research use only

Carbenoxolone Sodium

Cat.No.S4368

Carbenoxolone, a synthetic derivative of glycyrrhetinic acid, is also used as a blocker of the enzyme 11β-hydroxysteroid dehydrogenase (11β-HSD), of pannexon membrane channels (comprising 6 subunits of pannexin) and the related innexon channels.
Carbenoxolone Sodium Chemical Structure

Chemical Structure

Molecular Weight: 614.72

Quality Control

Batch: S436801 DMSO]23 mg/mL]false]Ethanol]6 mg/mL]false]Water]Insoluble]false Purity: 99.98%
99.98

Chemical Information, Storage & Stability

Molecular Weight 614.72 Formula

C34H48Na2O7

Storage (From the date of receipt)
CAS No. 7421-40-1 Download SDF Storage of Stock Solutions

Synonyms N/A 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+]

Solubility

In vitro
Batch:

DMSO : 23 mg/mL ( (37.41 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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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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Mechanism of Action

In vitro

Carbenoxolone induces astrocytes a reversible suppression of spontaneous action potential discharges, synaptic currents and synchronised calcium oscillations. Carbenoxolone inhibits oscillatory activity induced by the GABAA antagonist, bicuculline.Carbenoxolone causes an increase in the action potential threshold and strongly decreases the firing rate in response to a sustained depolarising current in astrocytes. [1] Carbenoxolone (100 μM) reduces photoreceptor-to-horizontal cell synaptic transmission by 92% in the Retina. Carbenoxolone (100 μM) reduces cone Ca channel current by 37%, reduces depolarization-evoked [Ca2+] signals in fluo-4 loaded retinal slices by 57% and inhibits Ca channels in Müller cells by 52% in the Retina. [2] Carbenoxolone abolishes the generation of full or partial ectopic spike generation, as well as spontaneous epileptiform activity in CA3 or CA1 regions of the rat hippocampal slices via closing GJ channels. [3]

In vivo

Carbenoxolone (400 mg/kg) decreases the duration of seizure producing protection against seizure but failing to protect against mortality.Carbenoxolone significantly increases sleeping time and decreased latency in doses of 100 mg/kg, 200 mg/kg and 300 mg/kg in mice dose dependently. Carbenoxolone (400 mg/kg) shows muscle relaxant activity and in the accelerated rotarod test, Carbenoxolone in doses of 200 mg/kg and 300 mg/kg shows a decline in motor coordination. [3] Carbenoxolone (12.5 mg/day) leads to a significant reduction in average birth weight (20% fall) in rats. [4] Carbenoxolone treatment lowers birthweight and induces hypertension in the offspring of rats fed a protein-replete diet. [5]

References
  • https://pubmed.ncbi.nlm.nih.gov/8932995/
  • https://pubmed.ncbi.nlm.nih.gov/9486087/

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