Secnidazole (RP-14539) 是一种唑类抗生素和黏质沙雷菌毒力的咪唑缓释剂，具有口服活性。Secnidazole 作为一种类似于酰基高丝氨酸内酯，能有效抑制 QS 导致铜绿假单胞菌的发病衰减。Secnidazole 在体外对多种厌氧革兰氏阴性和革兰氏阳性细菌均有抗菌活性。Secnidazole 可用于各种疾病的研究，如阿米巴病和贾第虫病，以及细菌性阴道炎。
| 生物活性 | Secnidazole (RP-14539) is an orally active azoleantibioticand a imidazole mitigator ofSerratia marcescensvirulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation ofPseudomonas aeruginosapathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positivebacterialspecies in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, andbacterialvaginitis[1][2][3]. |
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体外研究
(In Vitro) | Secnidazole (RP-14539) (0-5000 μM; 5 or 10 min) inhibits CYP2C19 and CYP3A4, with IC50values of 3873 μM and 3722 μM, respectively[2].
Secnidazole (0-5000 μM; 5 or 10 min) does not exhibit time-dependent inhibition[2].
Secnidazole (0-5000 μM; 5 or 10 min) has an apparent IC50value of 503 μM for direct inhibition of human ALDH2[2].
Secnidazole (0-5000 μM; 5 or 10 min) has concentration-dependent inhibition at higher concentration with some of the CYP isoforms notably CYP2A6, CYP2B6, and CYP2D6[2].
Secnidazole (10 μL; 20 h; the secnidazole solution was two-fold serially diluted using Mueller–Hinton broth to obtain dilutions ranging from 80 to 0.3125 mg/mL) inhibitsS.marcescensgrowth with a MIC50value of 10 mg/mL[3].
Cell Viability Assay[3] | Cell Line: | S.marcescens | | Concentration: | 10 μL (the secnidazole solution was two-fold serially diluted using Mueller–Hinton broth to obtain dilutions ranging from 80 to 0.3125 mg/mL) | | Incubation Time: | 20 h | | Result: | Had no inhibitory effect onS.marcescensgrowth at 2 mg/mL (equivalent to 1/5 MIC). |
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体内研究
(In Vivo) | Secnidazole (100 μL; ip.; for 5 days) has protective activity againstS.marcescenspathogenesis and can diminish its pathogenesis in mice[3].
| Animal Model: | Female healthy albino mice[3] | | Dosage: | 100 μL | | Administration: | 100 μL; ip.; for 5 days | | Result: | Significantly diminished the bacteria s capacity to kill mice. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : ≥ 30 mg/mL(162.00 mM) H2O : 25 mg/mL(135.00 mM;Need ultrasonic) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 5.4002 mL | 27.0008 mL | 54.0015 mL | | 5 mM | 1.0800 mL | 5.4002 mL | 10.8003 mL | | 10 mM | 0.5400 mL | 2.7001 mL | 5.4002 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-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: 50 mg/mL (270.01 mM); Clear solution; Need ultrasonic
*以上所有助溶剂都可在本网站选购。 |
