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| Targets |
Carbenoxolone sodium targets multiple enzymes and channels. It inhibits 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). It also acts as a gap junction inhibitor, blocking communication between cells. It modulates cell membrane channels. By inhibiting 11β-HSD1, carbenoxolone affects cortisol metabolism and has anti-inflammatory effects.
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| ln Vitro |
Carbenoxolone disodium (6-150 μM; 1 hour pretreatment) is hazardous to VACV-A5L-EGFP infection for 48 hours and inhibits the vaccinia virus (VACV) from replicating itself in gap junctions in HaCaT cells[2]. In hacat cells, carbenoxolone (30 μM; 1 h pre-treatment) increases late protein A27 expression but does not upregulate PP2A expression [2].
In vitro, carbenoxolone sodium inhibits 11β-HSD1. It acts as a gap junction inhibitor and modulates cell membrane channels. These activities have been demonstrated in various in vitro assays. Its anti-ulcerative and anti-inflammatory properties have been shown in cellular and tissue models. |
| ln Vivo |
When compared to saline, carbenoxolone (i.p. ; 100, 200, and 300 mg/kg; 30, 60, and 60 minutes prior to diazepam) exhibits muscle relaxant activity and is superior to the diazepam test in terms of its ability to produce this effect [3]. In mice used in the pentylenetetrazole (PTZ) seizure model, carbenoxolone (ip; 100, 200, and 300 mg/kg; 30, 60, and 60 minutes before to pentylenetetrazole) dramatically lengthens sleep duration and decreases latency in a dose-dependent way. ..83.3 mg/kg is the ED50 value (%95 CL:556.29)[3].
In vivo, carbenoxolone sodium has been shown to exhibit anti-ulcerative and anti-inflammatory properties. It is used in neuroscience research as a gap junction inhibitor. Its effects on 11β-HSD1 inhibition can influence cortisol metabolism and inflammation. However, specific details of in vivo efficacy studies are not extensively detailed in the available literature. |
| Enzyme Assay |
The in vitro enzyme assay for carbenoxolone sodium measures its ability to inhibit 11β-HSD1 activity. These cell-free assays use purified 11β-HSD1 and a substrate. The compound's inhibitory potency is determined by measuring the reduction in enzyme activity. Its effects on gap junctions can be assessed using electrophysiological or dye transfer assays.
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: HaCaT cells Tested Concentrations: 6 μM, 12 μM, 30 μM, 60 μM, 150 μM Incubation Duration: Pre-treatment 1 hour Experimental Results: Had no toxicity until 48 hrs (hours) at high dose in virus-infected cells. Western Blot Analysis[2] Cell Types: HaCaT cells Tested Concentrations: 30 μM Incubation Duration: Pre-treatment 1 hour Experimental Results: Presented an obvious upregulation of A27. In vitro cellular assays for carbenoxolone sodium assess its effects on gap junction communication and cell membrane channels. Cells are treated with carbenoxolone, and gap junction-mediated dye transfer or electrical coupling is measured. Its effects on 11β-HSD1 activity can also be assessed in cells. These assays demonstrate the compound's functional activity in a relevant cellular context. |
| Animal Protocol |
Animal/Disease Models: Male balb/c (Bagg ALBino) mouse[3]
Doses: 100, 200 and 300 mg/kg Route of Administration: intraperitoneal (ip)injection; 30, 60 and 60 min before Pentylenetetrazole Experimental Results: Dramatically increased the sleeping time in mice. In vivo animal studies for carbenoxolone sodium have been conducted to assess its anti-ulcerative and anti-inflammatory effects. However, specific details of these studies are not extensively detailed in the available literature. The compound is primarily used as a research tool in neuroscience and virology. |
| ADME/Pharmacokinetics |
Carbenoxolone sodium is administered orally. It is absorbed and distributed throughout the body. It is metabolized in the liver and excreted in bile and urine. Its pharmacokinetic properties support its use as a therapeutic agent. However, specific parameters such as half-life and bioavailability are not extensively detailed in the available literature.
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| Toxicity/Toxicokinetics |
Carbenoxolone sodium has a well-established safety profile. Common adverse effects include sodium and water retention, hypertension, and hypokalemia due to its inhibition of 11β-HSD1. Its safety has been established through clinical use for ulcer treatment. It is available as a prescription medication in some countries.
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| References | |
| Additional Infomation |
Carbenoxolone sodium is a triterpenoid compound extracted from licorice root. It is used to treat peptic ulcers, especially gastric ulcers. Antidiuretic side effects are relatively common, but otherwise, the drug has low toxicity. See also: Carbenoxolone (note moved to).
Carbenoxolone sodium is a synthetic derivative of glycyrrhetinic acid found in licorice root. It inhibits 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). It exhibits anti-ulcerative and anti-inflammatory properties. It is also used as a gap junction inhibitor in neuroscience research and modulates cell membrane channels. It is available as a prescription medication and is also used as a research tool. |
| Molecular Formula |
C34H48NA2O7
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|---|---|
| Molecular Weight |
614.73
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| Exact Mass |
614.32
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| CAS # |
7421-40-1
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| Related CAS # |
5697-56-3 (Parent)
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| PubChem CID |
636402
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| Appearance |
White to off-white solid powder
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| Boiling Point |
687.4ºC at 760 mmHg
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| Flash Point |
211.6ºC
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| LogP |
4.158
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
43
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| Complexity |
1190
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| Defined Atom Stereocenter Count |
9
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| SMILES |
C[C@]12CC[C@](C[C@H]1C3=CC(=O)[C@@H]4[C@]5(CC[C@@H](C([C@@H]5CC[C@]4([C@@]3(CC2)C)C)(C)C)OC(=O)CCC(=O)[O-])C)(C)C(=O)[O-].[Na+].[Na+]
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| InChi Key |
BQENDLAVTKRQMS-SBBGFIFASA-L
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| InChi Code |
InChI=1S/C34H50O7.2Na/c1-29(2)23-10-13-34(7)27(32(23,5)12-11-24(29)41-26(38)9-8-25(36)37)22(35)18-20-21-19-31(4,28(39)40)15-14-30(21,3)16-17-33(20,34)6/h18,21,23-24,27H,8-17,19H2,1-7H3,(H,36,37)(H,39,40)/q2*+1/p-2/t21-,23-,24-,27+,30+,31-,32-,33+,34+/m0../s1
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| Chemical Name |
sodium (2S,4aS,6aS,6bR,8aR,10S,12aS,12bR,14bR)-10-((3-carboxylatopropanoyl)oxy)-2,4a,6a,6b,9,9,12a-heptamethyl-13-oxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,11,12,12a,12b,13,14b-icosahydropicene-2-carboxylate
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| Synonyms |
PyrogastroneBiogastrone Bioral Duogastrone Sanodin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~50 mg/mL (~81.34 mM)
DMSO : ~16.67 mg/mL (~27.12 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (2.72 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.67 mg/mL (2.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 16.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 0.93 mg/mL (1.51 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 6.25 mg/mL (10.17 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6267 mL | 8.1337 mL | 16.2673 mL | |
| 5 mM | 0.3253 mL | 1.6267 mL | 3.2535 mL | |
| 10 mM | 0.1627 mL | 0.8134 mL | 1.6267 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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