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4-氨基苯甲脒二盐酸盐

4-氨基苯甲脒二盐酸盐用途

4-氨基苯甲脒(对氨基苯甲酰胺)盐酸盐是一种强胰蛋白酶抑制剂,也是一种相对较弱的尿激酶型纤溶酶原激活剂(uPA)抑制剂(Ki=82μM)。4-氨基苯甲脒可以抑制SCID小鼠中人类前列腺肿瘤的生长[1][2]。

4-氨基苯甲脒二盐酸盐名称

[ CAS 号 ]:
2498-50-2

[ 中文名 ]:
4-氨基苯甲脒二盐酸盐

[ 英文名 ]:
4-Aminobenzamidine dihydrochloride

[中文别名 ]:

[英文别名 ]:

4-AMBA dihydrochloride
4-aminobenzimidamide dihydrochloride
4-aminobenzimidine dihydrochloride
MFCD00013001
4-aminobenzoamidine dihydrochloride
P-AMINOBENZAMIDINE DIHCL
4-AMINOBENZAMIDINE 2HCL
Benzenecarboximidamide,4-amino-,dihydrochloride
4-Aminobenzenecarboximidamide dihydrochloride
p-Aminobenzamidine dihydrochloride

4-氨基苯甲脒二盐酸盐生物活性

[ 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 >> 癌症

[ 靶点 ]

Trypsin[1] Ki: 82 μM (uPA)[1]

[参考文献]

[1]. Nguyen AL, et al. The development and application of a new affinity partitioning system for enzyme isolation and purification. Enzyme Microb Technol. 1990 Sep;12(9):663-8.

[2]. Billström A, et al. The urokinase inhibitor p-aminobenzamidine inhibits growth of a human prostate tumor in SCID mice. Int J Cancer. 1995 May 16;61(4):542-7.

4-氨基苯甲脒二盐酸盐物理化学性质

[ 密度 ]:
1.26g/cm3

[ 沸点 ]:
289.8ºC at 760 mmHg

[ 熔点 ]:
>300 °C(lit.)

[ 分子式 ]:
C₇H₁₁Cl₂N₃

[ 分子量 ]:
208.088

[ 闪点 ]:
129ºC

[ 精确质量 ]:
207.033005

[ PSA ]:
75.89000

[ LogP ]:
3.53810

[ 外观性状 ]:
白色结晶粉末

[ 蒸汽压 ]:
0.00216mmHg at 25°C

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
水溶性：完全溶解

4-氨基苯甲脒二盐酸盐MSDS

4-氨基苯甲脒二盐酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: CV6126500

CHEMICAL NAME :: Benzamidine, p-amino-, dihydrochloride

CAS REGISTRY NUMBER :: 2498-50-2

LAST UPDATED :: 199007

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C7-H9-N3.2Cl-H

MOLECULAR WEIGHT :: 208.11

WISWESSER LINE NOTATION :: ZR DYZUM &GH 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 240 mg/kg

TOXIC EFFECTS :: Brain and Coverings - meningeal changes Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes

REFERENCE :: BIREBV Biology of Reproduction. (Soc. for the Study of Reproduction, 309 W. Clark St., Champaign, IL 61820) V.1- 1969- Volume(issue)/page/year: 20,1045,1979

4-氨基苯甲脒二盐酸盐安全信息

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn:Harmful;

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S37/39

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

[ WGK德国 ]:
3

[ RTECS号 ]:
CV6126500

4-氨基苯甲脒二盐酸盐合成路线

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4-氨基苯甲脒二盐酸盐制备

对硝基苯甲酸经清化、加成、胺化、还原而得。

4-氨基苯甲脒二盐酸盐文献

Comparative study on the inhibition of plasmin and delta-plasmin via benzamidine derivatives.

Biochem. Biophys. Res. Commun. 457(3) , 358-62, (2015)

The potent fibrinolytic enzyme, plasmin has numerous clinical applications for recannulizing vessels obstructed by thrombus. Despite its diminutive size, 91 kDa, success in the recombinant expression ...

p-Aminobenzamidine as a fluorescent probe for the active site of serine proteases.

J. Biol. Chem. 257 , 3014, (1982)

p-Aminobenzamidine is weakly fluorescent in neutral aqueous buffer, with excitation and emission maxima at 293 and 376 nm, respectively. Binding to trypsin results in a blue shift of the emission peak...

Comparative studies on the inhibition of trypsin, plasmin, and thrombin by derivatives of benzylamine and benzamidine.

Eur. J. Biochem. 6 , 502, (1968)

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