| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
11β-hydroxysteroid dehydrogenase (11β-HSD) type 1 and gap junction connexin channels. Carbenoxolone reversibly inhibits the conversion of inactive cortisone to cortisol by blocking 11β-HSD. It also directly interferes with connexin function by blocking gap junction channel activity.
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|---|---|
| ln Vitro |
Carbenoxolone inhibits 11β-HSD, an enzyme that regenerates cortisol from inactive cortisone. As a gap junction blocker, it inhibits connexin channel activity. Carbenoxolone also interacts with stable residues of beta-amyloid 42 peptides, fibrils, and oligomers, thereby inhibiting their aggregation. It inhibits macrophage migration into atria and prevents the development of fatty liver disease.
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| ln Vivo |
Carbenoxolone has been shown to alleviate liver fibrosis and inhibit macrophage migration into atria. It has antiviral activity against DENV infection targeting the virus itself. Carbenoxolone may decrease the amount of active glucocorticoid in the brain by inhibiting 11β-HSD type 1.
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| Enzyme Assay |
In vitro enzyme inhibition assays for Carbenoxolone involve measuring the activity of 11β-HSD in the presence of varying concentrations of the compound. The enzyme is incubated with cortisone substrate, and the conversion to cortisol is quantified. The IC50 is determined from the dose-response curve. Gap junction inhibition can be assessed using dye transfer assays in connexin-expressing cells.
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| Cell Assay |
In vitro cell-based assays for Carbenoxolone assess its effects on 11β-HSD activity and gap junction communication in cultured cells. Cells are treated with Carbenoxolone, and cortisol production or dye transfer through gap junctions is measured. Its antiviral activity can be assessed in DENV-infected cell cultures by measuring viral replication.
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| Animal Protocol |
In vivo studies of Carbenoxolone have been conducted in animal models of liver fibrosis, atrial inflammation, and viral infection. The compound is typically administered orally or intraperitoneally. Endpoints include measurement of liver fibrosis markers, macrophage migration, and viral load.
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| ADME/Pharmacokinetics |
Carbenoxolone is orally bioavailable. As a glycyrrhetinic acid derivative, it is absorbed from the gastrointestinal tract and metabolized in the liver. Detailed pharmacokinetic parameters such as half-life and clearance are not extensively reported but are characteristic of triterpenoid compounds.
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| Toxicity/Toxicokinetics |
Carbenoxolone has been licensed for use in the UK for esophageal ulceration and inflammation. It may cause mineralocorticoid-like side effects due to 11β-HSD inhibition, including sodium retention, potassium loss, and hypertension. Comprehensive toxicological data are available from its clinical use.
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| Additional Infomation |
drug 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.
Carbenoxolone is a licensed drug in the UK for esophageal ulceration and inflammation. It is also used as a research tool for studying 11β-HSD function, gap junction communication, and glucocorticoid metabolism. It has been investigated for antiviral activity against DENV infection and for its effects on beta-amyloid aggregation. |
| Molecular Formula |
C34H50O7
|
|---|---|
| Molecular Weight |
570.767
|
| Exact Mass |
570.356
|
| CAS # |
5697-56-3
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| Related CAS # |
7421-40-1 (di-hydrochloride salt)
|
| PubChem CID |
636403
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| Appearance |
Typically exists as solid at room temperature
|
| Density |
1.20
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| Boiling Point |
687.4ºC at 760 mmHg
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| Melting Point |
291-294 °C
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| Flash Point |
211.6ºC
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| LogP |
6.828
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| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
|
| Heavy Atom Count |
41
|
| Complexity |
1200
|
| Defined Atom Stereocenter Count |
9
|
| SMILES |
CC(C)([C@]1([H])CC[C@@]([C@@]2(CC[C@]3(CC[C@](C(O)=O)(C[C@]3(C2=C4)[H])C)C)C)5C)[C@@H](OC(CCC(O)=O)=O)CC[C@]1(C)[C@@]5([H])C4=O
|
| InChi Key |
OBZHEBDUNPOCJG-WBXJDKIVSA-N
|
| InChi Code |
InChI=1S/C34H50O7/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)/t21-,23-,24-,27+,30+,31-,32-,33+,34+/m0/s1
|
| Chemical Name |
(2S,4aS,6aR,6aS,6bR,8aR,10S,12aS,14bR)-10-(3-carboxypropanoyloxy)-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-carboxylic acid
|
| Synonyms |
Carbenoxolona; Bioral; Biogastrone
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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 |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7520 mL | 8.7601 mL | 17.5202 mL | |
| 5 mM | 0.3504 mL | 1.7520 mL | 3.5040 mL | |
| 10 mM | 0.1752 mL | 0.8760 mL | 1.7520 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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