甘珀酸钠

生物活性靶点体外研究体内研究甘珀酸钠试剂级价格

甘珀酸钠

CAS号:7421-40-1
英文名:Carbenoxolone disodium
中文名:甘珀酸钠
CBNumber:CB3680281
分子式:C34H48Na2O7
分子量:614.72
MOL File:7421-40-1.mol

甘珀酸钠化学性质

熔点 :>275°C (dec.)
储存条件 :2-8°C
溶解度 :Methanol (Slightly), Water (Slightly)
形态 :Solid
酸度系数(pKa) :pKa1 4.18; pKa2 5.52(at 25℃)
颜色 :White to Off-White
水溶解性 :Soluble in water to 100 mM.
稳定性 :Hygroscopic
LogP :7.083 (est)
CAS 数据库 :7421-40-1(CAS DataBase Reference)

安全信息

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)

甘珀酸钠化学药品说明书

甘珀酸钠胶囊
甘珀酸钠片

甘珀酸钠性质、用途与生产工艺

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.

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.