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编 号：F752136
分子式：C21H22O4
分子量：338.4
分子式：C21H22O4
分子量：338.4
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CAS No: 2408841-19-8
产品详情
生物活性：
PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.
体内研究：
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.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.Animal Model:LPS-induced mice (male 6-8 weeks old; 20.0-22.0 g)
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)
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.
体外研究：
PKM2-IN-3 (compound 10i) inhibits the TNF-α release of LPS-stimulated RAW264.7 macrophages, with an IC50 value of 5.2 μM. PKM2-IN-3 exhibits the lowest toxicity with a CC50 value of 43.6 μM.PKM2-IN-3 (0.1-100 μM; 20 min) inhibits PKM2 kinase activity in a cell-free molecular level with an IC50 value of 4.1 μM.
PKM2-IN-3 is an inhibitor of PKM2 kinase with an IC50 value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis and NLRP3 activation.
体内研究：
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.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.Animal Model:LPS-induced mice (male 6-8 weeks old; 20.0-22.0 g)
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)
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.
体外研究：
PKM2-IN-3 (compound 10i) inhibits the TNF-α release of LPS-stimulated RAW264.7 macrophages, with an IC50 value of 5.2 μM. PKM2-IN-3 exhibits the lowest toxicity with a CC50 value of 43.6 μM.PKM2-IN-3 (0.1-100 μM; 20 min) inhibits PKM2 kinase activity in a cell-free molecular level with an IC50 value of 4.1 μM.
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