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盐酸西曲酸酯

盐酸西曲酸酯用途

盐酸西曲沙汀(DV-1006),一种具有粘膜保护作用的口服活性抗溃疡剂,可用于胃溃疡研究[1]。盐酸西曲沙汀是一种有效的顶体蛋白酶顶体蛋白酶抑制剂,Ki和IC50分别为0.94μM和3.3μM[2]。

盐酸西曲酸酯名称

[ CAS 号 ]:
27724-96-5

[ 中文名 ]:
盐酸西曲酸酯

[ 英文名 ]:
Cetraxate HCl

[英文别名 ]:

盐酸西曲酸酯生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> Ser/Thr蛋白酶

研究领域 >> 炎症/免疫

[参考文献]

[1]. Fumihiko Katagiri, et al. Cetraxate raises levels of calcitonin gene-related peptide and substance P in human plasma. J Pharm Pharmacol. 2004 Apr;56(4):557-61.

[2]. H Sumi, et al. Inhibitors of the acrosomal proteinase acrosin: human urinary trypsin inhibitor (UTI) and 4-(2-carboxyethyl) phenyl trans 4-aminomethylcyclohexanecarboxylate hydrochloride (DV-1006). Experientia. 1980 Sep 15;36(9):1103-4.

盐酸西曲酸酯物理化学性质

[ 密度 ]:
1.182g/cm3

[ 沸点 ]:
480.9ºC at 760mmHg

[ 熔点 ]:
238-240ºC

[ 分子式 ]:
C₁₇H₂₄ClNO₄

[ 分子量 ]:
341.83000

[ 闪点 ]:
244.6ºC

[ 精确质量 ]:
341.13900

[ PSA ]:
89.62000

[ LogP ]:
3.87660

[ 折射率 ]:
1.551

[ 储存条件 ]:
库房低温通风干燥

盐酸西曲酸酯毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MW5350000

CHEMICAL NAME :: Hydrocinnamic acid, p-hydroxy-, 4-(aminomethyl)cyclohexanecarboxylate hydrochloride, trans-

CAS REGISTRY NUMBER :: 27724-96-5

LAST UPDATED :: 198703

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C17-H23-N-O4.Cl-H

MOLECULAR WEIGHT :: 341.87

WISWESSER LINE NOTATION :: L6TJ AVOR D2VQ& D1Z &GH

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 :: 1503 mg/kg

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

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 21,935,1979

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 716 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - hypermotility, diarrhea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 12,265,1976

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1415 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 298 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4310 mg/kg

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

REFERENCE :: YAKUD5 Gekkan Yakuji. Pharmaceuticals Monthly. (Yakugyo Jihosha, Inaoka Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo 101, Japan) V.1- 1959- Volume(issue)/page/year: 21,935,1979

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1520 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 12,265,1976

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 4210 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 666 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979