| Bioactivity | Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD[1]. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication[2]. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation. Carbenoxolone disodium inhibits Vaccinia virus replication. |
| Target | IC50: human 11β-HSD; bacterial 3α, 20β-HSD; gap junction; Vaccinia virus |
| Invitro | Carbenoxolone disodium (6-150 μM; pre-treatment 1 hour) inhibits Vaccinia virus (VACV) replication in a gap junction-independent in HaCaT cells, and it has toxicity effects on VACV-A5L-EGFP infected cells at 48 h[2].Carbenoxolone (30 μM; pre-treatment 1 hour) does not upregulate PP2A expression, but induces the late protein A27 expression in hacat cells[2]. Cell Viability Assay[2] Cell Line: |
| In Vivo | Carbenoxolone (intraperitoneal injection; 100, 200 and 300 mg/kg; 30, 60 and 60 min before Diazepam) does not induce a muscle relaxant activity and shows muscle relaxant activity compared to normal saline, and this effect was more than diazepam in the traction test[3].Carbenoxolone (intraperitoneal injection; 100, 200 and 300 mg/kg; 30, 60 and 60 min before Pentylenetetrazole) significantly increases sleeping time and decreases latency in mice as a dose-dependent manner in Pentylenetetrazole (PTZ) Seizure model. The ED50 value is 83.3 mg/kg (%95 CL:556.29)[3]. Animal Model: |
| Name | Carbenoxolone disodium |
| CAS | 7421-40-1 |
| Formula | C34H48Na2O7 |
| Molar Mass | 614.72 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. W L Duax, et al. Steroid Dehydrogenase Structures, Mechanism of Action, and Disease. Vitam Horm. 2000;58:121-48. [2]. Hossein Hosseinzadeh, et al. Anticonvulsant, Sedative and Muscle Relaxant Effects of Carbenoxolone in Mice. BMC Pharmacol. 2003 Apr 29;3:3. [3]. Ismar R Haga, et al. Carbenoxolone-mediated Cytotoxicity Inhibits Vaccinia Virus Replication in a Human Keratinocyte Cell Line. Sci Rep. 2018 Nov 16;8(1):16956. [4]. Ismar R Haga, et al. Carbenoxolone-mediated cytotoxicity inhibits Vaccinia virus replication in a human keratinocyte cell line. Sci Rep. 2018 Nov 16;8(1):16956. |