Doripenem Hydrate
(Synonyms: 多尼培南(一水合物),S 4661 monohydrate) 目录号 : GC16675
A broad-spectrum antibiotic
Cas No.:364622-82-2
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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
|
Cell lines |
bacteria |
|
Preparation method |
The solubility of this compound in DMSO is >11mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Applications |
S-4661 was potent against methicillin-susceptible Staphylococcus aureus and methicillin-susceptible Staphylococcus epidermidis with the MIC90 of 0.063 μg/ml. S-4661 was potent against penicillin-resistant S. pneumoniae. S-4661 showed activities against S. pyogenes and penicillin-resistant S. pneumoniae. S-4661 was active against Enterococcus faecalis. S-4661 was particularly active against Enterobacteriaceae and H. influenzae. The MIC90s for Escherichia, Klebsiella, Proteus, Providencia, Morganella, Citrobacter, Enterobacter, and Serratia spp. ranged from 0.063 to 0.5 μg/ml. |
| Animal experiment [1]: | |
|
Animal models |
Male SLC/ICR mouse model of bacteremia, mouse model of respiratory tract infection induced by S. pneumonia, male CBA/JNCrj mouse model of pulmonary infection induced by penicillin-resistant S. Pneumonia TUH741 |
|
Dosage form |
Subcutaneously administration, twice daily for 2 days |
|
Application |
The ED50 of S-4661 against S. aureus Smith was 0.066 mg/kg. The ED50 of S-4661 was 0.23 mg/kg against S. pneumonia TUH39, the same as that of imipenem-cilastatin. S-4661 (10 mg/kg) showed significant antibacterial activity. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Tsuji M, Ishii Y, Ohno A, et al. In vitro and in vivo antibacterial activities of S-4661, a new carbapenem[J]. Antimicrobial agents and chemotherapy, 1998, 42(1): 94-99. | |
Doripenem hydrate is a parenteral, potent, and well-balanced antibiotic against a wide range of both Gram+ and Gram- bacteria including Pseudomonas aeruginosa [1] with MIC90 values of ≤ 0.5 µg/ml against methicillin-susceptible streptococci and staphylococci, 0.032-0.5 µg/ml against members of the family Enterobacteriaceae, Moraxella catarrhalis, and Haemophilus influenza, and 8 µg/ml against Pseudomonas aeruginosa [2].
Patients with cystic fibrosis can be infected with several pathogens such as Haemophilus influenzae, Staphylococcus aureus and P. aeruginosa, chronically. By 18 years of age, 80% of cystic fibrosis patients are infected with P. aeruginosa [3].
Doripenem hydrate was potent against Staphylococcus aureus and Staphylococcus epidermidis with the same MIC90 value of 0.063 µg/ml. Doripenem hydrate was 2-4 times more active than other tested carbapenems against S. aureus. The activity of doripenem hydrate against S. pneumoniae was similar to that of imipenem but higher than that of other tested agents. Doripenem hydrate was potent against S. pneumonia with an activity similar to that of other tested carbapenems (MIC90, 0.5 µg/ml). Doripenem hydrate had an activity similar to that of cefpirome against S. pneumoniae and S. pyogenes. Doripenem hydrate was more active against Enterococcus faecalis than other tested agents except for imipenem [2].
In mice experimentally induced with acute bacteremia, the ED50 of doripenem hydrate against S. aureus Smith was 0.066 mg/kg. Doripenem hydrate was more effective than other tested carbapenems against S. aureus TUH1. Doripenem hydrate was more effective than other tested agents except for meropenem-cilastatin against E. coli C-11. Doripenem hydrate almost shared the same effectiveness with other tested carbapenems against P. aeruginosa E7. Against P. aeruginosa TUH302, doripenem hydrate was the most effective among tested drugs [2].
References:
[1]. Yutaka Nishino, Makoto Kobayashi, Taneyoshi Shinno, et al. Practical Large-Scale Synthesis of Doripenem: A Novel 1â-Methylcarbapenem Antibiotic. Organic Process Research & Development, 2003, 7:846-850.
[2]. Masakatsu Tsuji, Yoshikazu Ishii, Akira Ohno, et al. In Vitro and In Vivo Antibacterial Activities of S-4661, a New Carbapenem. Antimicrobial Agents and Chemotherapy, 1998, 42(1): 94-99.
[3]. Yunhua Chen, Elizabeth Garber, Qiuqu Zhao, et al. In Vitro Activity of Doripenem (S-4661) against Multidrug-Resistant Gram-Negative Bacilli Isolated from Patients with Cystic Fibrosis. Antimicrobial Agents and Chemotherapy, 2005, 49(6):2510-2511.
| Cas No. | 364622-82-2 | SDF | |
| 别名 | 多尼培南(一水合物),S 4661 monohydrate | ||
| 化学名 | (4R,5S,6S)-6-[(1R)-1-hydroxyethyl]-4-methyl-7-oxo-3-[(3S,5S)-5-[(sulfamoylamino)methyl]pyrrolidin-3-yl]sulfanyl-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid;hydrate | ||
| Canonical SMILES | CC1C2C(C(=O)N2C(=C1SC3CC(NC3)CNS(=O)(=O)N)C(=O)O)C(C)O.O | ||
| 分子式 | C15H24N4O6S2.H2O | 分子量 | 438.52 |
| 溶解度 | ≥ 10.96mg/mL 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 | 2.2804 mL | 11.402 mL | 22.804 mL |
| 5 mM | 0.4561 mL | 2.2804 mL | 4.5608 mL |
| 10 mM | 0.228 mL | 1.1402 mL | 2.2804 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。