KRN2 是选择性的 T 细胞激活核因子 (NFAT5) 的抑制剂，IC50值为 100 nM。KRN2 有潜力用于 NFAT5-介导的慢性关节炎的潜能。
| 生物活性 | KRN2 is a selective inhibitor ofnuclear factor of activated T cells(NFAT5), with anIC50of 100 nM. KRN2 has potential to treat NFAT5-mediated Chronic Arthritis[1]. |
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体外研究
(In Vitro) | KRN2 selectively suppresses the expression of pro-inflammatory genes, including Nos2 and Il6, without hampering high-salt-induced NFAT5 and its target gene expressions[1].
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) ofNfat5exon 1[1].
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体内研究
(In Vivo) | KRN2 (3 mg/kg, i.p., daily for 2 weeks) effectively suppresses AIA in which innate immune cells play a predominant role[1].
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[1].
| Animal Model: | 8-week-old C57BL/6 mice injected intradermally with 2 mg of complete Freund's adjuvant[1]. | | 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[1]. | | 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. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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