PKM2-IN-3

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PKM2-IN-3

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

2408841-19-8

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

PKM2-IN-3 是PKM2激酶的抑制剂，IC₅₀值为 4.1 μM。PKM2-IN-3 通过抑制 PKM2 介导的糖酵解和 NLRP3 激活，具有抗神经炎症的作用。

生物活性

PKM2-IN-3 is an inhibitor ofPKM2 kinasewith anIC₅₀value of 4.1 μM. PKM2-IN-3 exhibits an anti-neuroinflammatory effect by inhibiting PKM2-mediated glycolysis andNLRP3activation^[1].

IC₅₀& Target^[1]

PKM2

4.1 μM (IC₅₀)

体外研究
(In Vitro)

PKM2-IN-3 (compound 10i) inhibits the TNF-α release of LPS-stimulated RAW264.7 macrophages, with an IC₅₀value of 5.2 μM. PKM2-IN-3 exhibits the lowest toxicity with a CC₅₀value 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 IC₅₀value of 4.1 μM^[1].

体内研究
(In Vivo)

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.

分子量

338.40

Formula

C₂₁H₂₂O₄

CAS 号

2408841-19-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.