Bioactivity | Antifungal agent 22 (compound D16) is a potential and orally active antifungal agent for CM (cryptococcal meningitis), with an IC50 of 0.5 μg/mL. Antifungal agent 22 can penetrate the blood-brain barrier and kill the C. neoformans H99 cells by destroying the integrity of fungal cell membranes. Antifungal agent 22 shows selective anti-Cryptococcus activity with good metabolic stability and low cytotoxicity[1]. |
Target | IC50: 0.5 μg/mL (Fungal). |
Invitro | Antifungal agent 22 (compound D16) (0-1 μg/mL, 24 h) inhibits ergosterol biosynthesis, which results in stress-induced upregulation of ERG genes in C. neoformans H99[1].Antifungal agent 22 (0-8 μg/mL) effectively inhibits the growth of C. neoformans H99 (0-72 h), inhibits the formation of C. neoformans H99 biofilms in a concentration-dependent manner (24 h)[1].Antifungal agent 22 (0-8 μg/mL, 48-72 h) shows selective anti-Cryptococcus activity, has a fungistatic effect[1].Antifungal agent 22 (0-100 μM, 48 h) shows low cytotoxicity against a human HUVEC cell line with an IC50 of 20.18 μM[1]. Cell Proliferation Assay Cell Line: |
In Vivo | Antifungal agent 22 (D16) (15 mg/kg, Intragastrically, daily for 5 days) shows potent anti-Cryptococcal efficacy[1]. Animal Model: |
Name | Antifungal agent 22 |
CAS | 2640054-39-1 |
Formula | C21H26Cl3NOS |
Molar Mass | 446.86 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Li W, Yun Z, Ji C, et al. Discovery of Novel Sertraline Derivatives as Potent anti-Cryptococcus Agents.J Med Chem. 2022 Mar 6;10.1021/acs.jmedchem.1c01845. |