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编 号:F147318
分子式:C27H23BrFNO4
分子量:524.38
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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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25mg
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50mg
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100mg
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生物活性:
KRN2 (bromide) is a selective inhibitor of nuclear factor of activated T cells (NFAT5), with an IC50 of 0.1 μM.

体内研究:
KRN2 (3 mg/kg, i.p., daily for 2 weeks) effectively suppresses AIA in which innate immune cells play a predominant role.KRN2 (3 mg/kg, i.p., daily) effectively suppresses CIA as well as AIA in mice, decreasing the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration.Animal Model:8-week-old C57BL/6 mice injected intradermally with 2 mg of complete Freund's adjuvant.
Dosage:3 mg/kg.
Administration:Peritoneally (i.p.) daily for 2 weeks.
Result:Effective in suppressing AIA.
Animal Model:8-week-old DBA/1Jmice immunized with bovine type II collagen.
Dosage:3 mg/kg.
Administration:Peritoneally (i.p.) daily.
Result:Effective in suppressing CIA as well as AIA in mice, decreasing the production of pro-inflammatory cytokines and autoantibodies as well as macrophage infiltration.

体外研究:
KRN2 selectively suppresses the expression of pro-inflammatory genes, including Nos2 and Il6, without hampering high-salt-induced NFAT5 and its target gene expressions.KRN2 dose-dependently inhibits the NF-κB p65 binding to Nfat5 promoter 1 and directly blocks the interaction between NF-κB p65 and its DNA binding sequence in the upstream site (base pairs -3000 to +1) of Nfat5 exon 1.
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