< 生产厂家价格 >

((1R)-1-((2S)-2-Aminopropionamido)ethyl)phosphonic acid

用途

Alafosfalin 是一种细胞壁生物合成抑制剂。Alafosfalin 是一种磷酸二肽,具有抗菌 (antibacterial) 特性。

点击显示

名称

[ CAS 号 ]:
60668-24-8

[ 中文名 ]:
阿拉磷

[ 英文名 ]:
Alafosfalin

[中文别名 ]:

[英文别名 ]:

(1R)-1-(L-alanylamino)-ethylphosphonic acid
ALAFOSFALIN
H-L-Ala-L-AlaP(OH)2
N-(S)-alanyl-(R)-1-aminoethanephosphonic acid
ALAPHOSPHIN
L-alanyl-L-1-aminoethylphosphonic acid
1R-1-(L-alanylamino)-ethanephosphonic acid
L-ALANYL-L-ALA(P)-OH
((L)-(1-((N-L-alanyl)amino)ethyl))phosphonic acid

生物活性

[ 描述 ]:

Alafosfalin 是一种细胞壁生物合成抑制剂。Alafosfalin 是一种磷酸二肽,具有抗菌 (antibacterial) 特性。

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

Antibacterial[1]

[体外研究]

阿拉福林对大肠杆菌高度有效,对沙雷菌、克雷伯菌、肠杆菌和柠檬酸杆菌具有中等活性,但对革兰氏阳性菌的活性低于β-内酰胺类药物,如头孢唑林或氨苄西林,对吲哚阳性变形杆菌、假单胞菌和不动杆菌无效[1]。

[体内研究]

给大鼠皮下注射s.c.后,阿拉福林被迅速吸收,半衰期(t1/2)约为20分钟[2]。动物模型：雄性SpragueDawley大鼠对(250~350 g)[2]剂量：20、100、500 mg/kg(单次给药)或800 mg/kg/天,连续14天(药代动力学分析)给药：由s.c.给药。结果：迅速吸收,给药后20分钟内出现峰值浓度,半衰期约为20分钟。

[参考文献]

[1]. H B Maruyama, et al. Alafosfalin, a New Inhibitor of Cell Wall Biosynthesis: In Vitro Activity Against Urinary Isolates in Japan and Potentiation With Beta-Lactams. Antimicrob Agents Chemother. 1979 Oct;16(4):444-51.

[2]. J G Allen, et al. Phosphonopeptides as Antibacterial Agents: Metabolism and Pharmacokinetics of Alafosfalin in Animals and Humans. Antimicrob Agents Chemother. 1979 Sep;16(3):306-13.

物理化学性质

[ 分子式 ]:
C₅H₁₃N₂O₄P

[ 分子量 ]:
196.14100

[ 精确质量 ]:
196.06100

[ PSA ]:
125.45000

[ LogP ]:
0.76750

[ 外观性状 ]:
白色粉末

[ 储存条件 ]:
2-8°C，密封，干燥

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

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

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

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

[ 海关编码 ]:
2931900090

上下游产品

上游产品

下游产品

海关

[ 海关编码 ]: 2931900090

[ 中文概述 ]:
2931900090. 其他有机-无机化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:AB(入境货物通关单,出境货物通关单). 最惠国关税:6.5%. 普通关税:30.0%

[ Summary ]:
2931900090. other organo-inorganic compounds. VAT:17.0%. Tax rebate rate:13.0%. Supervision conditions:AB(certificate of inspection for goods inward,certificate of inspection for goods outward). MFN tariff:6.5%. General tariff:30.0%

文献

In vitro potentiation of cephalosporins by alafosfalin against urinary tract bacteria.

Antimicrob. Agents Chemother. 21(5) , 706-10, (1982)

Potentiating activity of alafosfalin was examined in detail with 8 cephalosporins and mecillinam against 164 urinary bacteria representing 8 genera. Alafosfalin was generally comparable in activity to...

Alafosfalin as a selective agent for isolation of salmonella from clinical samples.

J. Clin. Microbiol. 40(11) , 3913-6, (2002)

The selectivity of a range of culture media for the detection of Salmonella was assessed using 435 strains of gram-negative bacteria. These media showed limited ability to inhibit non-Salmonella strai...

Synergistic antibacterial activity between L-norvalyl-L-1-aminoethylphosphonic acid and nocardicin A.

Antimicrob. Agents Chemother. 25(5) , 607-11, (1984)

The phosphonopeptide L- norvalyl -L-1- aminoethylphosphonic acid [ Nva -Ala(P)] has been studied in combination with 12 beta-lactam antibiotics for activity against Pseudomonas aeruginosa. Nocardicin ...

更多文献