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编 号:F618186
分子式:C17H20BrN3O3S2
分子量:458.39
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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生物活性:
T6167923 is a selective inhibitor of MyD88-dependent signaling pathways. T6167923 directly binds to Toll/IL1 receptor (TIR) domain of MyD88 and disrupts MyD88 homodimeric formation. T6167923 inhibits NF-κB driven Staphylococcus enterotoxin AP (SEAP) activity, and improves anti-inflammatory activity with IC50s of 2.7 ?μM, 2.9 μM, 2.66 μM and 2.66 μM for IFN-γ, IL-1β, IL-6 and TNF-α, respectively.

体内研究:
T6167923 (0.17 and 1 mg; i.p. once) survives the mice from intoxication with SEB and LPS injection.Animal Model:16-20 week-old BALB/c mice with LPS potentiation model
Dosage:0.17 and 1 mg
Administration:Intraperitoneal injection; 0.17 and 1 mg once
Result:Dose-dependently showed a therapeutic efficacy against SEB intoxication.

体外研究:
T6167923 (0-500 μM; 20 h) inhibits the pro-inflammatory cytokine response of staphylococcal enterotoxin B (SEB) in peripheral blood mono nuclear cells.T6167923 (10-500 μM; 2 h) inhibits secreted alkaline phosphatase response (SEAP) expression in HEK 293T cells.T6167923 (100 μM; 16 h) binds to TIR protein and reduced the inhibitory effect onMyD88-signaling.T6167923 (1-500 μM; 13 h) inhibits full-length MyD88 homodimeric formation.
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