Dalfopristin (mesylate)
(Synonyms: RP 54476) 目录号 : GC14837
A streptogramin antibiotic
Sample solution is provided at 25 µL, 10mM.
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Dalfopristin (mesylate) is a streptogramin antibiotic and a 50S ribosome inhibitor [1][2].
Streptogramins are produced by a variety of Streptomyces sp as a mixture (ratio of 7:3) of two chemically unrelated compounds, type A and B. Dalfopristin, the type A Streptogramin, is often combined with type B streptogramin antibiotic, quinupristin, to produce Quinupristin-Dalfopristin Complex, known commercially as Synercid. Synercid is used to treat skin infections, and is also active against some Gram-negative and anaerobic bacteria [2][3].
The ribosome is composed of two ribonucleoprotein subunits, the 50S and 30S. The 50S ribosome inhibitors inhibited protein synthesis [2].
Dalfopristin is a cyclic polyunsaturated macrolactone that interferes with binding of tRNA substrates to both A- and P-sites [2]. Dalfopristin blocked the access of peptidyl-tRNAs to the ribosome and peptidyltransferase elongation reaction in bacteria [1]. quinupristin and dalfopristin acted synergistically to kill Gram-positive bacteria, as well as some Gram-negative and anaerobic bacteria [2][3]. Dalfopristin hydrolyzed rapidly to virginiamycin M under physiological conditions.
References:
[1]. Kohanski MA, Dwyer DJ, Collins JJ. How antibiotics kill bacteria: from targets to networks. Nat Rev Microbiol. 2010 Jun;8(6):423-35.
[2]. Wilson DN. The A-Z of bacterial translation inhibitors. Crit Rev Biochem Mol Biol. 2009 Nov-Dec;44(6):393-433.
[3]. Noeske J, Huang J, Olivier NB, et al. Synergy of streptogramin antibiotics occurs independently of their effects on translation. Antimicrob Agents Chemother. 2014 Sep;58(9):5269-79.
| Cas No. | SDF | ||
| 别名 | RP 54476 | ||
| 化学名 | (3R,4R,5E,10E,12E,14S,26R,26aS)-26-[[2-(diethylamino)ethyl]sulfonyl]-8,9,14,15,24,25,26,26a-octahydro-14-hydroxy-4,12-dimethyl-3-(1-methylethyl)-3H-21,18-nitrilo-1H,22H-pyrrolo[2,1-c][1,8,4,19]dioxadiazacyclotetracosine-1,7,16,22(4H,17H)-tetrone, monometh | ||
| Canonical SMILES | O=C(/C=C/[C@@H](C)[C@@H](C(C)C)OC(C1N(CC[C@H]1S(CC[NH+](CC)CC)(=O)=O)C(C2=COC(C3)=N2)=O)=O)NC/C=C\C(C)=C\[C@@H](O)CC3=O.CS([O-])(=O)=O | ||
| 分子式 | C34H51N4O9S • CH3SO3 | 分子量 | 787.0 |
| 溶解度 | Soluble in ethanol;methanol;DMSO;dimethyl formamide | 储存条件 | Store at -20°C |
| 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 | 1.2706 mL | 6.3532 mL | 12.7065 mL |
| 5 mM | 0.2541 mL | 1.2706 mL | 2.5413 mL |
| 10 mM | 0.1271 mL | 0.6353 mL | 1.2706 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet