Cloxacillin Sodium|7081-44-9|(氯唑西林钠一水合物)-陌孚医药/Medlife

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Cloxacillin Sodium (Synonyms: 氯唑西林钠一水合物)

目录号: PC11709 纯度: ≥98%

CAS No. :7081-44-9

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中文名称	Cloxacillin Sodium
中文别名	3,3-二甲基-6-[5-甲基-3-(2-氯苯基)-4-异噁唑甲酰氨基]-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-甲酸钠盐
英文名称	Cloxacillin Sodium
英文别名	Sodium 6-[3-(2-chlorophenyl)-5-methyl-oxazol-4-yl]carbonylamino-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate hydrate
Cas No.	7081-44-9
分子式	C₁₉H₁₇N₃O₅Scl-^.Na+^.H₂O
分子量	475.88
包装储存	4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

生物活性

Cloxacillin sodium monohydrate is an orally active antibacterial agent and β-lactamase inhibitor with an IC₅₀ of 0.04 μM. Cloxacillin sodium monohydrate can suppress the S. aureus-induced inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.

性状

Solid

IC50 & Target[1][2]

Tetracycline

体外研究(In Vitro)

Cloxacillin sodium monohydrate (0-2048 μg/mL; 20-24 h) shows good antibacterial activity for S. aureus 8325-4 and DU1090 with MIC values both of 0.125 μg/mL.
Cloxacillin sodium monohydrate (0.015625 μg/mL; 6 h) inhibits the hemolytic activity of Hlα 体外研究, and this inhibition is not only more pronounced when combined with TZ and TZ, but also suppresses the inflammatory response by inhibiting the activation of MAPKs, NF-кB and NLRP3-related proteins.

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

Cell Viability Assay

Cell Line:	S. aureus 8325-4, S. aureus DU1090 (an Hlα-deleted strain)
Concentration:	0-2048 μg/mL
Incubation Time:	20-24 h
Result:	Inhibited S. aureus 8325-4 and DU1090 with MIC values both of 0.125 μg/mL.

Western Blot Analysis

Cell Line:	S. aureus 8325-4
Concentration:	0.015625 μg/mL (combines with Thioridazine (TZ, 0.25 μg/mL) and Tetracycline (TC, 0.03125 μg/mL)).
Incubation Time:	6 h
Result:	Inhibited the expression of Hlα and the inhibition was more pronounced when combined with TZ and TC.

Western Blot Analysis

Cell Line:	RAW264.7 cells (exposes to S. aureus 8325-4/DU1090 or pure Hlα)
Concentration:	0.015625 μg/mL (combines with TZ (0.25 μg/mL) and TC (0.03125 μg/mL)).
Incubation Time:	6 h
Result:	Inhibited the activation of MAPKs, NF-кB and NLRP3-related proteins thereby inhibiting the inflammatory response when combined with TC and TZ.

体内研究(In Vivo)

Cloxacillin sodium monohydrate (1.6125 mg/kg; s.c.; 12-h intervals for 72 h) protects mice from S. aureus peritonitis in vivo when combines with Thioridazine and Tetracycline.
Cloxacillin sodium monohydrate (7.5 mg/per; i.p.; twice daily from day 3 for 3 days) develops less severe synovitis and reduces bone erosions when combines with anti-IL-15 antibodies.

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

Animal Model:	Female BALB/c mice (6-week-old; peritonitis model).
Dosage:	1.6125 mg/kg (combines with TC (3.125 mg/kg) and TZ (25 mg/kg))
Administration:	Subcutaneous injection; 12-h intervals for 72 h.
Result:	Reduced the degree of inflammatory cell infiltration in the mouse lung tissue and alveolar structures tended to be normal. Significantly reduced the pathological changes in spleen and liver tissue, as well as decreased the CFU counts of S. aureus in the peritoneal cavity.

Animal Model:	Female wildtype C57BL/6 mice (8-week-old; systemic S. aureus-induced arthritis model)
Dosage:	7.5 mg/per (combines with 25 μg/per anti-IL-15 antibodies)
Administration:	Intraperitoneal injection; twice daily from day 3 (after bacterial inoculation) and stopped at day 6.
Result:	Showed activities of reducing severe synovitis and bone erosions when combined with anti-IL-15 antibodies.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

ClinicalTrial

参考文献

[1]. Zhou H, et al. The combination of cloxacillin, thioridazine and tetracycline protects mice against Staphylococcus aureus peritonitis by inhibiting α-Hemolysin-induced MAPK/NF-κB/NLRP3 activation. Int J Biol Macromol. 2022 Feb 15;198:1-10. [Information]

[2]. Bergmann B, et al. Antibiotics with Interleukin-15 Inhibition Reduce Joint Inflammation and Bone Erosions but Not Cartilage Destruction in Staphylococcus aureus-Induced Arthritis. Infect Immun. 2018 Apr 23;86(5):e00960-17. [Information]

[3]. Lupiola-Gómez PA, et al. Group 1 beta-lactamases of Aeromonas caviae and their resistance to beta-lactam antibiotics. Can J Microbiol. 2003 Mar;49(3):207-15. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (210.14 mM; Need ultrasonic)

H₂O : 50 mg/mL (105.07 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1014 mL	10.5069 mL	21.0137 mL
5 mM	0.4203 mL	2.1014 mL	4.2027 mL
10 mM	0.2101 mL	1.0507 mL	2.1014 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (210.14 mM); Clear solution; Need ultrasonic
2.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
3.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.25 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.25 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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Data Sheet

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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