甘珀酸钠
中文名称:
甘珀酸钠
中文同义词:
甘珀酸钠;甘珀酸 二钠盐;氢琥珀酸甘草次酸;卡柏若克索龙;氢琥珀酸甘草次酸二钠盐;18β-甘草次酸半琥珀酸酯二钠
英文名称:
Carbenoxolone disodium
英文同义词:
(3BETA-HYDROXY-11-OXOOLEAN-12-EN-30-OIC ACID 3-HEMISUCCINATE) DISODIUM SALT;CARBENOXOLONE DISODIUM SALT;CARBENOXOLONE SODIUM;18-beta-glycyrrhetinicacidhydrogensuccinate,disodiumsalt;20-beta)-3-bet;3-beta-hydroxy-11-oxoolean-12-en-30-oicacidhydrogensuccinate,disodiumsal;3-o-(beta-carboxypropionyl)-11-oxo-18-beta-olean-12-en-30-oicacid,disodium;disodiumglycyrrhetinylsuccina
CAS号:
7421-40-1
分子式:
C34H48Na2O7
分子量:
614.72
EINECS号:
231-044-0
相关类别:
标准品;中药对照品;小分子抑制剂;OPTAFLEXX;Heterocycles;Intermediates Fine Chemicals;Pharmaceuticals;Miscellaneous;Steroids
Mol文件:
7421-40-1.mol
储存条件
2-8°C
酸度系数(pKa)
pKa1 4.18; pKa2 5.52(at 25℃)
水溶解性
Soluble in water to 100 mM.
CAS 数据库
7421-40-1(CAS DataBase Reference)
生物活性
Carbenoxolone disodium 是甘草酸 (HY-N0184) 的活性代谢物和人 11β-HSD 和细菌 3α, 20β-HSD 的抑制剂。Carbenoxolone disodium 是一种缝隙连接的解耦剂 (gap junctions) 和并且可以有效抑制牛痘病毒生长。Carbenoxolone disodium 可用于研究消化性、食道和口腔溃疡和炎症的相关研究。
靶点
IC50: human 11β-HSD; bacterial 3α, 20β-HSD; gap junction; Vaccinia virus
体外研究
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.Carbenoxolone (30 μM; pre-treatment 1 hour) does not upregulate PP2A expression, but induces the late protein A27 expression in hacat cells.
Cell Viability Assay
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
Cell Line: HaCaT cells
Concentration: 30 μM
Incubation Time: Pre-treatment 1 hour
Result: Presented an obvious upregulation of A27.
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.
Cell Line:
HaCaT cells
Concentration:
30 μM
Incubation Time:
Pre-treatment 1 hour
Result:
Presented an obvious upregulation of A27.
体内研究
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.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).
Animal Model: Male BALB/c mice
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.
Animal Model:
Male BALB/c mice
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.
类别
有毒物质
毒性分级
中毒
急性毒性
口服-大鼠 LD50: 2450 毫克/公斤; 腹腔-小鼠 LD50: 120 毫克/公斤
可燃性危险特性
热分解排出有毒氧化钠烟雾
储运特性
库房低温通风干燥
灭火剂
水, 二氧化碳, 泡沫, 干粉
危险品标志
Xn,Xi
危险类别码
22-36
安全说明
26-36
WGK Germany
3
RTECS号
RK0250000
毒性
LD50 in male mice (mg/kg): 198 i.v.; 120 i.p.; in male rats (mg/kg): 3200 orally (Robson, Sullivan)
