NLRP3-IN-2 是合成格列本脲的中间底物，可抑制心肌细胞中NLRP3炎症小体的形成，在小鼠心肌缺血/再灌注后限制梗死面积，且不影响代谢。
| 生物活性 | NLRP3-IN-2, an intermediate substrate in the synthesis of glyburide, inhibits the formation of theNLRP3inflammasome in cardiomyocytes and limits the infarct size following myocardial ischemia/reperfusion in the mouse, without affecting glucose metabolism[1]. |
体内研究
(In Vivo) | NLRP3-IN-2 is well tolerated with no effects on the glucose levels in vivo[1].
NLRP3-IN-2 (100 mg/kg) treatment in a model of AMI due to ischemia+reperfusion significantly inhibits the activity of inflammasome (caspase-1) in the heart by 90% (P<0.01) and reduced infarct size, measured at pathology (by >40%, P<0.01) and with troponin I levels (by >70%, P<0.01)[1].
| Animal Model: | Experimental acute myocardial infarction (AMI) model in mice[1]. | | Dosage: | 100 mg/kg. | | Administration: | Intraperitoneal administration 30 minutes prior to surgery, then every 6 hours for 3 additional doses. | | Result: | Led to a significant >90% reduction in caspase-1 activity (reflective of the formation of an active inflammasome) in the heart tissue measured 24 hours after ischemia.
Led to a significant reduction in the infarct size measured with TTC (>40% reduction) or troponin I levels (>70% reduction) when compared with vehicle alone.
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| 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 | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(338.90 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.7112 mL | 13.5560 mL | 27.1120 mL | | 5 mM | 0.5422 mL | 2.7112 mL | 5.4224 mL | | 10 mM | 0.2711 mL | 1.3556 mL | 2.7112 mL |
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储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-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: ≥ 2.08 mg/mL (5.64 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.64 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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%corn oil Solubility: ≥ 2.08 mg/mL (5.64 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (5.64 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 20.8 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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