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ZXX2-77是一种环氧合酶-1(COX-1)选择性抑制剂,属于苯磺酰苯胺类化合物。它被报道为一种镇痛剂,不会引起胃部损伤。ZXX2-77具有较弱的镇痛效果,但在体外表现出强效的COX-1抑制活性。ZXX2-77在口服吸收率低,导致其体内镇痛效果较弱。在30 mg/kg剂量下,ZXX2-77的最大血药浓度(1.2 mM)未达到其COX-1 IC50值(3.2 mM)。相比之下,其衍生物ZXX2-79虽然在体外COX抑制活性较弱,但吸收性更好,表现出更强的镇痛效果且几乎不引起胃部损伤。这些发现表明,ZXX2-77及其衍生物作为COX-1选择性抑制剂可能成为不引起胃部损伤的有效镇痛药。

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ZXX2-77 Chemical Structure

ZXX2-77 Chemical Structure

CAS No. : 304913-22-2

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生物活性

ZXX2-77 is a cyclooxygenase-1 (COX-1) selective inhibitor belonging to the benzenesulfonylanilide class of compounds. It is reported as a novel analgesic that does not cause gastric damage. ZXX2-77 has a weak analgesic effect but exhibits potent COX-1 inhibitory activity in vitro. The low oral absorption rate of ZXX2-77 leads to its weak analgesic effect in vivo. At a dose of 30 mg/kg, the maximum plasma concentration of ZXX2-77 (1.2 mM) did not reach its COX-1 IC50 value (3.2 mM). In contrast, its derivative ZXX2-79, although weaker in vitro COX inhibitory activity, is better absorbed, exhibits stronger analgesic effect and hardly causes gastric damage. These findings suggest that ZXX2-77 and its derivatives as COX-1 selective inhibitors may become effective analgesics that do not cause gastric damage.

分子量

296.77

Formula

C13H13ClN2O2S

CAS 号
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.

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ZXX2-77 相关分类

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产品名称:
ZXX2-77
目录号:
HY-136720
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