Secnidazole

Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis^[1][2][3]. IC50 & Target:IC50: 3873μM (CYP2C19), 3722 μM (CYP3A4), 503 μM (ALDH2)^[2].
MIC50: 10mg/mL (S.marcescens)^[3]. In Vitro: Secnidazole (RP-14539) (0-5000 μM; 5 or 10 min) inhibits CYP2C19 and CYP3A4, with IC₅₀ values 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 IC₅₀ value 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) inhibits S.marcescens growth with a MIC₅₀ value of 10 mg/mL^[3]. In Vivo: Secnidazole (100 μL; ip.; for 5 days) has protective activity against S.marcescens pathogenesis and can diminish its pathogenesis in mice^[3].