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Carbenoxolone disodium

Catalog No.GC10624

La carbenoxolona disÓdica es el metabolito activo del Ácido glicirrÍcico y el inhibidor de la 11β-HSD humana y la 3α, 20β-HSD bacteriana.

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Carbenoxolone disodium Chemical Structure

Cas No.: 7421-40-1

Tamaño Precio Disponibilidad Cantidad
10mM (in 1mL DMSO)
35,00 $
Disponible
50mg
35,00 $
Disponible

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Sample solution is provided at 25 µL, 10mM.

Description of Carbenoxolone disodium

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.

Chemical Properties of Carbenoxolone disodium

Cas No. 7421-40-1 SDF
Chemical Name 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+]
Formula C34H48Na2O7 M.Wt 614.72
Solubility ≥ 30.736mg/mL in DMSO Storage Store at 2-8°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Carbenoxolone disodium

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1 mg 5 mg 10 mg
1 mM 1.6268 mL 8.1338 mL 16.2676 mL
5 mM 325.4 μL 1.6268 mL 3.2535 mL
10 mM 162.7 μL 813.4 μL 1.6268 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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