基本信息
中文别名
阿拉磷L-丙氨酰-L-1-氨基乙基膦酸
英文别名
ALAPHOSPHINALAFOSFALIN
Alafosfalin >97%
L-ALANYL-L-ALA(P)-OH
L-ALANYL-L-1-AMINOETHYLPHOSPHONIC ACID
(S)-ALANYL-(R)-1-AMINOETHYLPHOSPHONIC ACID
[(1R)-1-[[(2S)-2-Aminopropanoyl]amino]ethyl]phosphonic acid
L-ALANYL-L-ALA(P)-OH, (S)-ALANYL-(R)-1-AMINOETHYLPHOSPHONIC ACID
Phosphonic acid, P-[(1R)-1-[[(2S)-2-amino-1-oxopropyl]amino]ethyl]-
(S)-Alanyl-(R)-1-aminoethylphosphonic acid, Alafosfalin, Alaphosphin
物理化学性质
熔点295-296° (dec)
比旋光度D20 -44.0° (c = 1 in H2O)
密度1.395±0.06 g/cm3(Predicted)
储存条件2-8°C
酸度系数(pKa)2.60±0.10(Predicted)
形态粉末
颜色无色或白色
旋光性 (optical activity)[α]20/D 45±2°, c = 1% in H2O
Merck13,202
BRN4801790
常见问题列表
生物活性
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。靶点
Antibacterial
体外研究
Alafosfalin is highly active against Escherichia coli and moderately active against Serratia , Klebsiella , Enterobacter , and Citrobacter , but less active against gram-positive organisms than were beta-lactams such as cephazolin or ampicillin and inactive against indole-positive Proteus , Pseudomonas , and Acinetobacter .
体内研究
After s.c. administration to rats, Alafosfalin is rapidly absorbed with half-lives (t 1/2 ) of approximately 20 minutes.
Animal Model: | Pairs of male SpragueDawley rats (250 to 350 g) |
Dosage: | 20, 100, and 500 mg/ kg (single doses) or 800 mg/kg per day for 14 days (Pharmacokinetic Analysis) |
Administration: | Administrated by s.c. |
Result: | Rapidly absorbed; peak concentrations were found within 20 minutes of dosing with half-lives of approximately 20 minutes. |