Cat. No.: HY-B1588

Carbenoxolone

10 Cited Publications

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Carbenoxolone is a blood-brain barrier-permeable Pannexin1 inhibitor, gap junction (Gap junction) blocker, and β-amyloid 42 inhibitor. Carbenoxolone modulates voltage-gated currents of wild-type and mutant Panx1, and inhibits stimulus-activated Panx1 channel function. Carbenoxolone interacts with stable residues of β-amyloid 42 peptides, fibrils and oligomers, thereby inhibiting their aggregation. Carbenoxolone alleviates liver fibrosis. Carbenoxolone exerts neuroprotective and nootropic effects. Carbenoxolone can be used in studies related to Alzheimer's disease and liver fibrosis.

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Pureté: 99.9%
CAS No.: 5697-56-3
Formule: C₃₄H₅₀O₇
Masse moléculaire:570.76

Stockage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Carbenoxolone Chemical Structure

CAS No.: 5697-56-3

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Fluorescent Dye

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Cellular Effect

Cell Line	Type	Value	Description	References
3T3-L1	EC₅₀	>500 μM Compound: 4; CBX	Cytotoxicity against mouse 3T3L1 cells measured after 72 hrs by celltiter-glo luminescent cell viability assay Cytotoxicity against mouse 3T3L1 cells measured after 72 hrs by celltiter-glo luminescent cell viability assay	[PMID: 31294974]
CHO	IC₅₀	0.5 μM Compound: Carbenoxolone	Inhibition of human 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay Inhibition of human 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay	[PMID: 21093259]
CHO	IC₅₀	250 nM Compound: Carbenoxolone	Inhibition of mouse 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay Inhibition of mouse 11beta-HSD1 expressed in CHO cells after 3 hrs by HTRF cortisol assay	[PMID: 21093259]
CHO-K1	IC₅₀	0.5 μM Compound: carbenoxolone	Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells using cortisone as substrate after 3 hrs by HTRF assay Inhibition of human 11beta-HSD1 expressed in CHO-K1 cells using cortisone as substrate after 3 hrs by HTRF assay	[PMID: 24900439]
CHO-K1	IC₅₀	1630 nM Compound: Carbenoxolone	Inhibition of human 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay Inhibition of human 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay	[PMID: 31759849]
CHO-K1	IC₅₀	243 nM Compound: Carbenoxolone	Inhibition of mouse 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay Inhibition of mouse 11beta-HSD1 expressed in CHOK1 cells using XL665-labeled cortisol as substrate measured after 24 hrs by HTRF assay	[PMID: 31759849]
HEK293	EC₅₀	82 nM Compound: Carbenoxolone	Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as [3H]cortisol production after 60 mins by SPA	[PMID: 22440625]
HEK293	IC₅₀	0.17 μM Compound: 4; CBX	Inhibition of 11beta-HSD2 (unknown origin) expressed in HEK293 cells using cortisone as substrate measured after 2 hrs in presence of NAD+ by HTRF assay Inhibition of 11beta-HSD2 (unknown origin) expressed in HEK293 cells using cortisone as substrate measured after 2 hrs in presence of NAD+ by HTRF assay	[PMID: 31294974]
HEK293	IC₅₀	206 nM Compound: carbenoxolone	Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay Inhibition of mouse 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone into [3H]cortisol by scintillation proximity assay	[PMID: 22360639]
HEK293	IC₅₀	82 nM Compound: carbenoxolone	Inhibition of mouse microsomal 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay Inhibition of mouse microsomal 11beta-HSD2 expressed in HEK293 cells assessed as conversion of [3H]cortisone to [3H]cortisol by scintillation proximity assay	[PMID: 19564108]
RAW264.7	IC₅₀	11.42 μM Compound: Carbenoxolone	Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of HMGB1-induced NO production pretreated with compounds for 15 mins followed by HMGB1 stimulation measured after 24 hrs by Griess reagent based assay Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of HMGB1-induced NO production pretreated with compounds for 15 mins followed by HMGB1 stimulation measured after 24 hrs by Griess reagent based assay	[PMID: 34800877]
RAW264.7	IC₅₀	6.64 μM Compound: Carbenoxolone	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production	[PMID: 34973341]
RAW264.7	IC₅₀	7.62 μM Compound: Carbenoxolone	Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of HMGB1-induced NO production Anti-inflammatory activity in mouse RAW264.7 cells assessed as inhibition of HMGB1-induced NO production	[PMID: 34973341]

In Vitro

Carbenoxolone (0.01-1000 μM) potently inhibits voltage-gated wild-type human Pannexin1 channel activity in HEK293 cells with an IC₅₀ of ~2 μM, with greater inhibition (up to ~90% at 100 mV) observed in strongly rectifying cell populations^[1].
Carbenoxolone (0.01-1000 μM) potentiates voltage-gated hPanx1/Panx3 loop1 chimera channel activity in HEK293 cells with an EC₅₀ of ~120 μM, producing a nearly fourfold increase in current at a saturating concentration of 562 μM^[1].
Carbenoxolone (50-100 μM; 4 days) inhibits amyloid-beta 42 peptide aggregation in a concentration-dependent manner, with 22.54% inhibition at 50 μM and 47.16% inhibition at 100 μM following 4-day incubation at 37 °C^[2].
Carbenoxolone (50 μM; 24-48 h) inhibits gap junction activity in primary rat hepatocytes^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Carbenoxolone (1 mg/kg body weight/day; administered via an osmoti pump implanted in the peritoneal cavity; 14 days)reduces liver fibrosis and hepatic stellate cell activation in TAA-induced fibrotic mice, while modulating hepatic inflammatory protein levels and glutathione peroxidase activity^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Balb/c (male, 22 g)^[3]
Dosage:

1 mg/kg body weight/day
Administration:

Administered via an osmoti pump implanted in the peritoneal cavity; daily; 14 days
Result:

Significantly reduced hepatic collagen deposition (p ≤ 0.05) and percentage of alpha smooth muscle actin (α-SMA)-positive cells (p ≤ 0.05).
Increased serum aspartate aminotransferase (AST) levels (p ≤ 0.05).
Significantly upregulated hepatic glutathione peroxidase (GPx) activity (p ≤ 0.05).
Significantly increased hepatic levels of eotaxin-2 (p ≤ 0.05) and Fas ligand (p ≤ 0.05).
Significantly reduced hepatic levels of interleukin 1α (p ≤ 0.01), interleukin 2 (p ≤ 0.05), interleukin 4 (p ≤ 0.05), growth-regulated alpha protein (KC) (p ≤ 0.01), lipopolysaccharide-induced CXC chemokine (LIX) (p ≤ 0.05), thymus-expressed chemokine (TECK) (p ≤ 0.01), and granulocyte-macrophage colony-stimulating factor (GM-CSF) (p ≤ 0.01).

Chemical Information

CAS No. 5697-56-3
Appearance Solid
Masse moléculaire 570.76
Formule C₃₄H₅₀O₇
Color White to off-white
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (10)

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Nat Neurosci

Spatiotemporally selective astrocytic ATP dynamics encode injury information sensed by microglia following brain injury in mice. [Abstract]

2024 Aug;27(8):1522-1533. PMID: 38862791

Carbenoxolone purchased from MedChemExpress. Usage Cited in: Nat Neurosci. 2024 Aug;27(8):1522-1533. [Abstract]

The gap-junction dependency of FLA-evoked astrocytic Ca2+ wave and ATP bursts (n = 10/9/7 slices from 4/4/3 mice for ACSF, 1-Octanol and Carbenoxolone disodium; CBX; 100 µM; 5 min).
Cell Chem Biol

Electrochemical sensor toolkit for simultaneous glutamate detection at edge of cleft and peri-soma. [Abstract]

2025 Jun 19;32(6):885-898.e11. PMID: 40466640
Free Radic Biol Med

Zinc ions facilitate metabolic bioenergetic recovery post spinal cord injury by activating microglial mitophagy through the STAT3-FOXO3a-SOD2 pathway. [Abstract]

2025 Feb 1:227:64-79. PMID: 39613048

Carbenoxolone purchased from MedChemExpress. Usage Cited in: Free Radic Biol Med. 2025 Feb 1:227:64-79. [Abstract]

Western blot analysis of p-FOXO3a (S253) and FOXO3a protein in BV2 cells post-Carbenoxolone disodium (CBX; 100 μM) and H₂O₂/zinc treatment.
Free Radic Biol Med

Connexin30-deficient mice increase susceptibility to noise via redox and lactate imbalances. [Abstract]

2024 Nov 20:225:641-653. PMID: 39396580
Transl Res

Counteracting TGM2 by a Fibroin peptide ameliorated Adriamycin-induced nephropathy via regulation of lipid metabolism through PANX1-PPAR α/PANK1 pathway. [Abstract]

2024 May 9:271:26-39. PMID: 38734063

Carbenoxolone purchased from MedChemExpress. Usage Cited in: Transl Res. 2024 May 9:271:26-39. [Abstract]

HK-2 cells were treated with PANX1 inhibitor PBN (1 mM),and Carbenoxolone disodium (CBX; 100 μM) with or without ADR. Intracellular lipid content was detected by oil red O staining.

Carbenoxolone purchased from MedChemExpress. Usage Cited in: Transl Res. 2024 May 9:271:26-39. [Abstract]

HK-2 cells were treated with PANX1 inhibitor PBN (1 mM), and Carbenoxolone disodium (CBX; 100 μM) with or without ADR. The protein expressions of Fibronectin, PANX1, PPAR α, and PANK1 were analyzed by western blotting.
Glia

Role of Cx43 and ACKR3 in Modulating Astrocytic Response and Neuronal Survival Post-Subarachnoid Hemorrhage. [Abstract]

2025 Apr 4. PMID: 40183383

Carbenoxolone purchased from MedChemExpress. Usage Cited in: Glia. 2025 Apr 4. [Abstract]

Evaluation of GJIC in different cell groups by assessing thespread of fluorescent dye LY in cultured astrocyte syncytia via scrape-loading. The results showed that LYdiffusion was significantly inhibited in cells treated with Carbenoxolone disodium (CBX; 50 μM), similar to the effects of CXCL12 and CXCL11 .
PLoS Pathog

Anti-orthopoxvirus drugs inhibit lumpy skin disease virus replication by targeting viral DNA polymerase. [Abstract]

2026 Jan 26;22(1):e1013903. PMID: 41587213
Biol Reprod

Suppression of FOXO3 by BMP signaling contribute to the different primordial germ cell proliferation between layers and broilers. [Abstract]

2025 May 13;112(5):942-954. PMID: 39987556
Food Chem Toxicol

Unveiling the mechanisms of trichloroethylene hypersensitivity syndrome: Exploring the role of connexin 43 gap junctions in severe skin damage. [Abstract]

2024 May:187:114594. PMID: 38485042
Res Sq

2025 Sep 11.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (175.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7520 mL

8.7602 mL

17.5205 mL

5 mM

0.3504 mL

1.7520 mL

3.5041 mL

10 mM

0.1752 mL

0.8760 mL

1.7520 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.38 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Références

[1]. Michalski K, et al. Carbenoxolone inhibits Pannexin1 channels through interactions in the first extracellular loop. J Gen Physiol. 2016;147(2):165-174. [Content Brief]

[2]. Sharma S, et al. Inhibition of Alzheimer's amyloid-beta aggregation in-vitro by carbenoxolone: Insight into mechanism of action. Neurochem Int. 2017;108:481-493. [Content Brief]

[3]. Crespo Yanguas S, et al. TAT-Gap19 and Carbenoxolone Alleviate Liver Fibrosis in Mice. Int J Mol Sci. 2018;19(3):817. Published 2018 Mar 12. [Content Brief]

[4]. Hirata K, et al. Formulation of carbenoxolone for delivery to the skin. Int J Pharm. 2013;448(2):360-365. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7520 mL	8.7602 mL	17.5205 mL	43.8012 mL
	5 mM	0.3504 mL	1.7520 mL	3.5041 mL	8.7602 mL
	10 mM	0.1752 mL	0.8760 mL	1.7520 mL	4.3801 mL
	15 mM	0.1168 mL	0.5840 mL	1.1680 mL	2.9201 mL
	20 mM	0.0876 mL	0.4380 mL	0.8760 mL	2.1901 mL
	25 mM	0.0701 mL	0.3504 mL	0.7008 mL	1.7520 mL
	30 mM	0.0584 mL	0.2920 mL	0.5840 mL	1.4600 mL
	40 mM	0.0438 mL	0.2190 mL	0.4380 mL	1.0950 mL
	50 mM	0.0350 mL	0.1752 mL	0.3504 mL	0.8760 mL
	60 mM	0.0292 mL	0.1460 mL	0.2920 mL	0.7300 mL
	80 mM	0.0219 mL	0.1095 mL	0.2190 mL	0.5475 mL
	100 mM	0.0175 mL	0.0876 mL	0.1752 mL	0.4380 mL

Keywords

Carbenoxolone

10 Cited Publications

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Carbenoxolone

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Publications Citing Use of MedChemExpress (MCE) Carbenoxolone

Activité biologique

Chemical Information

Publications (10)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Carbenoxolone

Neuronal Signaling Compound Library

FDA-Approved Drug Library

CNS-Penetrant Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Cytoskeleton Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Alzheimer's Disease Compound Library

Neuroprotective Compound Library

Neurodegenerative Disease-related Compound Library

Mechanoreceptors Compound Library

Rare Diseases Drug Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Carbenoxolone

Activité biologique

Chemical Information

Publications (10)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Carbenoxolone Related Classifications

HY-B1588 Related Classifications