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KRM-III 是一种有效的具有口服活性的 T 细胞抗原受体 (TCR) 抑制剂。KRM-III 抑制 TCR 和肉豆蔻酸乙酸酯/佛波霉素/离子霉素诱导的 NFAT 核因子活化和 T 细胞增殖,IC50 约为 5 μM。抗炎活性。
KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity[1].
[1]. Eun Joo Jung, et al. Oral administration of 1,4-aryl-2-mercaptoimidazole inhibits T-cell proliferation and reduces clinical severity in the murine experimental autoimmune encephalomyelitis model. J Pharmacol Exp Ther. 2009 Dec;331(3):1005-13.
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