Bioactivity | HSGN-94 is a potent antimicrobial agent with lipoteichoic acid (LTA) biosynthesis inhibition. HSGN-94 inhibits drug-resistant Gram-positive bacteria with MIC values of 0.25-2 μg/mL. HSGN-94 inhibits biofilm formation of MRSA and Vancomycin-resistant Enterococci. HSGN-94 also inhibits pro-inflammatory cytokines, exhibits in vivo efficacy in an MRSA murine wound infection model[1]. |
Invitro | HSGN-94(50 μM;30 分钟)直接结合 CDP-二酰基甘油-甘油-3-磷酸-3-磷脂酰转移酶 (PgsA)[1]。HSGN-94(0.25 μg/mL;2 小时)下调 PgsA 的表达水平,PgsA 是细菌中磷脂合成的必需蛋白质[1]。HSGN-94(16、32、64 和 128 μg/mL;2 小时)在浓度高达 64 μg/mL 时对 HaCat 细胞没有毒性[1]。 |
In Vivo | HSGN-94(2%;外用;每天两次,持续 5 天)减少小鼠受感染伤口中的 MRSA USA300,并导致感染模型中的炎症消退[1]。 Animal Model: |
Name | HSGN-94 |
Formula | C23H23F3N4O4S |
Molar Mass | 508.51 |
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]. Naclerio GA, et al. Mechanistic Studies and In Vivo Efficacy of an Oxadiazole-Containing Antibiotic. J Med Chem. 2022 May 12;65(9):6612-6630. |