Carbenoxolone disodium
(Synonyms: 甘珀酸钠) 目录号 : GC10624An 11β-HSD inhibitor
Cas No.:7421-40-1
Sample solution is provided at 25 µL, 10mM.
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.
Cas No. | 7421-40-1 | SDF | |
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 SMILES | CC1(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 tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.6268 mL | 8.1338 mL | 16.2676 mL |
5 mM | 0.3254 mL | 1.6268 mL | 3.2535 mL |
10 mM | 0.1627 mL | 0.8134 mL | 1.6268 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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- Purity: >99.50%
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