Cloxacillin sodium monohydrate 是一种口服有效的抗菌剂和β-lactamase抑制剂,其IC50值为 0.04 μM。Cloxacillin sodium monohydrate 可通过抑制MAPKs、NF-кB和NLRP3相关蛋白的激活从而抑制金黄色葡萄球菌所引起的炎症反应。
生物活性 | Cloxacillin sodium monohydrate is an orally activeantibacterialagent andβ-lactamaseinhibitor with anIC50of 0.04 μM. Cloxacillin sodium monohydrate can suppress theS. aureus-induced inflammatory response by inhibiting the activation ofMAPKs,NF-кBandNLRP3-related proteins[1][2][3]. |
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体外研究 (In Vitro) | Cloxacillin sodium monohydrate (0-2048 μg/mL; 20-24 h) shows good antibacterial activity forS. aureus8325-4 and DU1090 with MIC values both of 0.125 μg/mL[1]. Cloxacillin sodium monohydrate (0.015625 μg/mL; 6 h) inhibits the hemolytic activity of Hlα in vitro, 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[1].
Cell Viability Assay[1] Cell Line: | S. aureus8325-4,S. aureusDU1090 (an Hlα-deleted strain) | Concentration: | 0-2048 μg/mL | Incubation Time: | 20-24 h | Result: | InhibitedS. aureus8325-4 and DU1090 with MIC values both of 0.125 μg/mL. |
Western Blot Analysis[1] Cell Line: | S. aureus8325-4 | 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[1] Cell Line: | RAW264.7 cells (exposes toS. aureus8325-4/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. |
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体内研究 (In Vivo) | Cloxacillin sodium monohydrate (1.6125 mg/kg; s.c.; 12-h intervals for 72 h) protects mice fromS. aureusperitonitis in vivo when combines with Thioridazine and Tetracycline[1]. 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[3].
Animal Model: | Female BALB/c mice (6-week-old; peritonitis model)[1]. | 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 ofS. aureusin the peritoneal cavity. |
Animal Model: | Female wildtype C57BL/6 mice (8-week-old; systemicS. 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. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
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) |
溶解性数据 | In Vitro: DMSO : 100 mg/mL(210.14 mM;Need ultrasonic) H2O : 50 mg/mL(105.07 mM;Need ultrasonic) 配制储备液 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 |
*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℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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. 请依序添加每种溶剂: PBS Solubility: 100 mg/mL (210.14 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂: 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。 3. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 4. 请依序添加每种溶剂: 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。 *以上所有助溶剂都可在本网站选购。
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