68902-57-8
68902-57-8 structure
- Name: Metioprim
- Chemical Name: 5-[(3,5-dimethoxy-4-methylsulfanylphenyl)methyl]pyrimidine-2,4-diamine
- CAS Number: 68902-57-8
- Molecular Formula: C14H18N4O2S
- Molecular Weight: 306.38300
- Catalog: Signaling Pathways Anti-infection Bacterial
- Create Date: 2018-03-03 08:00:00
- Modify Date: 2025-08-25 19:21:34
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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].
| Name | 5-[(3,5-dimethoxy-4-methylsulfanylphenyl)methyl]pyrimidine-2,4-diamine |
|---|---|
| Synonyms |
Metioprim
He 909 Ro 12-6995 |
| 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 |
| 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 |