Caspofungin-Acetate-L-743872-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECaspofungin AcetateCat. No.: HY-17006CAS No.: 179463-17-3Synonyms: L 743872; L 743873; MK 0991分式: CHNO分量: 1213.42作靶点: Fungal作通路: Anti-infection储存式: -70C* 该产品在溶液状态不稳定，建议您现现配，即刻使。溶解性数据体外实验 H2O : 100 mg/mL (82.41 mM)DMSO : 83.3 mg/

2、mL (68.65 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 0.8241 mL 4.1206 mL 8.2412 mL5 mM 0.1648 mL 0.8241 mL 1.6482 mL10 mM 0.0824 mL 0.4121 mL 0.8241 mL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；该产品在溶液状态不稳定，建议您现现配，即刻使。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助

3、溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (1.71 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (1.71 mM); Clear solution1/3 Master of Smal

4、l Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (1.71 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Caspofungin Acetate种抗真 药，能够竞争性地抑制1，3-d葡聚糖合酶的合成。体内研究 Mice injected with caspofungin at vitreal concentrations from 0.41 to 4.1 M do not have significantalterations

5、in their ERG waveforms, and their retinas have no detectable morphologic changes or loss ofcells. At the vitreal concentration of 41 M, caspofungin reduces the amplitudes of the a-waves, b-waves,and scotopic threshold responses of the ERG and also produces a decrease in the number of cells in thegan

6、glion cell layer 1. Caspofungin (8 mg/kg) or amphotericin B at 1 mg/kg given i.p. once daily for 7 daysbeginning at 30 h after infection resulted in 100% survival through day 28 relative to vehicle controltreatment, which results in 100% mortality by day 11 after infectious challenge. Caspofungin re

7、ducesrecovery of viable Candida from kidney and brain tissues compared to vehicle control treatment on day 5,when control burden peaked. Caspofungin-treated mice dosed with 2 mg/kg or greater have significantlylower brain burden than amphotericin-B-treated mice at day 5. Amphotericin B and caspofung

8、in treatmentreduce kidney fungal burden by 1.7 log CFU/g and 2.46 to 3.64 log CFU/g, respectively 2.PROTOCOLAnimal Antifungal therapy is initiated at 30 h after infectious challenge and is given by intraperitoneal (i.p.) injectionAdministration 2 once daily for 7 days. Mice are treated with caspofun

9、gin at 1, 2, 4, or 8 mg/kg/day, amphotericin B at 1mg/kg/day, or vehicle control (sterile distilled water). Efficacy in this model is assessed in 3 ways: bymonitoring survival in a group of 10 animals in each treatment group, by monitoring Candida burden in kidneyand brain tissues in a second set of

10、 treated animals, and by histologically evaluating the kidneys and brainsin a third set of treated animals. Mice are euthanized by CO2 inhalation, and tissues for both culture andhistology are sampled at 30 h (vehicle-treated control only) and at days 5 (24 h after 4th dose), 8 (24 h afterlast dose)

11、, 14, 21 (caspofungin-treated only), and 28 after challenge.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Cell Physiol Biochem. 2016 Aug 12;39(3):939-949.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Mojumder DK, et

12、 al. Evaluating retinal toxicity of intravitreal caspofungin in the mouse eye. Invest Ophthalmol Vis Sci. 2010Nov;51(11):5796-803.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE2. Flattery, Amy M. et al. Efficacy of caspofungin in a juvenile mouse model of central nervous system candidiasis. Antimicrobial Agentsand Chemotherapy (2011), 55(7), 3491-3497.McePdfHeightCaution