Piperacillin Sodium
(Synonyms: 哌拉西林钠; Sodium piperacillin) 目录号 : GC16755
Piperacillin Sodium是一种广谱半合成青霉素类抗生素，用于治疗多种由敏感细菌引起的感染。Piperacillin Sodium通过抑制细菌细胞壁的合成发挥抗菌作用，能够有效对抗多种革兰氏阳性菌和革兰氏阴性菌，包括一些产β-内酰胺酶的菌株。
Cas No.:59703-84-3
Sample solution is provided at 25 µL, 10mM.
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Piperacillin Sodium is a broad-spectrum semisynthetic penicillin antibiotic used to treat a variety of infections caused by susceptible bacteria[1]. Piperacillin Sodium exerts its antibacterial action by inhibiting bacterial cell wall synthesis and is effective against a wide range of Gram-positive and Gram-negative bacteria, including some strains that produce β-lactamases[2]. Piperacillin Sodium is often used in combination with other drugs, such as tazobactam, to enhance antibacterial efficacy and broaden the spectrum of activity, better addressing resistant strains[3]. Piperacillin Sodium is commonly used to treat respiratory, urinary, intra-abdominal infections, and skin and soft tissue infections[4].
In vitro, Piperacillin Sodium (2μg/mL) inhibits Staphylococcus aureus with an efficacy rate of up to 93%, and Piperacillin Sodium (4μg/mL) inhibits Escherichia coli with an efficacy rate of up to 90%[5]. Piperacillin Sodium (2–8μg/mL) pre-treatment of various bacteria (Klebsiella pneumoniae, Streptococcus agalactiae, Proteus vulgaris, Haemophilus influenzae) for 18 hours significantly inhibits bacterial growth and reduces resistance[6].
In vivo, Piperacillin Sodium (2.5–5120mg/kg) in combination with the novel β-lactamase inhibitor IID572 (4–640mg/kg) administered subcutaneously three times daily was used in a neutropenic C57BL/6J mouse thigh infection model. The combination of Piperacillin/IID572 significantly reduced the infection burden caused by β-lactamase-producing Enterobacteriaceae and Staphylococcus aureus[7]. Subcutaneous injection of Piperacillin Sodium (10.7mg) in combination with oral β-lactamase (1 or 6mg/kg) was used in CF-1 mice. Compared with mice treated with Piperacillin Sodium alone, the combination with β-lactamase significantly reduced intestinal colonization by Piperacillin-resistant pathogens (including vancomycin-resistant Enterococcus faecium, Klebsiella pneumoniae, and Candida glabrata) and minimized disruption of the indigenous microbiota[8].
References:
[1] Fortner CL, Finley RS, Schimpff SC. Piperacillin sodium: antibacterial spectrum, pharmacokinetics, clinical efficacy, and adverse reactions. Pharmacotherapy. 1982 Nov-Dec;2(6):287-99.
[2] Holmes B, Richards DM, Brogden RN, et al. Piperacillin. A review of its antibacterial activity, pharmacokinetic properties and therapeutic use. Drugs. 1984 Nov;28(5):375-425.
[3] Eliopoulos GM, Moellering RC Jr. Azlocillin, mezlocillin, and piperacillin: new broad-spectrum penicillins. Ann Intern Med. 1982 Nov;97(5):755-60.
[4] Russo J Jr, Russo ME. Comparative review of two new wide-spectrum penicillins: mezlocillin and piperacillin. Clin Pharm. 1982 May-Jun;1(3):207-16.
[5] Frank U, Mutter J, Schmidt-Eisenlohr E, et al. Comparative in vitro activity of piperacillin, piperacillin-sulbactam and piperacillin-tazobactam against nosocomial pathogens isolated from intensive care patients. Clin Microbiol Infect. 2003 Nov;9(11):1128-32.
[6] Verbist L. In vitro activity of piperacillin, a new semisynthetic penicillin with an unusually broad spectrum of activity. Antimicrob Agents Chemother. 1978 Mar;13(3):349-57. doi: 10.1128/AAC.13.3.349.
[7] Growcott EJ, Gamboa L, Roth T, et al. Efficacy of piperacillin in combination with novel β-lactamase inhibitor IID572 against β-lactamase-producing strains of Enterobacteriaceae and Staphylococcus aureus in murine neutropenic thigh infection models. J Antimicrob Chemother. 2020 Jun 1;75(6):1530-1536.
[8] Stiefel U, Pultz NJ, Harmoinen J, et al. Oral administration of beta-lactamase preserves colonization resistance of piperacillin-treated mice. J Infect Dis. 2003 Nov 15;188(10):1605-9.
Piperacillin Sodium是一种广谱半合成青霉素类抗生素，用于治疗多种由敏感细菌引起的感染[1]。Piperacillin Sodium通过抑制细菌细胞壁的合成发挥抗菌作用，能够有效对抗多种革兰氏阳性菌和革兰氏阴性菌，包括一些产β-内酰胺酶的菌株[2]。Piperacillin Sodium通常与其他药物（如他唑巴坦）联合使用，以增强抗菌效果并扩大抗菌谱，更好地应对耐药菌株[3]。Piperacillin Sodium常用于治疗呼吸道感染、泌尿道感染、腹腔感染和皮肤软组织感染等[4]。
在体外，Piperacillin Sodium（2μg/mL）对Staphylococcus aureus的抑制率高达93%，Piperacillin Sodium（4μg/mL）对Escherichia coli的抑制率高达90%[5]。Piperacillin Sodium（2–8μg/mL）预处理多种细菌（Klebsiella pneumoniae、Streptococcus agalactiae、Proteus vulgaris、Haemophilus influenzae）18h，Piperacillin Sodium显著抑制细菌的生长，同时降低耐药性表现[6]。
在体内，Piperacillin Sodium（2.5–5120mg/kg）联合新型β-内酰胺酶抑制剂IID572（4–640mg/kg）每天三次皮下注射，用于处理中性粒细胞减少的C57BL/6J小鼠大腿感染模型。Piperacillin/IID572显著减少了由产β-内酰胺酶的肠杆菌科细菌和金黄色葡萄球菌引起的感染负担[7]。皮下注射Piperacillin Sodium（10.7mg）联合口服β-内酰胺酶（1或6mg/kg），用于处理CF-1小鼠。与仅接受Piperacillin Sodium的小鼠相比，联合β-内酰胺酶显著减少了由耐Piperacillin的病原体（包括vancomycin-resistant Enterococcus faecium、Klebsiella pneumoniae和Candida glabrata）引起的肠道定植，同时减少了对肠道菌群的干扰[8]。
| Cell experiment [1]: | |
Cell lines | Klebsiella pneumoniae, Streptococcus agalactiae, Proteus vulgaris, Haemophilus influenzae |
Preparation Method | The in vitro activity of Piperacillin Sodium was tested against these bacterial strains using agar dilution and broth microdilution methods. The minimum inhibitory concentrations (MICs) and minimum bactericidal concentrations (MBCs) were determined. |
Reaction Conditions | 2–8μg/mL; 24h |
Applications | Piperacillin Sodium was effective against Haemophilus influenzae and Streptococcus agalactiae at 2μg/mL. Piperacillin Sodium was more active than ampicillin against Klebsiella pneumoniae at 8μg/mL. |
| Animal experiment [2]: | |
Animal models | Neutropenic CD-1 mice |
Preparation Method | Mice were rendered neutropenic by intraperitoneal injections of cyclophosphamide (150 and 100mg/kg) on days 4 and 1, respectively. Two hours prior to treatment, bacterial inoculum (105–106CFU) was administered into the left gastrocnemius muscle via intramuscular injection. Subcutaneous treatment with Piperacillin Sodium (2.5–5120mg/kg/day)/IID572 (4–640mg/kg/day) or Piperacillin Sodium (5120mg/kg/day) was initiated every 3 hours for 24 hours. |
Dosage form | 2.5–5120mg/kg/day; s.c. |
Applications | IID572 significantly enhances the in vivo bactericidal effect of Piperacillin Sodium. |
References: | |
| Cas No. | 59703-84-3 | SDF | |
| 别名 | 哌拉西林钠; Sodium piperacillin | ||
| 化学名 | sodium;(2S,5R,6R)-6-[[(2R)-2-[(4-ethyl-2,3-dioxopiperazine-1-carbonyl)amino]-2-phenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate | ||
| Canonical SMILES | CCN1CCN(C(=O)C1=O)C(=O)NC(C2=CC=CC=C2)C(=O)NC3C4N(C3=O)C(C(S4)(C)C)C(=O)[O-].[Na+] | ||
| 分子式 | C23H26N5O7S.Na | 分子量 | 539.54 |
| 溶解度 | ≥ 18.6mg/mL in DMSO | 储存条件 | Store at 2-8°C, sealed storage, away from moisture |
| 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8534 mL | 9.2672 mL | 18.5343 mL |
| 5 mM | 370.7 μL | 1.8534 mL | 3.7069 mL |
| 10 mM | 185.3 μL | 926.7 μL | 1.8534 mL |
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动物平均体重 | g | |
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动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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- Purity: >98.00%
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