TLR4-C34 is a TLR4 inhibitor that inhibits TLR4 signaling in enterocytes and macrophages in vitro. 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.
CAS Number: 40592-88-9
Molecular Weight: 389.40
TLR4 C 34
Toll-Like Receptor 4-C34
Chemical Name: (2R,3S,4R,5R,6S)-5-acetamido-2-(acetoxymethyl)-6-isopropoxytetrahydro-2H-pyran-3,4-diyl diacetate
Appearance: Solid Power.
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: Soluble in DMSO
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined.
HS Tariff Code: 382200
How to use
TLR4-IN-C34 (C34, 1 mg/kg, orally daily) could attenuate NEC severity and demonstrates a marked preservation of the intestinal mucosa.
- Neal MD, et al. Discovery and validation of a new class of small molecule Toll-like receptor 4 (TLR4) inhibitors. PLoS One. 2013 Jun 12;8(6):e65779.
- Wipf P, et al. Synthesis of anti-inflammatory α-and β-linked acetamidopyranosides as inhibitors of toll-like receptor 4 (TLR4). Tetrahedron Lett. 2015 Jun 3;56(23):3097-3100.
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