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抑制剂描述:

产品名称:Naproxen sodium

产品别名:见爱必信官网

英文别名:Naproxen sodium

靶点:COX

CAS:26159-34-2

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Naproxen 是一种非选择性环氧合酶(COX)抑制剂,作用于COX-1和COX-2时,IC50分别为8.7 μM和5.2 μM。Naproxen作用于完整细胞,抑制COX-1和 COX-2效果差不多,IC50分别为2.2 μg/mL和1.3 μg/mL。 在体外,Naproxen作用于大鼠和人类,降低LPS诱导的PGE₂和TXB₂产量,抑制PGE₂ 时,IC50分别为30.7 μM和79.5 μM,抑制TXB₂时,IC50 分别为72.4 μM 和48.3 μM。 Naproxen抑制人血小板TXB₂产量和LPS诱导的人单核细胞TXB₂ 产量,IC50分别为5.7和6.4, 也稍微选择性抑制组成型和诱导型COX-2,作用于COX-1的IC50值与作用于COX-2 的IC50值之比为6.3。

溶解性:Water :25.2 mg/mL (100 mM)

体外研究:

Naproxen is approximately equipotent inhibitor of COX-1 and COX-2 in intact cells with IC50 of 2.2 μg/mL and 1.3 μg/mL, respectively. Naproxen decreases the in vitro LPS-induced PGE2 and TXB2 production in rats and humans with IC50 of 30.7 μM and 79.5 μM for PGE2 inhibition, 72.4 μM and 48.3 μM for TXB2 inhibition, respectively. Naproxen produces concentration-related inhibition of TXB2 production from human platelets and LPS-induced TXB2 production from human mononuclear cells with plC50 values (-log concentration inhibiting TXB2 by 50%) of 5.7 and 6.4, respectively, and exhibits slightly inhibitory selectivity for constitutive and induced COX-2 with IC50 COX-1/IC50 COX-2 of 6.3. Only high concentration of Naproxen can significantly induce apoptosis at 48 hours in HCA-7 colon cancer cells with IC50 of 1.45 mM.

体内研究:Administration of Naproxen reduces the LPS-induced PGE2 and TXB2 production in vivo in rats with IC50 values of 12.8 μM and 5.9 μM, respectively, which represents that Naproxen is a nonselective COX inhibitor with the log IC50 ratio (COX-2/COX-1) of 0.34. Naproxen displays IC50 of 27 μM for analgesia in a rat model with carrageenan-induced arthritis and IC50 of 40 μM for antipyretics in a yeast-induced fever rat model, while exhibits inhibition of PGE2 with IC50 of 13 μM and TXB2 with IC50 of 5 μM.

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