中文名稱:PKM2-IN-3 | 英文名稱:PKM2-IN-3 |
CAS:2408841-19-8 | 品牌: TargetMol |
產(chǎn)地: 美國(guó) | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
產(chǎn)品類別: 抑制劑 | |
貨號(hào): T39984 |
名稱 | PKM2-IN-3 |
描述 | PKM2-IN-3 is a potent PKM2 kinase inhibitor, displaying an IC 50 value of 4.1 μM. The compound effectively suppresses PKM2-mediated glycolysis and NLRP3 activation, thereby exerting an anti-neuroinflammatory effect. |
體外活性 | PKM2-IN-3 (compound 10i) inhibits the TNF-α release of LPS-stimulated RAW264.7 macrophages, with an IC 50 value of 5.2 μM. PKM2-IN-3 exhibits the lowest toxicity with a CC 50 value of 43.6 μM[1]. PKM2-IN-3 (0.1-100 μM; 20 min) inhibits PKM2 kinase activity in a cell-free molecular level with an IC 50 value of 4.1 μM[1]. |
體內(nèi)活性 | PKM2-IN-3 (1, 10 mg/kg; i.p.; daily for 3 days ) significantly reverses the LPS-induced mice behavior changes in open field test[1]. PKM2-IN-3 (1, 10 mg/kg; i.v.; injected at 4 hours and 24 hours after ischemia onset) reduces the infarct volume and improves neurological deficits of tMCAO rats[1]. Animal Model: LPS-induced mice (male 6-8 weeks old; 20.0-22.0 g)[1]Dosage: 1, 10 mg/kg Administration: i.p.; daily for 3 days Result: Reversed the LPS-induced mice behavior changes in open field test. Animal Model: tMCAO Sprague-Dawley rats (Male 8-10 weeks old; 250.0-280.0 g)[1]Dosage: 1, 10 mg/kg Administration: i.v.; injected at 4 hours and 24 hours after ischemia onset Result: Reduced the infarct volume and improved neurological deficits of tMCAO rats. |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
關(guān)鍵字 | PKM2 IN 3 | PKM2IN3 | PKM-2-IN-3 |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 589.8595萬(wàn)人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)行業(yè) | 中間體,天然產(chǎn)物,生物化工,化學(xué)試劑,生物技術(shù)服務(wù) | 經(jīng)營(yíng)模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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