乳酸甲氧苄啶

乳酸甲氧苄啶用途

Trimethoprim lactic 是一种抑菌抗生素,也是一种具有口服活性的二氢叶酸还原酶 (dihydrofolate reductase) 抑制剂。Trimethoprim lactic 对多种革兰氏阳性和革兰氏阴性需氧细菌 (Gram-positive 和 Gram-negative aerobic bacteria) 具有活性。Trimethoprim lactic 可用于尿路感染,志贺氏菌病和肺孢子菌肺炎的研究。

乳酸甲氧苄啶名称

[ CAS 号 ]:
23256-42-0

[ 中文名 ]:
乳酸甲氧苄啶

[ 英文名 ]:
Trimethoprim lactate

[中文别名 ]:

[英文别名 ]:

EINECS 245-533-1
Trimethoprim lactate
MFCD00171722
UNII:P3K8GP9FDQ

乳酸甲氧苄啶生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 感染

信号通路 >> 细胞周期/DNA损伤 >> 叶酸

信号通路 >> 抗感染 >> 细菌

[ 靶点 ]

Dihydrofolate reductase[1] Bacteria[1]

[体外研究]

甲氧苄啶通过抑制二氢叶酸还原酶(DHFR)的活性来中断叶酸代谢,DHFR将二氢叶酸还原为四氢叶酸(THF)[1]。甲氧苄啶能引起大肠杆菌细胞中的蛋白质聚集和主要热休克蛋白(Hsps)的诱导,这表明甲氧苄啶的存在导致了蛋白质的错误折叠。甲氧苄啶可诱导DnaK、DnaJ、GroEL、ClpB和IbpA/B热休克蛋白。在这些热休克蛋白中,IbpA/B最有效地由甲氧苄啶诱导,并与不溶性蛋白质共聚合。叶酸胁迫下,缺失delta-ibpA/B操纵子导致蛋白质聚集增加,但不影响细胞活力[1]。

[体内研究]

在小鼠腹腔感染中,仅甲氧苄啶对流感嗜血杆菌、肺炎链球菌、大肠杆菌和脑膜炎双球菌的CD50值分别为150 mg/kg、335 mg/kg、27.5 mg/kg和8.4 mg/kg[2]。

[参考文献]

[1]. Ewa Laskowska, et al. Trimethoprim Induces Heat Shock Proteins and Protein Aggregation in E. Coli Cells. Curr Microbiol. 2003 Oct;47(4):286-9.

[2]. R N Brogden, et al. Trimethoprim: A Review of Its Antibacterial Activity, Pharmacokinetics and Therapeutic Use in Urinary Tract Infections. Drugs. 1982 Jun;23(6):405-30.

[3]. Xiaojian Wang, et al. A Trimethoprim Conjugate of Thiomaltose Has Enhanced Antibacterial Efficacy In Vivo. Bioconjug Chem. 2018 May 16;29(5):1729-1735.

乳酸甲氧苄啶物理化学性质

[ 沸点 ]:
526ºC at 760mmHg

[ 分子式 ]:
C₁₇H₂₄N₄O₆

[ 分子量 ]:
380.396

[ 闪点 ]:
271.9ºC

[ 精确质量 ]:
380.169586

[ PSA ]:
163.04000

[ LogP ]:
1.87180

[ 外观性状 ]:
白色至淡黄色粉末

[ 蒸汽压 ]:
3.74E-11mmHg at 25°C

[ 储存条件 ]:
2-8°C

乳酸甲氧苄啶MSDS

详细MSDS(安全技术说明书)

乳酸甲氧苄啶安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
T:Toxic;

[ 风险声明 (欧洲) ]:
R23/24/25;R43;R61

[ 安全声明 (欧洲) ]:
S22-S36/37/39-S45-S53

[ 危险品运输编码 ]:
UN 2811

[ WGK德国 ]:
3

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2942000000

乳酸甲氧苄啶海关

[ 海关编码 ]: 2942000000

乳酸甲氧苄啶文献

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DrugBank 3.0: a comprehensive resource for 'omics' research on drugs.

Nucleic Acids Res. 39 , D1035-41., (2011)

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Arcobacter population dynamics in pigs on farrow-to-finish farms.

Appl. Environ. Microbiol. 77 , 1732-8, (2011)

Healthy pigs are an important reservoir for the emerging human pathogen Arcobacter which can result in contamination of porcine carcasses and pork and the spread of arcobacters into the environment. U...

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