Sulbactam sodium
(Synonyms: 舒巴坦钠; CP45899 sodium) 目录号 : GC12665
Sulbactam一种β-内酰胺酶抑制剂，常与β-内酰胺类抗生素联合使用，以增强其对抗耐药菌的效力。
Cas No.:69388-84-7
Sample solution is provided at 25 µL, 10mM.
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Sulbactam, a β-lactamase inhibitor, is commonly used in combination with β-lactam antibiotics to enhance their efficacy against drug-resistant bacteria[1]. One of the reasons for the development of bacterial resistance to β-lactam antibiotics is the production of β-lactamases[2]. Sulbactam irreversibly binds to bacterial β-lactamases, preventing these enzymes from hydrolyzing β-lactam antibiotics[3], thereby preserving the ability of β-lactam antibiotics to inhibit bacterial cell wall formation[4].
In vitro, when Sulbactam (0.5, 1, 2, 4, 8mg/L) is combined with β-lactam antibiotics (ampicillin, cefoperazone, imipenem) at various ratios (2:1, 1:1, 1:1.5, 1:2, 1:2.5, 1:3) to treat Acinetobacter baumannii, Sulbactam significantly enhances the bactericidal activity of the antibiotics against A. baumannii [5]. Zidebactam (4mg/L) combined with Sulbactam (0.12–512mg/L) significantly restores the susceptibility of carbapenem-resistant Acinetobacter baumannii (CRAB) clinical isolates to Sulbactam. Among 43 CRAB strains, 84% showed a ≥2-fold decrease in MIC of Sulbactam when tested in combination with Zidebactam [6].
In vivo, Sulbactam (10.0mg/kg) was administered via intracerebroventricular injection to prevent ischemic injury in a rat model of cerebral ischemia. The administration began 5 days before the occurrence of ischemia, once daily for a total of 5 consecutive days. Sulbactam pretreatment significantly improved the binding characteristics of glutamate transporter-1 (GLT-1) and inhibited the increase in extracellular glutamate concentration in the CA1 region of the hippocampus in ischemic rats. Sulbactam also protected neurons in the CA1 region and alleviated ischemia-induced delayed neuronal death[7]. Sulbactam (400, 1000, and 2000mg/kg/d) was administered via intraperitoneal injection to induce epilepsy in a chronic renal failure (CRF) mouse model, starting immediately after the CRF model was established. Sulbactam at all three doses significantly induced epileptic seizures in a dose-dependent manner in CRF mice, leading to death. In particular, the high dose (2000mg/kg/d) of Sulbactam caused seizures in CRF mice as early as 3 days after administration[8].
References:
[1] Noguchi JK, Gill MA. Sulbactam: a beta-lactamase inhibitor. Clin Pharm. 1988 Jan;7(1):37-51.
[2] Tooke CL, Hinchliffe P, Bragginton EC, et al. β-Lactamases and β-Lactamase Inhibitors in the 21st Century. J Mol Biol. 2019 Aug 23;431(18):3472-3500.
[3] Akova M. Sulbactam-containing beta-lactamase inhibitor combinations. Clin Microbiol Infect. 2008 Jan;14 Suppl 1:185-8.
[4] Fu Y, Asempa TE, Kuti JL. Unraveling sulbactam-durlobactam: insights into its role in combating infections caused by Acinetobacter baumannii. Expert Rev Anti Infect Ther. 2025 Jan;23(1):67-78.
[5] Wang L, Chen Y, Han R, et al. Sulbactam Enhances in vitro Activity of β-Lactam Antibiotics Against Acinetobacter baumannii. Infect Drug Resist. 2021 Sep 28;14:3971-3977.
[6] Cedano J, Baez M, Pasteran F, et al. Zidebactam restores sulbactam susceptibility against carbapenem-resistant Acinetobacter baumannii isolates. Front Cell Infect Microbiol. 2022 Jul 8;12:918868.
[7] Gu WW, Cui X, Liu LZ, et al. Sulbactam improves binding property and uptake capacity of glutamate transporter-1 and decreases glutamate concentration in the CA1 region of hippocampus of global brain ischemic rats. Amino Acids. 2021 Nov;53(11):1649-1661.
[8] Wu Y, Gu D, Li J, et al. Role of the gut microbiota in cefoperazone/sulbactam-induced epilepsy in mice with chronic renal failure. Ren Fail. 2024 Dec;46(2):2371551.
Sulbactam一种β-内酰胺酶抑制剂，常与β-内酰胺类抗生素联合使用，以增强其对抗耐药菌的效力[1]。细菌产生β-内酰胺类抗生素能力原因之一是β-内酰胺酶的出现[2]，而Sulbactam通过不可逆地结合到细菌的β-内酰胺酶上，阻止这些酶分解β-内酰胺类抗生素[3]，从而保护β-内酰胺类抗生素对细菌细胞壁形成的抑制能力[4]。
在体外，当Sulbactam（0.5、1、2、4、8mg/L）与β-内酰胺类抗生素（氨苄西林、头孢哌酮、亚胺培南）以不同比例（2:1、1:1、1:1.5、1:2、1:2.5、1:3）联合处理鲍曼不动杆菌，显著增强了抗生素对鲍曼不动杆菌的杀菌活性[5]。Zidebactam（4mg/L）联合Sulbactam（0.12–512mg/L）处理耐碳青霉烯类鲍曼不动杆菌（CRAB）临床菌株，显著恢复了CRAB对Sulbactam的敏感性。在43株CRAB菌株中，84%的菌株在联合Zidebactam后对Sulbactam的MIC降低≥2倍稀释度[6]。
在体内，Sulbactam（10.0mg/kg）通过侧脑室注射给药，用于预防脑缺血大鼠模型中的缺血性损伤，给药时间为缺血发生前5天开始，每天一次，连续给药5天。Sulbactam预处理能够显著改善谷氨酸转运体-1（GLT-1）的结合特性，并抑制缺血大鼠海马CA1区细胞外谷氨酸浓度的升高，保护CA1区神经元，减轻缺血引起的迟发性神经元死亡 [7]。Sulbactam（400、1000和2000mg/kg/d）通过腹腔注射给药，以建立慢性肾衰竭（CRF）小鼠模型的癫痫，给药时间为CRF模型建立后立即进行。Sulbactam在所有三个剂量下均能以剂量依赖性方式显著诱导CRF小鼠发生癫痫发作，并导致死亡。特别是高剂量（2000mg/kg/d）的Sulbactam使CRF小鼠在给药后3天内即发生癫痫发作[8]。
| Cell experiment [1]: | |
Cell lines | Clinical isolates of carbapenem-resistant Acinetobacter baumannii (CRAB) |
Preparation Method | A total of 43 geographically and genetically distinct CRAB clinical strains containing different mechanisms of resistance (OXA-23, OXA-58, IMP-1, NDM-1, ISAba1-OXA-66) were used to test Sulbactam or Sulbactam in combination with zidebactam. Additionally, three reference strains (AB0057, AB5075, and AYE) were included. The strains were tested against Sulbactam (range 0.12–512mg/l) and Sulbactam plus 4mg/l zidebactam using the microdilution method according to CLSI Standards. |
Reaction Conditions | Sulbactam (range 0.12–512mg/l) and Sulbactam plus 4mg/l zidebactam |
Applications | Sulbactam in combination with zidebactam significantly restored Sulbactam susceptibility against CRAB strains. The combination showed a ≥2 dilutions decrease in Sulbactam MICs in 84% of the isolates tested. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | Global brain ischemia was induced by tightening nylon sutures to block the blood flow of the bilateral common carotid arteries for 8 minutes. The rats were treated with Sulbactam (10.0mg/kg) via lateral ventricle injection once daily for five consecutive days prior to ischemia. After the last administration, global brain ischemia or sham treatment was performed. The sham rats received the same treatments except the bilateral vertebral artery and bilateral common carotid artery were not occluded. The rats were sacrificed at various time points after reperfusion for different assays. |
Dosage form | 10.0mg/kg; i.c.v. |
Applications | Sulbactam pretreatment significantly improved the binding characteristics of glutamate transporter-1 (GLT-1) and inhibited the increase in extracellular glutamate concentration in the CA1 region of the hippocampus in ischemic rats. Sulbactam also protected neurons in the CA1 region and alleviated ischemia-induced delayed neuronal death. |
References: | |
| Cas No. | 69388-84-7 | SDF | |
| 别名 | 舒巴坦钠; CP45899 sodium | ||
| 化学名 | sodium;(2S,5R)-3,3-dimethyl-4,4,7-trioxo-4λ6-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate | ||
| Canonical SMILES | CC1(C(N2C(S1(=O)=O)CC2=O)C(=O)[O-])C.[Na+] | ||
| 分子式 | C8H10NO5S.Na | 分子量 | 255.22 |
| 溶解度 | ≥ 10.75mg/mL in Water | 储存条件 | Store at -20°C, protect from light, stored under nitrogen |
| 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 | 3.9182 mL | 19.5909 mL | 39.1819 mL |
| 5 mM | 0.7836 mL | 3.9182 mL | 7.8364 mL |
| 10 mM | 0.3918 mL | 1.9591 mL | 3.9182 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。
Quality Control & SDS
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- Purity: >98.00%
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