| Description |
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].
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| Related Catalog |
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| In Vitro |
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]。
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| 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: MRSA murine wound infection model[1] Dosage: 2% Administration: External use; twice daily for 5 days Result: Reduced the levels of the pro-inflammatory cytokines, monocyte chemo attractant protein-1 (MCP-1), tumor necrosis factor-α (TNF-α), and interleukin-1 beta (IL-1β) in MRSA USA300 skin lesions.
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| References |
[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.
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