吲哚美辛钠

中文名称:

吲哚美辛钠

中文同义词:

吲哚美辛钠;2-甲基-1-(4-氯苯甲酰基)-5-甲氧基-1H-吲哚-3-乙酸钠;吲哚美辛钠 水溶性;INDOMETHACIN SODIUM SALT TRIHYDRATE英文同义词:SODIUM,2-[1-(4-CHLOROBENZOYL)-5-METHOXY-2-METHYLINDOL-3-YL]ACETATE,TRIHYDRATE;吲哚美辛钠中文名称:吲哚美辛钠中文同义词:吲哚美辛钠;水溶性吲哚美辛;吲哚美辛钠盐三水合物

英文名称:

INDOMETHACIN SODIUM SALT TRIHYDRATE

英文同义词:

INDOMETHACIN SODIUM SALT TRIHYDRATE;1H-Indole-3-acetic acid, 1-(4-chlorobenzoyl)-5-methoxy-2-methyl-, sodi um salt, trihydrate;INDOMETACIN FARNESIL;1H-Indole-3-aceticacid, 1-(4-chlorobenzoyl)-5-Methoxy-2-Methyl-, sodiuM salt, hydrate (1:1:3);Indometacin Sodium;Sodium salt trihydrate;sodium,2-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetate,trihydrate;Indomethacin sodium hydrate

CAS号:

74252-25-8

分子式:

C34H40ClNO4

分子量:

562.146

EINECS号:

相关类别:

解热镇痛药;化合物：原料药;兽药;饲料添加剂;医药兽药;化工原料;医用原料;兽药原料药;原料药

Mol文件:

74252-25-8.mol

产品描述

吲哚美辛钠是在吲哚美辛基础上研制成功可水溶的非甾体类解热镇痛药物，其具有显著的解热、消炎、镇痛、抗风湿，减轻免疫反应、止泻和增加抗菌药物组织血药浓度，改善精液品质等特点。

产品用途

吲哚美辛钠可用于治疗高热性疾病、治疗胸腔感染、肠炎、腹泻等疾病。

生物活性

Indomethacin sodium hydrate (Indometacin sodium hydrate) 是一种有效的，可透过血脑屏障的，非选择性的 COX1 和 COX2 抑制剂，在 CHO 细胞中，对人 COX-1 和 COX-2 的 IC50 值分别为 18 nM 和 26 nM。Indomethacin sodium hydrate 通过干扰溶酶体的正常功能来破坏自噬流 (autophagic flux)。

靶点

Target Value COX1 () 0.11 μM COX2 () 0.78 μM

Target

Value

COX1 ()

0.11 μM

COX2 ()

0.78 μM

体外研究

Indomethacin is a potent and nonselective inhibitor of COX1 and COX2 , with IC 50 s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells. Indomethacin inhibits lipopolysaccharide (LPS)-induced PGE2 production (COX-2) in a human whole blood assay with a potency (IC 50 =0.68±0.17 μM), and suppresses coagulation-induced TXB2 production (COX-1) (IC 50 =0.19±0.02 μM). Indomethacin blocks COX-1 with an IC 50 of 20±1 nM in U937 cell microsomes at a low arachidonic acid concentration (0.1 μM).

体内研究

Indomethacin dose-dependently inhibits both the carrageenan-induced rat paw oedema (ED 50 , 2.0 mg/kg), hyperalgesia (ED 50 , 1.5 mg/kg), and is also effective at reversing LPS-induced pyrexia in rats (ED 50 , 1.1 mg/kg). Indomethacin (2.5 mg/kg, i.p) decreases the number of NeuN + cells in the animals at 8 days after ET-1 injection. Indomethacin also reduces microglia/macrophage activation at 14 days. Indomethacin significantly increases the number of SVZ DCX + cells/field at 14 days post stroke. Indomethacin (22.9 mg/kg, p.o.) produces 8 to 10 linear mucosal lesions extended from the fundic to pyloric area of stomach wall.