[CAS NO. 7421-40-1] Carbenoxolone disodium
PRODUCTS SPECIFICATIONS [7421-40-1]
DESCRIPTION [7421-40-1]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 614.72 |
| Molecular Formula | C34H48Na2O7 |
| SMILES | CC(C)([C@]1([H])CC[C@@]([C@@]2(CC[C@]3(CC[C@](C[C@@]3([H])C2=C4)(C)C(O[Na])=O)C)C)5C)[C@@H](OC(CCC(O[Na])=O)=O)CC[C@]1(C)[C@@]5([H])C4=O |
Summary
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.
In Vitro
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]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [2]
| Cell Line: | HaCaT cells |
| Concentration: | 6 μM, 12 μM, 30 μM, 60 μM, 150 μM |
| Incubation Time: | Pre-treatment 1 hour |
| Result: | Had no toxicity until 48 hours at high dose in virus-infected cells. |
Western Blot Analysis [2]
| Cell Line: | HaCaT cells |
| Concentration: | 30 μM |
| Incubation Time: | Pre-treatment 1 hour |
| Result: | Presented an obvious upregulation of A27. |
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 ED
50
value is 83.3 mg/kg (%95 CL:556.29)
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male BALB/c mice [3] |
| Dosage: | 100, 200 and 300 mg/kg |
| Administration: | Intraperitoneal injection; 30, 60 and 60 min before Pentylenetetrazole |
| Result: | Significantly increased the sleeping time in mice. |
Appearance
Solid
Shipping
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)
Solvent & Solubility
H 2 O : 50 mg/mL ( 81.34 mM ; Need ultrasonic)
DMSO : 16.67 mg/mL ( 27.12 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6268 mL | 8.1338 mL | 16.2676 mL |
| 5 mM | 0.3254 mL | 1.6268 mL | 3.2535 mL |
| 10 mM | 0.1627 mL | 0.8134 mL | 1.6268 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 6.25 mg/mL (10.17 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 1.67 mg/mL (2.72 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.93 mg/mL (1.51 mM); Clear solution
References
- [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.
Synonyms