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阿加曲班

阿加曲班用途

Argatroban单水合物是thrombin选择性抑制剂。

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阿加曲班名称

[ CAS 号 ]:
141396-28-3

[ 中文名 ]:
阿加曲班

[ 英文名 ]:
Argatroban

[中文别名 ]:

阿加曲班

[英文别名 ]:

Argatroban
MFCD00895735
Argatroban monohydrate
Argatroban anhydrous
UNII:IY90U61Z3S
UNII:OCY3U280Y3
Argatroban (monohydrate)

阿加曲班生物活性

[ 描述 ]:

Argatroban单水合物是thrombin选择性抑制剂。

[ 相关类别 ]:

信号通路 >> 代谢酶/蛋白酶 >> 凝血酶

研究领域 >> 心血管疾病

[参考文献]

[1]. Kawada, T., et al., Argatroban, an attractive anticoagulant, for left heart bypass with centrifugal pump for repair of traumatic aortic rupture. Jpn J Thorac Cardiovasc Surg, 1999. 47(3): p. 104-9.

[2]. Jang, I.K., et al., A multicenter, randomized study of argatroban versus heparin as adjunct to tissue plasminogen activator (TPA) in acute myocardial infarction: myocardial infarction with novastan and TPA (MINT) study. J Am Coll Cardiol, 1999. 33(7): p. 1879-85.

[相关活性小分子]

阿加曲班物理化学性质

[ 密度 ]:
1.5±0.1 g/cm3

[ 沸点 ]:
801.3±75.0 °C at 760 mmHg

[ 熔点 ]:
-41.5 °C

[ 分子式 ]:
C₂₃H₃₈N₆O₆S

[ 分子量 ]:
526.65

[ 闪点 ]:
438.4±37.1 °C

[ PSA ]:
195.32000

[ LogP ]:
2.56

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 蒸汽压 ]:
0.0±3.0 mmHg at 25°C

[ 折射率 ]:
1.674

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
水溶性：不溶；微溶：甲醇；极微溶：乙醇；不溶：丙酮,乙醚

阿加曲班MSDS

详细MSDS(安全技术说明书)

阿加曲班毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM6126625

CHEMICAL NAME :: 2-Piperidinecarboxylic acid, 1-(5-((aminoiminomethyl)amino)-1-oxo-2-(((1,2,3,4-tet rahydro-3- methyl-8-quinolinyl)sulfonyl)amino)pentyl)methyl-, monohydrate, (2R-((2S*),2-alpha,4-beta))-

CAS REGISTRY NUMBER :: 141396-28-3

LAST UPDATED :: 199706

DATA ITEMS CITED :: 13

MOLECULAR FORMULA :: C23-H36-N6-O5-S.H2-O

MOLECULAR WEIGHT :: 526.73

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 :: >15 gm/kg

TOXIC EFFECTS :: Blood - hemorrhage Blood - normocytic anemia

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),933,1986

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 320 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity) Blood - normocytic anemia

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),933,1986

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 620 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - dyspnea Blood - normocytic anemia Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),933,1986

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >81 mg/kg

TOXIC EFFECTS :: Blood - hemorrhage

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),933,1986

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >15 gm/kg

TOXIC EFFECTS :: Blood - hemorrhage Blood - normocytic anemia

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),933,1986

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 475 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - dyspnea Blood - normocytic anemia

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),933,1986

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 3750 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Blood - normocytic anemia Skin and Appendages - dermatitis, other (after systemic exposure)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),933,1986

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: >81 mg/kg

TOXIC EFFECTS :: Blood - hemorrhage

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),933,1986 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 810 mg/kg/30D-I

TOXIC EFFECTS :: Blood - other changes

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),941,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4914 mg/kg/26W-I

TOXIC EFFECTS :: Behavioral - fluid intake Kidney, Ureter, Bladder - urine volume increased Kidney, Ureter, Bladder - other changes

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),971,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 810 mg/kg/30D-I

TOXIC EFFECTS :: Gastrointestinal - nausea or vomiting

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),951,1986 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 297 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - physical

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),1023,1986

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 22 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - other effects to embryo

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 14(Suppl 5),1049,1986

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阿加曲班安全信息

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36:Irritating to the eyes. R10:Flammable.

[ 安全声明 (欧洲) ]:
S39-S26-S16

[ 危险品运输编码 ]:
NONH for all modes of transport

[ RTECS号 ]:
TM6126610

[ 海关编码 ]:
2935009090

阿加曲班海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%