DuP 105
目录号 : GC32267
DuP105是一种可口服的恶唑烷酮类化合物，能够抗葛兰素阳性菌。
Cas No.:96800-41-8
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
|
Animal experiment: |
The mice are made neutropenic by the intraperitoneal administration of 100 mg of cyclophosphamide per kg on days -5, -3, and 0 (the day of infection). The extent of immunosuppression is assessed by using a standard hematological technique to determine leukocyte counts. In all experiments, the leukocyte count in the cyclophosphamide-treated mice is less than 15% of that in nontreated mice from day 0 through day 7. On day 0, the mice are injected intraperitoneally with a bacterial inoculum suspended in 0.2 mL of saline containing 5% gastric porcine mucin. This inoculum (2×104 CFU) is fivefold that required to kill all the nontreated immunosuppressed mice in 48 h. Graded doses of the test compounds are administered by the subcutaneous or oral route at 1 and 4 h after infection. In parallel with the immunosuppressed mice, groups of nonimmunosuppressed mice are infected, and treated with the antibacterial drugs. The number of survivors on day 7 in each group is used to calculate the ED50 values of the test compounds. |
|
References: [1]. Slee AM, et al. Oxazolidinones, a new class of synthetic antibacterial agents: in vitro and in vivo activities of DuP 105 and DuP 721. Antimicrob Agents Chemother. 1987 Nov;31(11):1791-7. |
|
DuP 105 is an orally active oxazolidinone, a new class of synthetic antimicrobial agent with activity against gram-positive bacteria.
DuP 105 shows inhibitory activities against staphylococcal isolates and B. fragilis isolates with MIC90s of 4 to 16 μg/mL and 16 μg/mL[1]. DuP 105 MICs for 50% of the 216 gram-positive isolates tested (MIC50s) range from 4.0 to 16 μg/mL[2].
DuP 105 administered by either the oral or the parenteral route is protective against staphylococcal and streptococcal infections in mice with the 50% effective doses of 9 to 23 mg/kg[1].
[1]. Slee AM, et al. Oxazolidinones, a new class of synthetic antibacterial agents: in vitro and in vivo activities of DuP 105 and DuP 721. Antimicrob Agents Chemother. 1987 Nov;31(11):1791-7. [2]. Barry AL, et al. In vitro evaluation of DuP 105 and DuP 721, two new oxazolidinone antimicrobial agents. Antimicrob Agents Chemother. 1988 Jan;32(1):150-2.
| Cas No. | 96800-41-8 | SDF | |
| Canonical SMILES | CC(NC[C@H]1CN(C2=CC=C(S(C)=O)C=C2)C(O1)=O)=O | ||
| 分子式 | C13H16N2O4S | 分子量 | 296.34 |
| 溶解度 | Soluble in DMSO | 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 | 3.3745 mL | 16.8725 mL | 33.745 mL |
| 5 mM | 0.6749 mL | 3.3745 mL | 6.749 mL |
| 10 mM | 0.3375 mL | 1.6873 mL | 3.3745 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。
In-vitro microbiological activities of DuP 105 and DuP 721, novel synthetic oxazolidinones
J Antimicrob Chemother 1988 Jun;21(6):711-20.PMID:3137206DOI:10.1093/jac/21.6.711.
DuP 105 and 721, synthetic antibiotics belonging to a totally novel chemical class (oxazolidinones), have been found to be active in vitro against a wide range of Gram-positive bacteria, including methicillin-resistant Staphylococcus aureus. DuP 721 had geometric mean MICs ranging from 1.1 to 16 mg/l against 167 strains of Staph. aureus, Staph. epidermidis, Staph. saprophyticus, streptococci of Groups A, B and D and diphtheroids. DuP 105 was between 1.5 and eight-fold less active. Bacteroides fragilis strains were also susceptible to the DuP compounds (mean MICs being 8.3 and 14.9 mg/l for DuP 721 and 105, respectively), but other Gram-negative species and yeasts were not inhibited by concentrations in excess of 100 mg/l. Both compounds had a predominantly bacteriostatic action. No primary resistance was found, and the incidence of resistant variants in 105 strains tested was less than 1 per 10(8) bacteria.
Activity and mechanism of action of DuP 105 and DuP 721, new oxazolidinone compounds
J Antimicrob Chemother 1988 Jun;21(6):721-30.PMID:3410799DOI:10.1093/jac/21.6.721.
The in-vitro activities of DuP 721 and DuP 105, new oxazolidinone antibacterials, were compared with those of cefazolin, cephalexin, ciprofloxacin, clindamycin, oxacillin, penicillin, and vancomycin against Gram-positive cocci. DuP 721 was approximately four-fold more active than DuP 105 with an MIC of 2.0 mg/l for 90% of the Staphylococcus aureus, beta-haemolytic streptococcus and Streptococcus faecalis strains tested, and an MIC of 4.0 mg/l for 90% of the Str. faecium, penicillin-resistant Str. pneumoniae and viridans streptococcus strains tested. DuP 105 was most active against strains of Staph. epidermidis with an MIC of 4.0 mg/l for 90% of the strains tested. There was no cross resistance between these and the other antibacterial agents that were tested. Both oxazolidinones had bacteriostatic activity in broth against susceptible organisms. Both DuP 721 and DuP 105 inhibited ribosomal protein synthesis in a cell-free system. These synthetic, orally absorbable compounds represent a new series of antibacterial agents unrelated by chemical structure to any other currently available antimicrobial agents.
Oxazolidinones, a new class of synthetic antibacterial agents: in vitro and in vivo activities of DuP 105 and DuP 721
Antimicrob Agents Chemother 1987 Nov;31(11):1791-7.PMID:3435127DOI:10.1128/AAC.31.11.1791.
DuP 721 (p-acetylphenyloxooxazolidinylmethylacetamide) and DuP 105 (a methylsulfinyl derivative) are orally active representatives of the oxazolidinones, a new class of synthetic antibacterial agents. Their antibacterial spectrum includes staphylococci, streptococci, and Bacteroides fragilis strains. The compounds have equal activity against staphylococcal strains susceptible or resistant to beta-lactam antibiotics, including methicillin-resistant strains. The MICs for 90% of the strains (MIC90s) against staphylococcal isolates were 1 to 4 micrograms/ml for DuP 721 and 4 to 16 micrograms/ml for DuP 105, compared with 1 to 2 micrograms/ml for vancomycin, 0.5 microgram/ml for ciprofloxacin, and 2 to greater than 16 micrograms/ml for imipenem. The MIC90s against group D streptococci were 4 micrograms/ml for DuP 721, 16 micrograms/ml for DuP 105, and 2 micrograms/ml for vancomycin, ciprofloxacin, and imipenem. MIC90s against B. fragilis isolates were 4 micrograms/ml for DuP 721, 16 micrograms/ml for DuP 105, and 8 micrograms/ml for cefoxitin. DuP 721 and DuP 105 administered by either the oral or the parenteral route were protective against staphylococcal and streptococcal infections in mice. The 50% effective doses were 2 to 10 mg/kg for DuP 721, 9 to 23 mg/kg for DuP 105, and 2 to 12 mg/kg for vancomycin. These results indicate that further studies of compounds of the oxazolidinone series are warranted.
In vitro activities of two oxazolidinone antimicrobial agents, DuP 721 and DuP 105
Antimicrob Agents Chemother 1988 Apr;32(4):580-3.PMID:3377467DOI:10.1128/AAC.32.4.580.
The antibacterial activities of DuP 105 and DuP 721, new oxazolidinone antimicrobial agents, were compared with those of beta-lactams and glycopeptides. Ninety percent of Staphylococcus aureus and Staphylococcus epidermidis isolates, including methicillin-resistant isolates, were inhibited by 4 micrograms of DuP 105 and 1 microgram of DuP 721 per ml. DuP 721 inhibited hemolytic streptococcus groups A, B, C, F, and G at a concentration of less than or equal to 1 microgram/ml, and it inhibited viridans group streptococci at a concentration of 2 micrograms/ml. Both agents inhibited Listeria monocytogenes, Corynebacterium group JK species, anaerobic cocci, and Clostridium spp. including Clostridium difficile. They did not inhibit members of the family Enterobacteriaceae or Pseudomonas aeruginosa, but the MIC for 90% of Bacteroides fragilis isolates was 8 micrograms of DuP 721 per ml.
Comparative in vitro activity of the new oxazolidinones DuP 721 and DuP 105 against staphylococci and streptococci
Eur J Clin Microbiol Infect Dis 1989 Mar;8(3):256-60.PMID:2523807DOI:10.1007/BF01965273.
The in vitro activity of DuP 721 and DuP 105, two orally active members of the oxazolidinones, was compared with that of glycopeptides and ciprofloxacin against 185 gram-positive isolates. Ninety percent of Staphylococcus aureus isolates, including penicillin- and methicillin-resistant strains, were inhibited by DuP 721 at 1 micrograms/ml and by DuP 105 at 16 micrograms/ml; DuP 721 inhibited 90% of coagulase-negative staphylococci tested at 1 micrograms/ml. The MIC90 for Streptococcus faecalis was 4 micrograms/ml with DuP 721 and 16 micrograms/ml with DuP 105; DuP 721 inhibited 90% of beta-hemolytic streptococci of group A at 0.5 micrograms/ml. Similar results on selected strains were obtained by continuously recording the optical density of cultures.