Dup-721
目录号 : GC62945
DuP-721 是一种广谱口服活性抗菌剂 (antibacterial agent)，对多种临床敏感和耐药细菌有效，特别是结核杆菌 M. tuberculosis。
Cas No.:104421-21-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
DuP-721 is a broad spectrum and orally active antibacterial agent against a variety of clinically susceptible and resistant bacteria, especially M. tuberculosis[1].
DuP-721 (1.5-4 μg/ml) inhibits equally the strains of Mycobacterium tuberculosis susceptible and resistant to conventional antituberculosis drug. And it does not show cross resistance to any of the anti-tuberculosis drugs tested[1].DuP-721 is inactive against M. avium and M. intracellulare at 250 μg/ml. It inhibits M. gordonoe and M. fortuitum at 3.9 μg/ml and M. kansassi and M. scrofulaceum at 1.95 μg/ml and 15.6 μg/ml, respectively[1].
DuP-721 (oral gavage; 50-160 mg/kg) is protective against M. tuberculosis infection in mice. DuP-721 protects 100% of the infected animals at 50 mg/kg p.o. dose when administered daily for 17 days, and the same effect is observed at 160 mg/kg dose when the drug is administered only on day 11 and 12 post infection[1].
[1]. Affiliatio, et al. Antimycobacterial activities of oxazolidinones: a review. Infect Disord Drug Targets. 2006 Dec;6(4):343-54.
| Cas No. | 104421-21-8 | SDF | |
| 分子式 | C14H16N2O4 | 分子量 | 276.29 |
| 溶解度 | DMSO : 100 mg/mL (361.94 mM; Need ultrasonic) | 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。 |
||
| 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 | 3.6194 mL | 18.0969 mL | 36.1939 mL |
| 5 mM | 0.7239 mL | 3.6194 mL | 7.2388 mL |
| 10 mM | 0.3619 mL | 1.8097 mL | 3.6194 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。
Oxazolidinones, a new class of synthetic antituberculosis agent. In vitro and in vivo activities of Dup-721 against Mycobacterium tuberculosis
Diagn Microbiol Infect Dis 1991 Nov-Dec;14(6):465-71.PMID:1802533DOI:10.1016/0732-8893(91)90002-w.
DL-S-n-(3-(4-acetyl)-2-oxo-5-oxazolidynyl methyl) acetamide (Dup-721) is an orally active representative of the oxazolidinone series of antimicrobials. At concentrations ranging from 1.5 to 4 micrograms/ml, Dup-721 inhibited equally the strains of Mycobacterium tuberculosis susceptible and resistant to conventional antituberculosis drugs. Dup-721 inhibited M. gordonae and M. fortuitum at 3.9 micrograms/ml, M. kansasii at 1.95, and M. scrofulaceum at 15.6 micrograms/ml. It was not active against M. avium and M. intracellulare at concentrations of 250 micrograms/ml. The inhibition of the metabolism of M. tuberculosis as indicated by the liquid scintillation radiometric method was 56% at fourfold the minimum inhibitory concentration (MIC) of Dup-721 that compared well to that of the fourfold MIC concentrations of rifampicin and isoniazid. The in vitro activity of Dup-721 was not affected by reducing the pH from 6.8 to 5.5. In mice infected with M. tuberculosis, the 50% effective dose (ED50) for Dup-721 was 13.2 mg/kg when administered daily beginning 4 hr postinfection for 17 days. The ED50 was 71.8 mg/kg when Dup-721 was administered only on days 11 and 12 postinfection. A 100% survival rate was obtained at 50 and 160 mg/kg when Dup-721 was administered daily for 17 days, and only on days 11 and 12 after the infection, respectively. The increase in the survival time by Dup-721 at 100 mg/kg (eightfold the ED50 dose) when administered daily for 17 days beginning 4 hr after infection was inferior to that by eightfold the ED50 dose of rifampicin and isoniazid administered on days 11 and 12 postinfection.(ABSTRACT TRUNCATED AT 250 WORDS)
Oxazolidinones as Anti-tubercular Agents: Discovery, Development and Future Perspectives
Curr Med Chem 2015;22(38):4379-97.PMID:26549430DOI:10.2174/0929867323666151106125759.
TB drug development pipeline represents varied structural classes of molecules. Oxazolidinones represent synthetic anti-bacterial agents with unique mechanism of action having wide spectrum of activity, oral bioavailability and well established SAR. They act by inhibiting translation at the initiation phase of protein synthesis. Linezolid was the first oxazolidinone to reach the market in the year 2000 for the treatment of methicillin-resistant staphylococcal and vancomycin-resistant enterococcal infections. Oxazolidinones have shown very good anti-mycobacterial activities. Several oxazolidinones are currently in development for their possible use in TB therapy. Oxazolidinones are classified on the basis of C-ring modifications. Dup-721 was the first oxazolidinone having good anti-TB activity. Linezolid, sutezolid and AZD5847 are in clinical development. Several other C-ring modifications have shown promising results. The usefulness of these oxazolidinones in the drug resistant TB is already established. Toxicity, especially myelosuppression, has been an important limiting factor for their development.
Antimycobacterial activities of oxazolidinones: a review
Infect Disord Drug Targets 2006 Dec;6(4):343-54.PMID:17168800DOI:10.2174/187152606779025860.
Oxazolidinones are a new class of totally synthetic antibacterial agents with wide spectrum of activity against a variety of clinically significant susceptible and resistant bacteria. These compounds have been shown to inhibit translation at the initiation phase of protein synthesis. Dup-721, the first oxazolidinone showed good activity against M. tuberculosis when given orally or parenterally to experimental animals but was not developed further due to lethal toxicity in animal models. Later two oxazolidinones, PNU-100480 and Linezolid, demonstrated promising antimycobacterial activities in the murine model. While Linezolid has been approved for clinical use, PNU-100480 was not been developed further. DA-7867 showed good in vitro and better in vivo efficacy than Linezolid but was poorly tolerated in rat toxicology studies. The antimycobacterial activity of AZD-2563 has not been explored. RBx 7644 had modest antimycobacterial activity while RBx 8700 has potent antibacterial and concentration dependent activity against all slow growing mycobacteria. It demonstrated better activity than RBx 7644 against MDR strains of M. tuberculosis along with intracellular activity. Toxicity, especially myelosuppression, has been an important limiting factor for development of an oxazolidinones. The GM-CSF assay has helped in selecting molecules with less myleosuppressive potential. We report, a review on the promising antituberculosis activities of the class oxazolidinones.