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Trimethoprim

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Chemical Structure| 738-70-5 同义名 : 甲氧苄氨嘧啶 ;NIH 204;BW 56-72;NSC-106568
CAS号 : 738-70-5
货号 : A327622
分子式 : C14H18N4O3
纯度 : 98%
分子量 : 290.318
MDL号 : MFCD00036761
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(172.23 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Trimethoprim (TMP), an inhibitor of dihydrofolate reductase, decreases the level of tetrahydrofolate supplying one-carbon units for biosynthesis of nucleotides, proteins, and panthotenate. TMP caused induction of DnaK, DnaJ, GroEL, ClpB, and IbpA/B Hsps[3]. Trimethoprim exerts antimicrobial activity by blocking the reduction of dihydrofolate to tetrahydrofolate, the active form of folic acid, by susceptible organisms. It has inhibitory activity for most gram-positive aerobic cocci and some gram-negative aerobic bacilli. Trimethoprim constitutes very effective therapy for women with acute symptomatic urinary tract infections caused by E. coli[4]. The antimicrobial combination of trimethoprim and sulfamethoxazole is active in vitro against a variety of gram-positive and gram-negative bacteria[5]. At the dosages used, trimethoprim has generally been well tolerated and in studies comparing it with co-trimoxazole overall, skin rashes and gastrointestinal upset have occurred less frequently with trimethoprim than with co-trimoxazole[6].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.44mL

0.69mL

0.34mL

17.22mL

3.44mL

1.72mL

34.44mL

6.89mL

3.44mL
参考文献

[1]Vouloumanou EK, Karageorgopoulos DE, et al. Trimethoprim/sulfametrole: evaluation of the available clinical and pharmacokinetic/pharmacodynamic evidence. Int J Antimicrob Agents. 2011 Sep;38(3):197-216.

[2]Cribb AE, Lee BL, et al. Adverse reactions to sulphonamide and sulphonamide-trimethoprim antimicrobials: clinical syndromes and pathogenesis. Adverse Drug React Toxicol Rev. 1996 Mar;15(1):9-50.

[3]Laskowska E, Kuczyńska-Wiśnik D, Bak M, Lipińska B. Trimethoprim induces heat shock proteins and protein aggregation in E. coli cells. Curr Microbiol. 2003 Oct;47(4):286-9

[4]Gleckman R, Blagg N, Joubert DW. Trimethoprim: mechanisms of action, antimicrobial activity, bacterial resistance, pharmacokinetics, adverse reactions, and therapeutic indications. Pharmacotherapy. 1981 Jul-Aug;1(1):14-20

[5]Cockerill FR 3rd, Edson RS. Trimethoprim-sulfamethoxazole. Mayo Clin Proc. 1987 Oct;62(10):921-9

[6]Brogden RN, Carmine AA, Heel RC, Speight TM, Avery GS. Trimethoprim: a review of its antibacterial activity, pharmacokinetics and therapeutic use in urinary tract infections. Drugs. 1982 Jun;23(6):405-30