Sulopenem

(Synonyms: CP-70429)
目录号: PL12198 纯度: ≥98%
Sulopenem (CP-70429) 是一种具有口服活性的肠胃外青霉烯类抗生素,对革兰氏阳性菌和革兰氏阴性菌具有广谱活性。Sulopenem 可用于尿路感染和腹腔内感染的研究。Sulopenem 对铜绿假单胞菌和嗜黄单胞菌的嗜麦芽孢杆菌无效。
CAS No. :120788-07-0
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中文名称
Sulopenem
中文别名
硫培南;硫陪南
英文名称
Sulopenem
英文别名
4-Thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylicacid,6-[(1R)-1-hydroxyethyl]-7-oxo-3-[[(1R,3S)-tetrahydro-1-oxido-3-thienyl]thio]-,(5R,6S)-;4-Thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylicacid,6-[(1R)-1-hydroxyethyl]-7-oxo-3-[[(1R,3S)-tetrahydro-1-oxido-3-thienyl];4-Thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylicacid,6-[(1R)-1-hydroxyethyl]-7-oxo-3-[[(1R,3S...;SULOPENEM;(3S)-3-({(5R;(5R,6S)-6-(1(R)-Hydroxyethyl)-2-[(1(R)-oxo-3(S)-thiolanyl)thio]-2-penem-3-carboxylic acid;6S)-2-carboxy-6-[(1R)-1-hydroxyethyl]-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-2-en-3-yl}sulfanyl)tetrahydrothiophenium-1-olate;(5R,6S)-6-[(1R)-1-Hydroxyethyl]-7-oxo-3-[[(1R,3S)-tetrahydro-1-oxido-3-thienyl]thio]-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid;CP-70429;CP-65207-S;(S)-3-[[(5R)-2-Carboxy-6β-[(R)-1-hydroxyethyl]-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-2-en-3-yl]thio]tetrahydrothiophene 1-oxide;Sulopenem
Cas No.
120788-07-0
分子式
C12H15NO5S3
分子量
349.45
包装储存
Powder -20°C 3 years;4°C 2 years
详情描述
Sulopenem (CP-70429) 是一种具有口服活性的肠胃外青霉烯类抗生素,对革兰氏阳性菌和革兰氏阴性菌具有广谱活性。Sulopenem 可用于尿路感染和腹腔内感染的研究。Sulopenem 对铜绿假单胞菌和嗜黄单胞菌的嗜麦芽孢杆菌无效。
产品详情
Sulopenem (CP-70429) 是一种具有口服活性的肠胃外青霉烯类抗生素,对革兰氏阳性菌和革兰氏阴性菌具有广谱活性。Sulopenem 可用于尿路感染和腹腔内感染的研究。Sulopenem 对铜绿假单胞菌和嗜黄单胞菌的嗜麦芽孢杆菌无效。
生物活性
Sulopenem (CP-70429) is an orally active, parenteral penem antibiotic with broad-spectrum activities against Gram-positive and Gram-negative bacteria. Sulopenem has the potential for urinary tract infections and intra-abdominal infections treatment. Sulopenem is inactive against Pseudomonas aeruginosa and Xanthomonas maltophilia.
性状
Solid
IC50 & Target[1][2]
β-lactam
体外研究(In Vitro)
Sulopenem has the potential for uncomplicated and complicated urinary tract infections and intra-abdominal infections treatment, including multidrug-resistant (MDR) infections and infections attributable to quinolone-nonsusceptible and/or extended-spectrum β-lactamase (ESBL)-producing Gram-negative bacilli.
Sulopenem inhibits the growth of most isolates of aerobic and anaerobic Gram-positive and Gram-negative bacteria, including methicillin-susceptible Staphylococcus aureus , Streptococcus pneumoniae (penicillin-susceptible and -resistant isolates), group A and B β-hemolytic streptococci, Listeria monocytogenes , Enterobacteriaceae , Haemophilus influenzae , and Moraxella catarrhalis but excluding P. aeruginosa and Stenotrophomonas maltophilia , at a concentration of ≤1?μg/mL.
体内研究(In Vivo)
The protective effects of Sulopenem in murine experimental systemic infections are superior to those of Imipenem/Cilastatin. In murine experimental mixed infection with Escherichia coli and Bacteroides fragilis, Sulopenem has lower ED 50 . In guinea pigs experimental lung infection with Klebsiella pneumoniae, Sulopenem is more effective than CZON or Cefotiam. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. James A Karlowsky, et al. In Vitro Activity of Sulopenem, an Oral Penem, Against Urinary Isolates of Escherichia coli. Antimicrob Agents Chemother. 2018 Dec 21;63(1):e01832-18.
[2]. M Minamimura, et al. In Vitro Antibacterial Activity and Beta-Lactamase Stability of CP-70,429 a New Penem Antibiotic. Antimicrob Agents Chemother. 1993 Jul;37(7):1547-51.
溶解度数据
In Vitro: DMSO : 83.33 mg/mL (238.46 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)
[1]. James A Karlowsky, et al. In Vitro Activity of Sulopenem, an Oral Penem, Against Urinary Isolates of Escherichia coli. Antimicrob Agents Chemother. 2018 Dec 21;63(1):e01832-18.
[2]. M Minamimura, et al. In Vitro Antibacterial Activity and Beta-Lactamase Stability of CP-70,429 a New Penem Antibiotic. Antimicrob Agents Chemother. 1993 Jul;37(7):1547-51.

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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