Metioprim
Names
Biological Activity
[Description]:
Metioprim is a competitive inhibitor of bacterial Dihydrofolate reductase (DHFR). Metioprim has inhibitory activity against anaerobic bacteria. Metioprim shows synergistic activity in combination with DDS (HY-B0688) against E. coli. and various mycobacteria[1][2].
[Related Catalog]:
[In Vitro]
Metioprim 对部分厌氧菌有抑制作用,平均 MIC 值为 3.2 μg/mL[1]。 Metioprim (0-1.0 μM;0-8 h) 抑制细菌生长动力学,抑制大肠杆菌的 MIC 值为 0.7 μg/mL[2]。
[In Vivo]
Metioprim (5 mg/kg or 10 mg/kg; 静脉注射; 单剂量) 在羊中的消除半衰期比猪的短 (23 min vs 169 min),它的主要代谢产物为蛋氨酸亚砜和甲氧磷磺酸[3]。 药代动力学分析[1] Animal Route Dose (mg/kg) C0 (μg/mL) A (μg/mL) α (1/min) t1/2α (min) B (μg/mL) β (1/min) t1/2β (min) VC (1/kg) Vp (1/kg) Vd,ss (1/kg) Clβ (mL/min/kg) Pigs i.v. 5 3.6 2.1 0.032 25 1.5 0.00415 169 1.45 0.74 2.19 10.0 Goats i.v. 10 12.2 6.4 0.220 4 5.6 0.03138 23 0.85 0.44 1.28 49
[References]
Chemical & Physical Properties
[ Density]:
1.31g/cm3
[ Boiling Point ]:
563.3ºC at 760 mmHg
[ Molecular Formula ]:
C14H18N4O2S
[ Molecular Weight ]:
306.38300
[ Flash Point ]:
294.5ºC
[ Exact Mass ]:
306.11500
[ PSA ]:
123.04000
[ LogP ]:
1.83110
[ Index of Refraction ]:
1.642