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薁磺酸钠

薁磺酸钠用途

Sodium gualenate (Guaiazulenesulfonate sodium) 是桂皮烯的亲水性衍生物,具有优良的抗炎和愈伤作用,主要用于治疗十二指肠溃疡,胃溃疡和胃炎。

薁磺酸钠名称

[ CAS 号 ]:
6223-35-4

[ 中文名 ]:
磺酸钠

[ 英文名 ]:
sodium gualenate

[中文别名 ]:

[英文别名 ]:

sodium 5-isopropyl-3,8-dimethylazulene-1-sulfonate
Gualenate de sodium
sodium gualenate
Azulene sulfonate sodium
Natrii gualenas
Sodium guiazulene sulfonate
Gualenato sodidico
Azulen SN
Azupromin

薁磺酸钠生物活性

[ 描述 ]:

Sodium gualenate (Guaiazulenesulfonate sodium) 是桂皮烯的亲水性衍生物,具有优良的抗炎和愈伤作用,主要用于治疗十二指肠溃疡,胃溃疡和胃炎。

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 炎症/免疫

[体外研究]

瓜氨酸钠是一种不稳定的化合物,在室温下以固态逐渐分解。加热后,瓜氨酸钠在1周内几乎完全分解。发现用于与水压片的芥酸钠和玉米淀粉(重量比; 1：250)的捏合混合物是稳定的。因此,在生产过程中,瓜氨酸钠可以用水稳定[1]。瓜氨酸钠略微抑制大鼠腹膜肥大细胞释放组胺,并强烈抑制fMLP诱导的白细胞迁移[2]。

[体内研究]

瓜氨酸钠经常用于治疗人胃炎。细胞保护被定义为瓜氨酸钠保护胃粘膜的主要机制,体内抗菌作用也已被证实[2]。

[参考文献]

[1]. Nakamichi K, et al. Stabilization of sodium guaiazulene sulfonate in granules for tableting prepared using a twin-screw extruder. Eur J Pharm Biopharm. 2003 Nov;56(3):347-54.

[2]. Cao T, et al. Synthesis and Biological Evaluation of 3, 8-dimethyl-5-isopropylazulene Derivatives as Anti-gastric Ulcer Agent. Chem Biol Drug Des. 2016 Aug;88(2):264-71.

[相关活性小分子]

薁磺酸钠物理化学性质

[ 熔点 ]:
98°C(lit.)

[ 分子式 ]:
C₁₅H₁₇NaO₃S

[ 分子量 ]:
300.348

[ 精确质量 ]:
300.079620

[ PSA ]:
65.58000

[ LogP ]:
4.51650

[ 外观性状 ]:
固体;Blue to Dark blue powder to crystaline

[ 储存条件 ]:
<0°C;存放于惰性气体之中;避免光,湿气 (分解),加热

薁磺酸钠毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CO4826000

CHEMICAL NAME :: 1-Azulenesulfonic acid, 5-isopropyl-3,8-dimethyl-, sodium salt

CAS REGISTRY NUMBER :: 6223-35-4

LAST UPDATED :: 199806

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C15-H18-O3-S.Na

MOLECULAR WEIGHT :: 301.38

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6380 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 19,615,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 180 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: SHNSAS Shinryo to Shinyaku. Medical Consultation and New Remedies. (Iji Shuppan Sha, 1-2-8 Shinkawa, Chuo-Ku, Tokyo 104, Japan) V.1- 1964- Volume(issue)/page/year: 11,2533,1974

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 520 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

REFERENCE :: SHNSAS Shinryo to Shinyaku. Medical Consultation and New Remedies. (Iji Shuppan Sha, 1-2-8 Shinkawa, Chuo-Ku, Tokyo 104, Japan) V.1- 1964- Volume(issue)/page/year: 11,2533,1974

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1540 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 19,615,1969

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 105 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :: SHNSAS Shinryo to Shinyaku. Medical Consultation and New Remedies. (Iji Shuppan Sha, 1-2-8 Shinkawa, Chuo-Ku, Tokyo 104, Japan) V.1- 1964- Volume(issue)/page/year: 11,2533,1974

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 145 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

REFERENCE :: SHNSAS Shinryo to Shinyaku. Medical Consultation and New Remedies. (Iji Shuppan Sha, 1-2-8 Shinkawa, Chuo-Ku, Tokyo 104, Japan) V.1- 1964- Volume(issue)/page/year: 11,2533,1974

薁磺酸钠安全信息

[ RTECS号 ]:
CO4826000

[ 海关编码 ]:
2904100000

薁磺酸钠合成路线

详细合成路线

薁磺酸钠上下游产品

薁磺酸钠上游产品

薁磺酸钠下游产品

薁磺酸钠海关

[ 海关编码 ]: 2904100000

[ 中文概述 ]:
2904100000 仅含磺基的衍生物及其盐和乙酯。监管条件:无。增值税率:17.0%。退税率:9.0%。最惠国关税:5.5%。普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2904100000 derivatives containing only sulpho groups, their salts and ethyl esters。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:5.5%。General tariff:30.0%