Introduction：Basic information about CAS 68902-57-8|Metioprim, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Metioprim |
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| CAS Number | 68902-57-8 | Molecular Weight | 306.38300 |
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| Density | 1.31g/cm3 | Boiling Point | 563.3ºC at 760 mmHg |
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| Molecular Formula | C14H18N4O2S | Melting Point | / |
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| MSDS | / | Flash Point | 294.5ºC |
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Names
| Name | 5-[(3,5-dimethoxy-4-methylsulfanylphenyl)methyl]pyrimidine-2,4-diamine |
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| Synonym | More Synonyms |
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Metioprim BiologicalActivity
| 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]. |
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| Related Catalog | Research Areas >>InfectionSignaling Pathways >>Anti-infection >>Bacterial |
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| 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]。 |
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| 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 |
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| References | [1]. Wüst J, et al. Activity of brodimoprim and metioprim alone and in combination with sulfonamides against anaerobic bacteria. Antimicrob Agents Chemother. 1983 Mar;23(3):490-2. [2]. Seydel JK, et al. Bacterial growth kinetics of Escherichia coli and mycobacteria in the presence of brodimoprim and metioprim alone and in combination with sulfamerazine and dapsone (VI). Chemotherapy. 1983;29(4):249-61. [3]. Nielsen P, et al. Pharmacokinetics and metabolism of metioprim in pigs and goats. Pharmacol Toxicol. 1987 Nov;61(5):330-4. |
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Chemical & Physical Properties
| Density | 1.31g/cm3 |
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| Boiling Point | 563.3ºC at 760 mmHg |
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| Molecular Formula | C14H18N4O2S |
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| Molecular Weight | 306.38300 |
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| Flash Point | 294.5ºC |
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| Exact Mass | 306.11500 |
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| PSA | 123.04000 |
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| LogP | 1.83110 |
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| Index of Refraction | 1.642 |
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| InChIKey | HRZQMMXCASMDBP-UHFFFAOYSA-N |
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| SMILES | COc1cc(Cc2cnc(N)nc2N)cc(OC)c1SC |
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Synonyms
| Metioprim |
| He 909 |
| Ro 12-6995 |
