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甘珀酸

甘珀酸用途

Carbenoxolone 是甘草次酸的半合成衍生物,由于其抗炎特性,被广泛用于消化不良和消化性溃疡的治疗。Carbenoxolone,半通道和间隙连接蛋白抑制剂,具有治疗慢性肝病的治疗潜力。Carbenoxolone 抑制 Aβ42 聚集,是抗 AD 治疗潜力的合适候选者。Carbenoxolone 是小分子 Pannexin1 (Panx1,是一种 ATP 释放通道) 抑制剂,通过调节第一个细胞外环来减弱 Panx1 通道活性。 Carbenoxolone 是 11β-羟基类固醇脱氢酶1型 (11β-HSD1) 抑制剂,可将无活性的糖皮质激素转化为活性形式。 Carbenoxolone 具有抗 DENV 感染的抗病毒活性,靶点针对病毒本身。
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甘珀酸名称

[ CAS 号 ]:
5697-56-3

[ 中文名 ]:
甘珀酸

[ 英文名 ]:
Carbenoxolone

[英文别名 ]:

甘珀酸生物活性

[ 描述 ]:

Carbenoxolone 是甘草次酸的半合成衍生物,由于其抗炎特性,被广泛用于消化不良和消化性溃疡的治疗。Carbenoxolone,半通道和间隙连接蛋白抑制剂,具有治疗慢性肝病的治疗潜力。Carbenoxolone 抑制 Aβ42 聚集,是抗 AD 治疗潜力的合适候选者。Carbenoxolone 是小分子 Pannexin1 (Panx1,是一种 ATP 释放通道) 抑制剂,通过调节第一个细胞外环来减弱 Panx1 通道活性。 Carbenoxolone 是 11β-羟基类固醇脱氢酶1型 (11β-HSD1) 抑制剂,可将无活性的糖皮质激素转化为活性形式。 Carbenoxolone 具有抗 DENV 感染的抗病毒活性,靶点针对病毒本身。

[ 相关类别 ]:

研究领域 >> 感染
研究领域 >> 炎症/免疫
研究领域 >> 神经疾病

[参考文献]

[1]. Sharma S, et al. Inhibition of Alzheimer's amyloid-beta aggregation in-vitro by carbenoxolone:Insight into mechanism of action. Neurochem Int. 2017 Sep;108:481-493.

[2]. Crespo Yanguas S, et al. TAT-Gap19 and Carbenoxolone Alleviate Liver Fibrosis in Mice. Int J Mol Sci. 2018 Mar 12;19(3). pii: E817.

[3]. Hirata K, et al. Formulation of carbenoxolone for delivery to the skin. Int J Pharm. 2013 May 20;448(2):360-5.

[4]. Michalski K, et al. Carbenoxolone inhibits Pannexin1 channels through interactions in the first extracellular loop. J Gen Physiol. 2016 Feb;147(2):165-74.

[5]. Kim J, et al. Protective effect of carbenoxolone on ER stress-induced cell death in hypothalamic neurons. Biochem Biophys Res Commun. 2015 Dec 25;468(4):793-9.

[6]. Pu J, et al. Antiviral activity of Carbenoxolone disodium against dengue virus infection. J Med Virol. 2017 Apr;89(4):571-581

甘珀酸物理化学性质

[ 密度 ]:
1.20

[ 沸点 ]:
687.4ºC at 760 mmHg

[ 熔点 ]:
291-294 °C

[ 分子式 ]:
C34H50O7

[ 分子量 ]:
570.75700

[ 闪点 ]:
211.6ºC

[ 精确质量 ]:
570.35600

[ PSA ]:
117.97000

[ LogP ]:
6.82830

[ 外观性状 ]:
白色结晶粉末

[ 储存条件 ]:
通风低温干燥

甘珀酸MSDS

甘珀酸毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
RK0200000
CHEMICAL NAME :
Olean-12-en-30-oic acid, 3-beta-hydroxy-11-oxo-, hydrogen succinate
CAS REGISTRY NUMBER :
5697-56-3
LAST UPDATED :
199712
DATA ITEMS CITED :
10
MOLECULAR FORMULA :
C34-H50-O7
MOLECULAR WEIGHT :
570.84
WISWESSER LINE NOTATION :
L F6 E6 B666 CV DUTJ A1 HVQ H1 K1 N1 O1 S1 S1 TOV2VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
120 mg/kg/56D-I
TOXIC EFFECTS :
Peripheral Nerve and Sensation - flaccid paralysis without anesthesia (usually neuromuscular blockage) Behavioral - muscle weakness
REFERENCE :
BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 2,150,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2450 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,323,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
128 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,323,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1720 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,323,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1400 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4224327
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
290 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4363816
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
1060 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,323,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
371 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,323,1980 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
1313 mg/kg
SEX/DURATION :
female 1-21 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - biochemical and metabolic
REFERENCE :
DBTGAJ Diabetologia. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) V.1- 1965- Volume(issue)/page/year: 39,1299,1996
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甘珀酸安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38:Irritating to eyes, respiratory system and skin .

[ 安全声明 (欧洲) ]:
S26-S36-S37/39

[ WGK德国 ]:
3

[ 海关编码 ]:
2938909030

甘珀酸海关

[ 海关编码 ]: 2938909030

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区域:上海市浦东新区

价格:
¥需询单/1g

联系人:赖经理

产品详情:Carbenoxolone


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区域:上海市浦东新区

价格:
¥729.0/5g ¥2499.0/25g ¥199.0/1g ¥需询单/1g

联系人:阿拉丁

产品详情:甘珀酸


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相关化合物

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