Sulfamethoxazole
(Synonyms: 磺胺甲恶唑; Ro 4-2130) 目录号 : GC11874
Sulfamethoxazole是一种抑菌磺酰胺类抗生素。
Cas No.:723-46-6
Sample solution is provided at 25 µL, 10mM.
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Sulfamethoxazole is a bacteriostatic sulfonamide antibiotic [1]. Sulfamethoxazole competitively inhibits bacterial dihydropteroate synthase (DHPS), blocking folate synthesis and thereby interfering with DNA and protein synthesis [2-3]. Sulfamethoxazole is widely used to treat urinary tract infections, respiratory tract infections, and gastrointestinal infections [4].
In E. coli, after Sulfamethoxazole (1.6mg/mL; 24h) treatment, the activity of bacterial was significantly inhibited [5]. In mouse pancreatic β cells, Sulfamethoxazole (0.1-10mM; 3h) treatment inhibits the channel current of KATP and the inhibition is dose-dependent [6].
In Toxoplasma gondii infected mouse model, Sulfamethoxazole (300mg/kg; po; 24d) significantly decreased mortality among the infected WT C57BL/6 and GKO mice [7]. In danio rerio, Sulfamethoxazole (250ppm; embryo culture;5d) induces brain capillary toxicity by upregulating VEGF and chemokine signaling [8].
References:
[1]. Rudy B C, Senkowski B Z. Sulfamethoxazole[M]//Analytical profiles of drug substances. Academic Press, 1973, 2: 467-486.
[2]. Fernández-Villa D, Aguilar M R, Rojo L. Folic acid antagonists: antimicrobial and immunomodulating mechanisms and applications[J]. International journal of molecular sciences, 2019, 20(20): 4996.
[3]. Cheong M S, Seo K H, Chohra H, et al. Influence of sulfonamide contamination derived from veterinary antibiotics on plant growth and development[J]. Antibiotics, 2020, 9(8): 456.
[4]. Petri W A. Sulfonamides, trimethoprim, sulfamethoxazole, quinolones, and agents for urinary tract infections[J]. Goodman & Gilman’s the pharmacological basis of therapeutics. New York (NY): McGraw Hill, 2006: 1111-1125.
[5]. Park H B, Wei Z, Oh J, et al. Sulfamethoxazole drug stress upregulates antioxidant immunomodulatory metabolites in Escherichia coli[J]. Nature microbiology, 2020, 5(11): 1319-1329.
[6]. Ogata H, Kitamura S, Fujiwara M, et al. Dose dependent effect of sulfamethoxazole on inhibiting KATP channel of mouse pancreatic β cell[J]. Dose-Response, 2023, 21(3): 15593258231203611.
[7]. Norose K, Aosai F, Mun H S, et al. Effects of sulfamethoxazole on murine ocular toxoplasmosis in interferon-γ knockout mice[J]. Investigative ophthalmology & visual science, 2006, 47(1): 265-271.
[8]. Xu Y, Luo L, Chen J. Sulfamethoxazole induces brain capillaries toxicity in zebrafish by up-regulation of VEGF and chemokine signalling[J]. Ecotoxicology and Environmental Safety, 2022, 238: 113620.
Sulfamethoxazole是一种抑菌磺酰胺类抗生素 [1]。Sulfamethoxazole竞争性抑制细菌二氢叶酸合酶（DHPS），阻断叶酸合成，从而干扰DNA和蛋白质合成 [2-3]。Sulfamethoxazole广泛用于治疗泌尿道感染、呼吸道感染和胃肠道感染 [4]。
在大肠杆菌中，Sulfamethoxazole（1.6mg/mL；24h）处理后，细菌活性受到显著抑制 [5]。在小鼠胰腺β细胞中，Sulfamethoxazole（0.1-10mM；3h）处理可抑制KATP通道电流，且这种抑制作用呈剂量依赖性 [6]。
在弓形虫感染的小鼠模型中，Sulfamethoxazole（300mg/kg；口服；24d）显著降低了感染的野生型C57BL/6小鼠和GKO小鼠的死亡率 [7]。在斑马鱼中，Sulfamethoxazole（250ppm；胚胎培养；5d）通过上调VEGF和趋化因子信号传导诱导脑毛细血管毒性 [8]。
| Antibacterial experiments [1]: | |
Bacterial | E. coli |
Preparation Method | E. coli strains were grown on LB agar plates [1% tryptone (w/v), 0.5% yeast extract (w/v), 1% sodium chloride (w/v), and 1.5% agar (w/v)] at 37℃ for 18h. Three well-defined colonies from each of the strains were inoculated into 5mL of LB broth and incubated at 37℃ with agitation (250rpm). Overnight E. coli cultures (5μL) were seeded into 5mL LB broth and were further grown for 18h. Sulfamethoxazole, when needed, was prepared in fresh LB medium with a highest concentration of 1.6mg/mL, which was then serially diluted. The 5mL of Sulfamethoxazole-containing medium was dispensed into 14mL sterile culture tubes, and 5μL of E. coli culture was inoculated and grown at 37℃ for 24h at 250rpm. The optical density (OD600) of cultures was measured, and growth curves were generated to determine sub-inhibitory levels of Sulfamethoxazole against E. coli. |
Reaction Conditions | 1.6mg/mL; 24h |
Applications | After Sulfamethoxazole treatment, the activity of E. coli was significantly inhibited. |
| Animal experiment [2]: | |
Animal models | Toxoplasma gondii infected mouse model |
Preparation Method | Wild-type (WT) C57BL/6 and WT BALB/c mice and interferon-γ knockout (GKO) mice were infected orally with Toxoplasma gondii of the Fukaya strain. Mice were classified into groups. The first group (G1) remained untreated, the second group (G2) had a short Sulfamethoxazole treatment period, and the third group (G3) received treatment continuously. WT and GKO mice were divided into G1 and G3, and G1, G2, and G3, respectively. T. gondii burdens were evaluated by QC-PCR assay. The effect on stage distribution was analyzed by reverse transcription-PCR. |
Dosage form | 300mg/kg; po; 24d |
Applications | Sulfamethoxazole significantly decreased mortality among the infected WT C57BL/6 and GKO mice. |
References: | |
| Cas No. | 723-46-6 | SDF | |
| 别名 | 磺胺甲恶唑; Ro 4-2130 | ||
| 化学名 | 4-amino-N-(5-methyl-1,2-oxazol-3-yl)benzenesulfonamide | ||
| Canonical SMILES | CC1=CC(=NO1)NS(=O)(=O)C2=CC=C(C=C2)N | ||
| 分子式 | C10H11N3O3S | 分子量 | 253.28 |
| 溶解度 | ≥ 7.75mg/mL in DMSO | 储存条件 | Store at 2-8°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。 |
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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 | 3.9482 mL | 19.741 mL | 39.482 mL |
| 5 mM | 0.7896 mL | 3.9482 mL | 7.8964 mL |
| 10 mM | 0.3948 mL | 1.9741 mL | 3.9482 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。
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Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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