KRN5

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KRN5 具有治疗 NFAT5 介导的慢性关节炎的潜力。 KRN5 是 KRN2 的衍生物，是一种口服活性活化 T 细胞核因子 5 (NFAT5) 抑制剂，IC50 为 750 nM。

KRN5 has potential to treat NFAT5-mediated Chronic Arthritis. KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM.(In Vitro):KRN5 (1 μM) inhibits the expressions of NFAT5, IL-6,MCP-1, and GM-CSF in RAW264.7 macrophages stimulated with LPS.(In Vivo):In DBA/1Jmice immunized with bovine type II collagen, KRN5 (15 and 60 mg/kg; oral) dose-dependently mitigates arthritis severity. KRN5 significantly decreases the concentration of serum anti-type II collagen IgG in the sera. KRN5 lowers TNF-α and IL-6 production by LPS-stimulated splenocytes in mice.

KRN5 is less toxic than BBR as determined by a cytotoxicity assay, hERG K+ channel assay, cytochrome inhibition assay, and liver microsomal metabolic stability test, which makes it a potential drug candidate.KRN5 at a concentration of 1 μM inhibits the expressions of NFAT5, IL-6,MCP-1, and GM-CSF,which are NFAT5 target molecules, in RAW264.7 macrophages stimulated with LPS.

Oral feeding of KRN5 (15 mg/kg and 60 mg/kg) every other day for 3 weeks from day 21 dose-dependently mitigates arthritis severity.The concentration of serum anti-type II collagen IgG also significantly decreases in the sera of KRN5-treated mice. TNF-α and IL-6 production by LPS-stimulated splenocytes are significantly lower in KRN5-treated CIA mice than in vehicle-treated mice. Animal Model:8-week-old DBA/1Jmice immunized with bovine type II collagen.Dosage:15 mg/kg and 60 mg/kg.Administration:Orally on alternate days (every other day) for 3 weeks.Result:Dose-dependently mitigated arthritis severity.

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Others

Other Targets

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1800465-47-7

459.473

C27H22FNO5

>98% (HPLC)

In Vitro:?DMSO : 5 mg/mL (10.88 mM)

COc1ccc2c(Cc3ccccc3F)c3-c4cc5OCOc5cc4CCn3c(=O)c2c1OC

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(-20℃)

With Ice Pack

≥ 2 years