
KRN5
CAS No. 1800465-47-7
KRN5 ( —— )
产品货号. M26570 CAS No. 1800465-47-7
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。
纯度: >98% (HPLC)






规格 | 价格/人民币 | 库存 | 数量 |
5MG | ¥7857 | 有现货 |
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100MG | 获取报价 | 有现货 |
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200MG | 获取报价 | 有现货 |
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500MG | 获取报价 | 有现货 |
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1G | 获取报价 | 有现货 |
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生物学信息
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产品名称KRN5
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注意事项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
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产品简述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。
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产品描述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.
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体外实验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.
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体内实验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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同义词——
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通路Others
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靶点Other Targets
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受体——
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研究领域——
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适应症——
化学信息
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CAS Number1800465-47-7
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分子量459.473
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分子式C27H22FNO5
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO : 5 mg/mL (10.88 mM)
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SMILESCOc1ccc2c(Cc3ccccc3F)c3-c4cc5OCOc5cc4CCn3c(=O)c2c1OC
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.ThomasBriggs, et al. Allocholic acid, the major component in bile from the river carpsucker, Carpiodes carpio (Rafinesque) (Catostomidae). Comp Biochem Physiol B. 1972 Jul 15;42(3):493-6.
产品手册




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