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Carbenoxolone disodium
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。
Carbenoxolone disodium图片
CAS NO:7421-40-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议

产品介绍
Carbenoxolone disodium 是甘草酸的活性代谢物,是人 11β-HSD 和细菌 3α、20β-HSD 的抑制剂。
Cas No.7421-40-1
别名甘珀酸钠
化学名disodium;10-(3-carboxylatopropanoyloxy)-2,4a,6a,6b,9,9,12a-heptamethyl-13-oxo-3,4,5,6,6a,7,8,8a,10,11,12,14b-dodecahydro-1H-picene-2-carboxylate
Canonical SMILESCC1(C2CCC3(C(C2(CCC1OC(=O)CCC(=O)[O-])C)C(=O)C=C4C3(CCC5(C4CC(CC5)(C)C(=O)[O-])C)C)C)C.[Na+].[Na+]
分子式C34H48Na2O7
分子量614.72
溶解度≥ 30.736mg/mL in DMSO
储存条件Store at 2-8°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Carbenoxolone disodium is an inhibitor of 11β-hydroxysteroid dehydrogenase (11β-HSD) [1].

11β-HSD is a family of enzymes that regulating the access of glucocorticoids to the steroid receptors.

In bovine aortic endothelial cells (BAEC), carbenoxolone disodium can block gap junction communication (GJC) and modulates Cx43 expression, which based on junctional patency [2].

Carbenoxolone disodium is an inhibitor of 11β-HSD and causes hypokalemia and hypernatremia. In male rats, 11β-HSD was inhibited in the liver, kidney, pituitary, hippocampus, hypothalamus and amygdala 1h after intraperitoneal administration of CX (100 mg/kg). Injection of CX (1.5mg/kg) into the 3rd ventricle inhibited corticosterone to 11-dehydrocorticosterone by 11-HSD in the hippocampus and pituitary and produced behavioral hyperactivity, while had no effect in the liver or kidney. Injection of CX (10-50ug/rat) into intracerebroventricularly inhibited 11β-HSD differentially in the hypothalamus and hippocampus [1]. These results show that low doses of CX can alter the activity of 11β-HSD in specific brain regions without affecting its activity in peripheral tissues, and only marginally in the pituitary, provides a method to study the central role of this enzyme.

References:
[1].  Jellinck PH, Monder C, McEwen BS, et al. Differential inhibition of 11 beta-hydroxysteroid dehydrogenase by carbenoxolone in rat brain regions and peripheral tissues. J Steroid Biochem Mol Biol, 1993, 46(2): 209-213.
[2].  Sagar GD, Larson DM. Carbenoxolone inhibits junctional trasnfer and upregulates connexin43 expression by a protein kinase A-dependent pathway. J Cell Biochem, 2006, 98(6): 1543-1551.