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product name Enoxolone


Description: Enoxolone, also known as Glycyrrhetic acid,  is a pentacyclic triterpenoid derivative of the beta-amyrin type obtained from the hydrolysis of glycyrrhizic acid, which was obtained from the herb liquorice. Enoxolone is used for the treatment of inflammation. Enoxolone is used topically for allergic or infectious skin inflammation and orally for its aldosterone effects in electrolyte regulation. 

References: J Pharm Pharmacol. 2003 Jun;55(6):811-7; Steroids. 1996 Mar;61(3):110-5.



Molecular Weight (MW)

470.68
Formula

C30H46O4
CAS No.

471-53-4
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 94 mg/mL (199.7 mM)
Water: <1 mg/mL
Ethanol: <1 mg/mL
Solubility (In vivo)

2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 10mg/mL
Synonyms

Glycyrrhetin 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19410427

In Vitro

In vitro activity: JEG-3 cell line was derived from a human choriocarcinoma. In this cell line, the enzyme activity of 11β-HSD-3 was inhibited by glycyrrhetinic acid


Kinase Assay


Cell Assay: Before glucocorticoids bind the mineralocorticoid receptor (MR), the selectivity of MR for aldosterone can be exerted by enzymes, and hence competing glucocorticoids is inactivated. 11β-HSD-1 and 11β-HSD-2 and 11β-HSD-3 are three of the enzymes. 11β-HSD-1 has bidirectional activity and a Km value in the micromolar range. It is NADP+-dependent. 11β-HSD-2 exhibits only oxidase activity and has a Km in the nanomolar range. It is NAD+-dependent. In the kidney, it colocalizes with the MR.

In Vivo In rats, 3 h after the administration of glycyrrhetinic acid at concentration of 200 mg/kg, p.o. significantly inhibited 11β-HSD activity in the kidney and the liver. In addition, glycyrrhetinic acid slightly increased the circulating corticosterone level. In differential inhibitory effects on 11β-HSD isozyme activity, the 11-, 24- and 30-positions of glycyrrhetinic acid may play important roles. This had been showed by Data. 
Animal model  
Formulation & Dosage  
References J Pharm Pharmacol. 2003 Jun;55(6):811-7; Steroids. 1996 Mar;61(3):110-5.

MEK162

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Author: Sodium channel