range, 0.25-1.0), and C. krusei 2.0 μg/mL (range, 0.5-2.0)[4].
Clinical trials: In a trial of 128 patients with Candida esophagitis, clinical response rates were higher with caspofungin acetate 50 or 70 mg/day (85%) than with amphotericin B 0.5 mg/kg/day (67%)[2].
References:
[1]. Bowman J C, Hicks P S, Kurtz M B, et al. The antifungal echinocandincaspofungin acetate kills growing cells of Aspergillus fumigatus in vitro[J]. Antimicrobial agents and chemotherapy, 2002, 46(9): 3001-3012.
[2]. Hoang A. Caspofungin acetate: an antifungal agent[J]. American journal of health-system pharmacy, 2001, 58(13): 1206-1214.
[3]. Pacetti S A, Gelone S P. Caspofungin acetate for treatment of invasive fungal infections[J]. Annals of Pharmacotherapy, 2003, 37(1): 90-98.
[4]. Bartizal K, Gill C J, Abruzzo G K, et al. In vitro preclinical evaluation studies with the echinocandin antifungal MK-0991 (L-743,872)[J]. Antimicrobial Agents and Chemotherapy, 1997, 41(11): 2326-2332.
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 | |||
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。