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Secnidazole hemihydrate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Secnidazole hemihydrate图片
CAS NO:227622-73-3

塞克硝唑半水合物
RP-14539 hemihydrate
PM-185184 hemihydrate
Secnidazole (RP-14539) hemihydrate 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 hemihydrate 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 hemihydrate 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 hemihydrate 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) hemihydrate is an orally active azoleantibioticand a imidazole mitigator ofSerratia marcescensvirulence. Secnidazole hemihydrate, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation ofPseudomonas aeruginosapathogenesis. Secnidazole hemihydrate has antimicrobial activity against many anaerobic Gram-negative and Gram-positivebacterialspecies in vitro. Secnidazole hemihydrate can be used for the research of various diseases, such as amoebiasis and giardiasis, andbacterialvaginitis[1][2][3].

IC50& Target

Amebae

 

体外研究
(In Vitro)

Secnidazole (RP-14539) hemihydrate (0-5000 μM; 5 or 10 min) inhibits CYP2C19 and CYP3A4, with IC50values of 3873 μM and 3722 μM, respectively[2].
Secnidazole hemihydrate (0-5000 μM; 5 or 10 min) does not exhibit time-dependent inhibition[2].
Secnidazole hemihydrate (0-5000 μM; 5 or 10 min) has an apparent IC50value of 503 μM for direct inhibition of human ALDH2[2].
Secnidazole hemihydrate (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 hemihydrate (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).
体内研究
(In Vivo)

Secnidazole (RP-14539) hemihydrate (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.
Clinical Trial
分子量

194.19

Formula

C7H13N3O4

CAS 号

227622-73-3

中文名称

塞克硝唑半水合物

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

 
 
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