| Bioactivity | KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis[1]. | ||||||||||||
| Target | IC50: 750 nM (NFAT5). | ||||||||||||
| Invitro | 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[1].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[1]. | ||||||||||||
| In Vivo | 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[1].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[1]. Animal Model: | ||||||||||||
| Name | KRN5 | ||||||||||||
| CAS | 1800465-47-7 | ||||||||||||
| Formula | C27H22FNO5 | ||||||||||||
| Molar Mass | 459.47 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Han EJ, et al. Suppression of NFAT5-mediated Inflammation and Chronic Arthritis by Novel κB-binding Inhibitors. EBioMedicine. 2017 Apr;18:261-273. |