Daptomycin 是一种脂肽类抗生素，具有体外快速杀除革兰氏阳性细菌的活性。

储备液保存：

-80°C, 1 years

-20°C, 6 months

体内实验：

1、请依序添加每种溶剂： PBS

Solubility: 100 mg/mL (61.70 mM); Clear solution; Need ultrasonic

2、请依序添加每种溶剂： 10% DMSO→40% PEG300→5% Tween-80→45% saline

Solubility: ≥ 2.08 mg/mL (1.28 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (1.28 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

3、请依序添加每种溶剂： 10% DMSO→90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.08 mg/mL (1.28 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (1.28 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

4、请依序添加每种溶剂： 10% DMSO→90% corn oil

Solubility: ≥ 2.08 mg/mL (1.28 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (1.28 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

＜1mg/ml表示微溶或不溶。

提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。

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。

体外研究：

Daptomycin has excellent in-vitro inhibitory and bactericidal activity against nafcillin-susceptible and resistant

staphylococci (MIC90 less than or equal to 0.5 mg/L) and against enterococci (MIC90 less than or equal to 2.0 mg/L). Daptomycin is more active than vancomycin against the majority of isolated tested. With the exception of trimethoprim-sulphamethoxazole, daptomycin is the most active agent in vitro against enterococci, and is the most active against nafcillin-resistant staphylococci. Daptomycin and vancomycin show a marked increase in MIC when the inoculum is increased from 105 to 107 cfu/mL. Daptomycin is effective within a very narrow range of drug concentrations (from 0.125 to 2.0 tLg/mL) and is more active than other agents tested against S. faecalis. Daptomycin inhibits the formation of these nucleotide-linked intermediates.

体内研究：

At a dose of 10 mg/kg given twice daily, daptomycin reduces the number of organisms per kidney significantly compared with that in infected untreated controls within 48 h after the initiation of therapy. At 20 mg/kg given once a day, daptomycin is less effective but reduces colony counts significantly after 4 days of therapy, and its activity is comparable to that of vancomycin or vancomycin-gentamicin given twice daily.

动物实验：

动物模型：ICR/Swiss小鼠

剂量：0, 1, 2.5, 5, 10, 15 或 20 mg/kg

给药处理：i.p.