2. Anti-infection
  3. Antibiotic Bacterial Penicillin-binding protein (PBP)
  4. Cefozopran dihydrochloride

Cefozopran dihydrochloride  (Synonyms: SCE-2787 dihydrochloride)

目录号: HY-W740077
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Cefozopran (SCE-2787) dihydrochloride 是一种具有广谱抗菌活性的强效抗生素。Cefozopran dihydrochloride 可结合 PBPs，诱导细胞壁破坏、细胞伸长、丝状体形成、不规则隔膜形成，以及杀菌、溶菌活性。Cefozopran dihydrochloride 可降低小鼠呼吸道、泌尿道和大腿肌肉感染模型中的细菌数量并清除细菌。Cefozopran dihydrochloride 可用于细菌感染的相关研究。

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Cefozopran dihydrochloride

Cefozopran dihydrochloride Chemical Structure

CAS No. : 1262200-57-6

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Cefozopran dihydrochloride 的其他形式现货产品:

Other Forms of Cefozopran dihydrochloride:

Cefozopran dihydrochloride 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cefozopran (SCE-2787) dihydrochloride is a potent antibiotic with broad-spectrum antibacterial activity. Cefozopran dihydrochloride binds PBPs, induces cell wall destruction, cell elongation, filamentation, irregular septa formation, and bactericidal, bacteriolytic activity. Cefozopran dihydrochloride reduces bacterial counts and eradicates bacteria in mouse respiratory, urinary, and thigh muscle infections. Cefozopran dihydrochloride can be used for the research of bacterial infections[1][2][3][4].

体外研究
(In Vitro)

Cefozopran (20 h) dihydrochloride 可强效抑制化脓性链球菌 (Streptococcus pyogenes)、金黄色葡萄球菌 (Staphylococcus aureus)、粪肠球菌 (Enterococcus faecalis) 的生长，且对链球菌属 (Streptococcus species)、肠杆菌科 (普通变形杆菌 Proteus vulgaris 除外) 以及甲氧西林 (HY-121544) 敏感葡萄球菌表现出尤为显著的活性[4]。
Cefozopran (20 h) dihydrochloride 可抑制多种实验室需氧菌株的生长，其 MIC 值范围为 0.1 μg/mL 至 50 μg/mL，且对受试厌氧菌株的活性有限[4]。
Cefozopran (20 h) dihydrochloride 对头孢他啶 (HY-B0593) 耐药的弗氏柠檬酸杆菌 (MIC90 = 3.13 μg/mL) 和阴沟肠杆菌 (MIC90 = 12.5 μg/mL) 具有高活性，但对 Ceftazidime (HY-B0593) 耐药的铜绿假单胞菌 (MIC90 >100 μg/mL) 表现出与头孢他啶的交叉耐药性[4]。
Cefozopran (200 μM) dihydrochloride 对多数常见 β-内酰胺酶的水解作用具有高度抗性，包括 Bush 1、2a、2b 和 2c 组酶，但会被 Bush 2b'、2d 和 2e 组酶不同程度地水解[4]。
Cefozopran dihydrochloride 对所有受试 β-内酰胺酶的亲和力较低，其 Km/Ki 值均>100 μM，表明它与这些酶的相互作用极弱[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cefozopran dihydrochloride 相关抗体:
体内研究
(In Vivo)

Cefozopran (5-80 mg/kg；皮下注射；每日 2 次；连续 5 天) dihydrochloride 对小鼠急性 K. pneumoniae 呼吸道感染表现出强效活性[2]。
Cefozopran (20-80 mg/kg；皮下注射；每日 2 次；共 7 天) dihydrochloride 可有效清除小鼠体内慢性肺炎克雷伯菌呼吸道感染[2]。
Cefozopran (1.56-100 mg/kg；皮下注射；每日 2 次；连续 5 天；感染后 3 天开始) dihydrochloride 对小鼠 P. aeruginosa 尿路感染表现出强效抑制活性[2]。
Cefozopran (0.625-40 mg/kg；皮下注射；感染后 2、18、26 小时给药) dihydrochloride 对小鼠 MSSA 大腿肌肉脓肿感染显示出强效作用[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: ICR mice (4-week-old, male) with acute respiratory tract infection induced by aerosol exposure to Klebsiella pneumoniae DT-S for 40 minutes[2]
Dosage: 5; 20; 80 mg/kg
Administration: s.c.; twice daily; 5 days
Result: Showed 0/10 survival rate and 0/10 lung sterilization rate at 5 mg/kg.
Showed 8/10 survival rate and 2/10 lung sterilization rate at 20 mg/kg.
Showed 10/10 survival rate and 10/10 lung sterilization rate at 80 mg/kg.
Achieved an SD50 of 13.8 mg/kg and a CD50 of 29.0 mg/kg.
Had an MIC of 0.05 μg/mL against Klebsiella pneumoniae DT-S.
Animal Model: CBA/J mice (5-week-old, female) with chronic respiratory tract infection induced by aerosol exposure to Klebsiella pneumoniae 27 for 60 minutes[2]
Dosage: 20; 40; 80 mg/kg
Administration: s.c.; twice daily; 7 days
Result: Showed 1/12 lung sterilization rate at 20 mg/kg.
Showed 0/11 lung sterilization rate at 40 mg/kg.
Showed 12/12 lung sterilization rate at 80 mg/kg.
Achieved a CD50 of 55.2 mg/kg.
Had an MIC of 0.05 μg/mL against Klebsiella pneumoniae 27.
Animal Model: CBA/J mice with urinary tract infection induced by transurethral inoculation of Pseudomonas aeruginosa P9 with urethral clamping for 6 hours[2]
Dosage: 1.56; 6.25; 25; 100 mg/kg
Administration: s.c.; twice daily; 5 days; tarting 3 days after infection
Result: Showed 3/15 kidney sterilization rate at 1.56 mg/kg.
Showed 7/15 kidney sterilization rate at 6.25 mg/kg.
Showed 11/15 kidney sterilization rate at 25 mg/kg.
Showed 12/15 kidney sterilization rate at 100 mg/kg.
Achieved a CD50 of 8.78 mg/kg.
Had an MIC of 0.78 μg/mL against Pseudomonas aeruginosa P9.
Animal Model: ICR mice with thigh muscle infection induced by injection of Methicillin-sensitive Staphylococcus aureus[2]
Dosage: 0.625; 2.5; 10; 40 mg/kg
Administration: s.c.; single dose at 2, 18, 26 hours post-infection
Result: Showed a mean bacterial count of 6.14 log CFU and an effective rate of 2/8 at 0.625 mg/kg.
Showed a mean bacterial count of 5.38 log CFU and an effective rate of 3/8 at 2.5 mg/kg.
Showed a mean bacterial count of 4.77 log CFU and an effective rate of 6/8 at 10 mg/kg.
Showed a mean bacterial count of 4.59 log CFU and an effective rate of 8/8 at 40 mg/kg.
Achieved an ED50 of 2.87 mg/kg.
Had an MIC of 0.39 μg/mL against methicillin-sensitive Staphylococcus aureus.
Animal Model: ICR mice with thigh muscle infection induced by injection of Methicillin-resistant Staphylococcus aureus N133[2]
Dosage: 3.125; 12.5; 50; 200 mg/kg
Administration: s.c.; single dose at 2, 18, 26 hours post-infection
Result: Showed a mean bacterial count of 7.63 log CFU and an effective rate of 0/8 at 3.125 mg/kg.
Showed a mean bacterial count of 7.55 log CFU and an effective rate of 0/8 at 12.5 mg/kg.
Showed a mean bacterial count of 6.54 log CFU and an effective rate of 2/8 at 50 mg/kg.
Showed a mean bacterial count of 4.82 log CFU and an effective rate of 7/8 at 200 mg/kg.
Achieved an ED50 of 79.8 mg/kg.
Had an MIC of 50 μg/mL against methicillin-resistant Staphylococcus aureus N133.
分子量

588.45

Formula

C19H19Cl2N9O5S2
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Cefozopran dihydrochloride 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cefozopran1262200-57-6SCE-2787SCE2787SCE 2787AntibioticBacterialPenicillin-binding protein (PBP)β-lactamasesEscherichia coli PBP 3methicillin-resistant Staphylococcus aureusStaphylococcus aureus PBPs 1-2Citrobacter freundiiKlebsiella pneumoniaeEnterococcus faecalisEnterobacter cloacaeStreptococcus pyogenesPseudomonas aeruginosa PBPs 1-3Inhibitorinhibitorinhibit

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