Anti-inflammatory agent 35,229

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Anti-inflammatory agent 35

CAS No. : 2293951-00-3

MCE 国际站：Anti-inflammatory agent 35

产品活性：Anti-inflammatory agent 35 (化合物 5a27) 是一种口服有效的姜黄素类似物，具有抗炎活性。Anti-inflammatory agent 35 可阻断丝裂原活化蛋白激酶 (MAPK) 信号和 NF-kB 的核易位。Anti-inflammatory agent 35 还抑制黄中性粒细胞浸润和促炎细胞因子产生。Anti-inflammatory agent 35 在体内研究中显著减轻脂多糖 (LPS) 诱导的急性肺损伤 (ALI)。

研究领域：MAPK/ERK Pathway  |  Stem Cell/Wnt  |  NF-κB  |  Immunology/Inflammation  |  Apoptosis

作用靶点：p38 MAPK  |  ERK  |  NF-κB  |  Interleukin Related  |  TNF Receptor

In Vitro: Anti-inflammatory agent 35 (compound 5a27) (10 μM; 30 min) inhibits the production of proinflammatory cytokines (IL-6, TNF-α) induced by LPS (0.5 μg/mL; 24 h) without cytotoxicity in mouse primary macrophages (MPMs). Anti-inflammatory agent 35 inhibits the production of IL-6, TNF-α with IC50s of 2.23 μM and 2.40 μM, respectively.
Anti-inflammatory agent 35 (10 μM; 30 min) significantly inhibits LPS-induced activation in RAW 264.7 mouse macrophages. And it markedly inhibits p-p38 and p-ERK, decreases IκB level, indicating the suppression of MAPK and NF-κB signaling.

In Vivo: Anti-inflammatory agent 35 (compound 5a27) (50 mg/kg; po; single dose, monitored 0-25 min) has a better bioavailability than curcumin (HY-N0005).
Anti-inflammatory agent 35 (10 mg/kg; ip; once daily for 1 week) improves LPS-induced ALI by inhibiting inflammation in mice model.

The pharmacokinetic parameters in rats

Route	Dose (mg/kg)	AUC(0-t) (μg/L·h)	AUC(0-∞) (μg/L·h)	MRT(0-t) (h)	MRT(0-∞) (h)	t1/2 (h)	Tmax (h)	CLz/F (L/h/kg)	Vz/F (L/kg)	Cmax
p.o	50	231.2	325.6	7.8	12.3	6.7	3.3	5062.6	827.1	113.3
i.v	5	34.3	122.4	11.3	19.9	0.2	0.1	404.4	59.5	16.4

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