产品说明书

Pyrimethamine

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Chemical Structure| 58-14-0 同义名 : 乙胺嘧啶 ;Pirimecidan;Pirimetamin;NSC 3061;Khloridin;Daraprim®;Darapram;RP 4753
CAS号 : 58-14-0
货号 : A195764
分子式 : C12H13ClN4
纯度 : 98% HPLC
分子量 : 248.71
MDL号 : MFCD00057350
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 18 mg/mL(72.37 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
靶点

  • DHFR

    DHFR, IC50:15.4 nM
描述 Pyrimethamine is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR). Based on susceptibility levels, 73 and 68 of 96 fresh clinical isolates were susceptible to pyrimethamine (mean IC50 15.4 nM) and cycloguanil (mean IC50 11.1 nM), respectively. A highly significant positive correlation was found between pyrimethamine and cycloguanil, indicating in vitro cross-resistance between these antifolates[3]. Additionally, pyrimethamine failed to repress levels of SOD1 protein in HeLa cells or homogenates of liver, spinal cord and brain of wild-type mice[4]. The combinations of fluconazole plus sulfadiazine and pyrimethamine or fluconazole plus pyrimethamine were remarkably effective against T. gondii in vivo[5]. Sulfadoxine/pyrimethamine is well tolerated as treatment and when used as intermittent preventive treatment in pregnant African women[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00164710 Malaria, Falciparum Phase 4 Completed - Malawi ... 展开 >> Kawale Health Center Lilongwe, Lilongwe District, Malawi Machinga District Hospital Liwonde, Machinga District, Malawi Matiki Health Center Dwangwa, Nkhotakota District, Malawi 收起 <<
NCT00711906 Malaria in Pregnancy Phase 3 Terminated(Malaria prev. fell ... 展开 >>in the study area, so we cannot evaluate the primary endpoint) 收起 << - Zambia ... 展开 >> Choma hospital Choma, Zambia Shampande Clinic Shampande, Zambia 收起 <<
NCT01084213 Malaria Pregn... 展开 >>ancy Anaemia 收起 << Phase 4 Completed - Burkina Faso ... 展开 >> Université de Ouagadougou Ouagadougou, Burkina Faso Gambia Medical Research Council Laboratories Basse, Gambia Ghana Navrongo Health Research Centre Navrongo, Ghana Mali Medical Research and Training Centre Bamako, Mali 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.02mL

0.80mL

0.40mL

20.10mL

4.02mL

2.01mL

40.21mL

8.04mL

4.02mL
参考文献

[1]Maegawa GH, Tropak M, et al. Pyrimethamine as a potential pharmacological chaperone for late-onset forms of GM2 gangliosidosis. J Biol Chem. 2007 Mar 23;282(12):9150-61.

[2]Akao M, Teshima Y, Marban E. Antiapoptotic effect of nicorandil mediated by mitochondrial atp-sensitive potassium channels in cultured cardiac myocytes. J Am Coll Cardiol. 2002 Aug 21;40(4):803-10.

[3]Basco LK, Ramiliarisoa O, Le Bras J. In vitro activity of pyrimethamine, cycloguanil, and other antimalarial drugs against African isolates and clones of Plasmodium falciparum. Am J Trop Med Hyg. 1994 Feb;50(2):193-9

[4]Wright PD, Huang M, Weiss A, Matthews J, Wightman N, Glicksman M, Brown RH Jr. Screening for inhibitors of the SOD1 gene promoter: pyrimethamine does not reduce SOD1 levels in cell and animal models. Neurosci Lett. 2010 Oct 4;482(3):188-92

[5]Martins-Duarte ÉS, de Souza W, Vommaro RC. Toxoplasma gondii: the effect of fluconazole combined with sulfadiazine and pyrimethamine against acute toxoplasmosis in murine model. Exp Parasitol. 2013 Mar;133(3):294-9

[6]Taylor WR, White NJ. Antimalarial drug toxicity: a review. Drug Saf. 2004;27(1):25-61