KRN2 bromide 是选择性的 T 细胞激活核因子 (NFAT5) 的抑制剂,IC50值为 100 nM。KRN2 bromide 有潜力用于 NFAT5-介导的慢性关节炎的潜能。
生物活性 | KRN2 (bromide) is a selective inhibitor ofnuclear factor of activated T cells(NFAT5), with anIC50of 0.1 μM. |
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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 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
溶解性数据 | In Vitro: DMSO : 18.33 mg/mL(34.96 mM;Need ultrasonic) H2O : 1.1 mg/mL(2.10 mM;Need ultrasonic) 配制储备液 1 mM | 1.9070 mL | 9.5351 mL | 19.0701 mL | 5 mM | 0.3814 mL | 1.9070 mL | 3.8140 mL | 10 mM | 0.1907 mL | 0.9535 mL | 1.9070 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 1.83 mg/mL (3.49 mM); Clear solution
此方案可获得 ≥ 1.83 mg/mL (3.49 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 18.3 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 1.83 mg/mL (3.49 mM); Clear solution
此方案可获得 ≥ 1.83 mg/mL (3.49 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 18.3 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 1.83 mg/mL (3.49 mM); Clear solution
此方案可获得 ≥ 1.83 mg/mL (3.49 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 18.3 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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