生物活性 | |||
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描述 | The innate immune receptor toll-like receptor 4 (TLR4) is a pattern recognition receptor expressed in both hematopoietic and non-hematopoietic cells. C34 is a 2-acetamidopyranoside that inhibits TLR4 in IEC-6 enterocytes and RAW264.7 macrophages in vitro at a dosage of 10μM. Pretreatment with 1mg/kg C34 30 minutes before LPS (3mg/kg) injection significantly reduced luciferase activity in mice. In a mouse model of experimental necrotizing enterocolitis (NEC), oral gavage of C34 (1mg/kg/day) for 4 days attenuated the severity of NEC as demonstrate by marked preservation of the intestinal mucosa, downregulation of pro-inflammatory iNOS expression, and reduced NEC severity score. C34 at 10μM inhibited TLR4 signaling ex vivo in human tissues isolated from infants with NEC[2]. | ||
作用机制 | C34 is an inhibitor of TLR4 that docks into the hydrophobic internal pocket of the TLR4 co-receptor MD-2[2]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.57mL 0.51mL 0.26mL |
12.84mL 2.57mL 1.28mL |
25.68mL 5.14mL 2.57mL |
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