KRN5|1800465-47-7|-陌孚医药/Medlife

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KRN5

目录号: PL07884 纯度: ≥98%

CAS No. :1800465-47-7

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中文名称	KRN5
英文名称	KRN5
英文别名	KRN5
Cas No.	1800465-47-7
分子式	C₂₇H₂₂FNO₅
分子量	459.47
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	KRN5 是 KRN2 的衍生物，是具有口服活性的 T 细胞激活核因子 (NFAT5) 的抑制剂，IC₅₀ 值为 750 nM。KRN5 有潜力用于 NFAT5-介导的慢性关节炎的研究。
生物活性	KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC 50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis.
性状	Solid
IC50 & Target[1][2]	IC50: 750 nM (NFAT5).
体外研究(In Vitro)	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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(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. 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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Han EJ, et al. Suppression of NFAT5-mediated Inflammation and Chronic Arthritis by Novel κB-binding Inhibitors. EBioMedicine. 2017 Apr;18:261-273.

溶解度数据	In Vitro: DMSO : 5 mg/mL (10.88 mM; ultrasonic and warming and heat to 80°C)配制储备液

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