Caspofungin (Acetate) 醋酸卡泊芬净
货号：
IC0130
品牌：
Jinpan
暂无详情
产品简介
| MDL | MFCD08141839 |
| EC | EINECS 605-859-0 |
| 别名 | Cancidas; Caspofungin Diacetate |
| CAS | 179463-17-3 |
| 分子式 | C56H96N10O19 |
| 分子量 | 1213.42 |
| 纯度 | ≥98% |
| 单位 | 瓶 |
| 生物活性 | Caspofungin Acetate 是一种抗真菌药，能够非竞争性地抑制1，3-β-d葡聚糖合酶的合成。[1-2] |
| In Vivo | 注射卡泊芬净的小鼠在0.41至4.1μM的玻璃体浓度下，其ERG波形没有显著改变，并且它们的视网膜没有可检测的形态变化或细胞损失。在41μM的玻璃体浓度下，卡泊芬净降低了ERG的a波，b波和暗视阈值响应的幅度，并且还导致神经节细胞层中细胞数量的减少[1]。卡普芬净（8 mg/kg）或两性霉素B 1 mg/kg，感染后30 h每天一次腹膜内注射，连续7天，相对于媒介物对照治疗，第28天100％存活，导致白天100％死亡率11，传染性挑战后。与第5天的媒介物对照治疗相比，当控制负荷达到峰值时，卡泊芬净降低了肾和脑组织中存活念珠菌的恢复。给予2mg/kg或更高剂量的卡泊芬净治疗的小鼠在第5天具有比两性霉素B治疗的小鼠显著更低的脑负荷。两性霉素B和卡泊芬净治疗使肾脏真菌负荷减少1.7log CFU/g和2.46至3.64log CFU/g，分别为[2]。 |
| SMILES | OC1=CC=C(C=C1)[C@H]([C@@H]([C@@H]2NC([C@@H]3C[C@H](CN3C([C@H]([C@H](O)C)NC([C@H](C[C@H]([C@@H](NCCN)NC([C@@H]4[C@H](CCN4C([C@H]([C@H](O)CCN)NC2=O)=O)O)=O)O)NC(CCCCCCCCC(CC(CC)C)C)=O)=O)=O)O)=O)O)O.OC(C)=O.OC(C)=O |
| 靶点 | Fungal |
| 动物实验 | Antifungal therapy is initiated at 30 h after infectious challenge and is given by intraperitoneal (i.p.) injection once daily for 7 days. Mice are treated with caspofungin at 1, 2, 4, or 8 mg/kg/day, amphotericin B at 1 mg/kg/day, or vehicle control (sterile distilled water). Efficacy in this model is assessed in 3 ways: by monitoring survival in a group of 10 animals in each treatment group, by monitoring Candida burden in kidney and brain tissues in a second set of treated animals, and by histologically evaluating the kidneys and brains in a third set of treated animals. Mice are euthanized by CO2 inhalation, and tissues for both culture and histology are sampled at 30 h (vehicle-treated control only) and at days 5 (24 h after 4th dose), 8 (24 h after last dose), 14, 21 (caspofungin-treated only), and 28 after challenge.[2] |
| 数据来源文献 | [1]. Mojumder DK, et al. Evaluating retinal toxicity of intravitreal caspofungin in the mouse eye. Invest Ophthalmol Vis Sci. 2010 Nov;51(11):5796-803. [2]. Flattery, Amy M. et al. Efficacy of caspofungin in a juvenile mouse model of central nervous system candidiasis. Antimicrobial Agents and Chemotherapy (2011), 55(7), 3491-3497. |
| 规格 | 5mg 10mg 10mM*1mL (in Water) 10mM*1mL in DMSO 20mg |
能够非竞争性地抑制1，3-β-d葡聚糖合酶的合成。