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吲哚布芬

吲哚布芬用途

Indobufen 是一种血小板聚集抑制剂。Indobufen 是一种可逆的血小板环加氧酶 (Cox) 活性抑制剂。Indobufen 抑制血栓素 A2 (TxA2) 合成。Indobufen 降低单核细胞中的组织因子。

吲哚布芬名称

[ CAS 号 ]:
63610-08-2

[ 中文名 ]:
吲哚布芬

[ 英文名 ]:
Indobufen

[中文别名 ]:

2-[4-(1-氧代-2-异吲哚啉基)苯基]丁酸

[英文别名 ]:

2-[4-(1-Oxo-1,3-dihydro-isoindol-2
MFCD00572250
K-3920
UNII-6T9949G4LZ
EINECS 264-364-4
2-(4-(1-Oxo-2-isoindolinyl)phenyl)butyric acid
Ibustrin
2-[4-(1-Carboxypropyl)phenyl]-1-isoindolinone
(±)-2-[p-(1-Oxo-2-isoindolinyl)phenyl]butyric Acid
Indobufen

吲哚布芬生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 免疫及炎症 >> COX

[ 靶点 ]

COX

[体外研究]

Indobufen不影响Cox-1和Cox-2蛋白,而Indobufen降低TxB2水平。吲哚布芬抑制LPS刺激的单核细胞中的TxA2但不抑制PGE2合成。吲哚布芬降低了ERK1/2磷酸化的程度,而磷酸化的p38水平则没有改变[1]。

[参考文献]

[1]. Eligini S, et al. Indobufen inhibits tissue factor in human monocytes through a thromboxane-mediated mechanism. Cardiovasc Res. 2006 Jan;69(1):218-26.

吲哚布芬物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
518.1±50.0 °C at 760 mmHg

[ 熔点 ]:
33-34 °C(lit.)

[ 分子式 ]:
C₁₈H₁₇NO₃

[ 分子量 ]:
295.33

[ 闪点 ]:
267.1±30.1 °C

[ 精确质量 ]:
295.120850

[ PSA ]:
57.61000

[ LogP ]:
3.30

[ 外观性状 ]:
固体;White to Light yellow powder to crystal

[ 蒸汽压 ]:
0.0±1.4 mmHg at 25°C

[ 折射率 ]:
1.630

[ 储存条件 ]:
存放于惰性气体之中;避免空气

吲哚布芬毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: ET5955800

CHEMICAL NAME :: Butyric acid, 2-(p-(1-oxo-2-isoindolinyl)phenyl)-, (+-)-

CAS REGISTRY NUMBER :: 63610-08-2

LAST UPDATED :: 199710

DATA ITEMS CITED :: 8

MOLECULAR FORMULA :: C18-H17-N-O3

MOLECULAR WEIGHT :: 295.36

WISWESSER LINE NOTATION :: T56 BVN DHJ CR DY2&VQ

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 :: 373 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,109,1979

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 345 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,109,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 333 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,109,1979

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 697 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,109,1979

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 365 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,109,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 370 mg/kg

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

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,109,1979

吲哚布芬安全信息

[ WGK德国 ]:
3

[ 海关编码 ]:
2942000000

吲哚布芬制备

方法1：3.92g(0.02mo1)邻氰基苄基溴和(0.02mo1)2-(4-氨基苯基)丁酸溶于80ml99.9%乙醇中，回流6h。减压浓缩至约30ml后，将其倾入约400ml乙醚中。分离出的固体用乙醇和乙醚重结晶，得2-[4-(1-亚氨基-2-异吲哚啉基)苯基]丁酸，收率80%。将其溶于60ml 95%乙醇后，加到6.9lg(0.05mo1)碳酸钾溶于50ml水的溶液。回流12h后得澄清溶液。减压蒸去乙醇，过滤除去不溶物，滤液用8%的盐酸(约30ml)酸化。过滤析出的沉淀，依次用80ml水、15ml 8%盐酸和40ml水洗，再用95%乙醇重结晶，得吲哚布芬，收率84%，熔点180～182℃。
方法2：邻苯二甲酸酐、2-(4-氨基苯基)丁酸和乙酸混合，回流。倾入冰水，过滤，水洗，干燥，乙醇重结晶，得2-[4-(1，3-二氧代-2-异吲哚啉基)苯基]丁酸，收率85.1%。将其溶于乙酸，在剧烈搅拌下加入锌粉，回流。过滤，滤渣用乙酸洗。滤液减压蒸去溶剂，剩余物悬浮于水中，用碳酸钠溶液中和至Ph值6。过滤，乙醇重结晶，得吲哚布芬，收率68.5%，熔点181～183℃。

吲哚布芬海关

[ 海关编码 ]: 2918300090

[ 中文概述 ]:
2918300090 其他含醛基或酮基不含其他含氧基羧酸（包括酸酐、酰卤化物、过氧化物和过氧酸及该税号的衍生物）. 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:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2918300090 other carboxylic acids with aldehyde or ketone function but without other oxygen function, their anhydrides, halides, peroxides, peroxyacids and their derivatives。Supervision conditions:None。VAT:17.0%。Tax rebate rate:9.0%。MFN tariff:6.5%。General tariff:30.0%