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7421-40-1

中文名稱 甘珀酸鈉
英文名稱 Carbenoxolone disodium
CAS 7421-40-1
EINECS 編號 231-044-0
分子式 C34H48Na2O7
MDL 編號 MFCD00079043
分子量 614.72
MOL 文件 7421-40-1.mol
更新日期 2024/10/24 09:33:04
7421-40-1 結(jié)構(gòu)式 7421-40-1 結(jié)構(gòu)式

基本信息

中文別名
氫琥珀酸甘草次酸二鈉鹽
18β-甘草次酸半琥珀酸酯二鈉
卡柏若克索龍
甘珀酸鈉
英文別名
(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
duogastrone
glycyrrhetinicacidhydrogensuccinate,disodiumsalt
neogel
olean-12-en-29-oicacid,3-(3-carboxy-1-oxopropoxy)-11-oxo-,disodiumsalt,(
olean-12-en-30-oicacid,3-beta-hydroxy-11-oxo-,hydrogensuccinate,disodiums
pyrogastrone
sanodin
sodium3-beta-hydroxy-11-oxo-12-oleanen-30-oatesodiumsuccinate
sodiumcarbenoxolone
ulcus-tablinen
carbenoxolone disodium
disodium 4-(20-carboxylato-11-oxo-30-beta-norolean-12-en-3-yloxy)-4-oxobutyrate
所屬類別
原料藥:抗酸及胃黏膜保護藥

物理化學(xué)性質(zhì)

熔點>275°C (dec.)
儲存條件2-8°C
儲存條件2-8°C
溶解度少許溶于甲醇和水
酸度系數(shù)(pKa)pKa1 4.18; pKa2 5.52(at 25℃)
形態(tài)固體
顏色白色至灰白色
水溶解性Soluble in water to 100 mM.
穩(wěn)定性吸濕性
LogP7.083 (est)
CAS 數(shù)據(jù)庫7421-40-1(CAS DataBase Reference)

安全數(shù)據(jù)

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H319
防范說明P305+P351+P338
危險品標志Xn,Xi
危險品標志Xn
危險類別碼22-36
危險類別碼R22-R36
安全說明26-36
安全說明S26-S36
WGK Germany3
WGK Germany3
RTECS號RK0250000
毒性LD50 in male mice (mg/kg): 198 i.v.; 120 i.p.; in male rats (mg/kg): 3200 orally (Robson, Sullivan)

7421-40-1(安全特性,毒性,儲運)

儲運特性
庫房低溫通風(fēng)干燥
毒性分級
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
可燃性危險特性
熱分解排出有毒氧化鈉煙霧
類別
有毒物質(zhì)
滅火劑
水, 二氧化碳, 泡沫, 干粉

知名試劑公司產(chǎn)品信息

常見問題列表

生物活性
Carbenoxolone disodium 是甘草酸 (HY-N0184) 的活性代謝物和人 11β-HSD 和細菌 3α, 20β-HSD 的抑制劑。Carbenoxolone disodium 是一種縫隙連接的解耦劑 (gap junctions) 和并且可以有效抑制牛痘病毒生長。Carbenoxolone disodium 可用于研究消化性、食道和口腔潰瘍和炎癥的相關(guān)研究。
靶點

IC50: human 11β-HSD; bacterial 3α, 20β-HSD; gap junction; Vaccinia virus

體外研究

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.
體內(nèi)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.
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