Pyrimethamine(RP4753) is a medication used for protozoal infections; interferes with tetrahydrofolic acid synthesis from folic acid by inhibiting the enzyme dihydrofolate reductase (DHFR).IC50 Value: 15.4 nM (Plasmodium falciparum) [1]Target: DHFR; antifolatein vitro: Three susceptibility levels (susceptible, intermediate, and resistant) were observed in the response of culture-adapted clones and strains to pyrimethamine (50% inhibitory concentration [IC50]) < 100, 100-2,000, and > 2,000 nM) and cycloguanil (IC50 < 50, 50-500, and > 500 nM). Based on these 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 [1]. We tested pyrimethamine(previously reported to suppress SOD1 expression), several compounds currently in trials in human and murine ALS, and a set of 1040 FDA-approved compounds. In a PC12 cell-based assay, no compounds reduced SOD1 promoter activity without concomitant cytotoxicity. Additionally,pyrimethamine failed to repress levels of SOD1 protein in HeLa cells or homogenates of liver, spinal cord and brain of wild-type mice [3].in vivo: (131)I-Pyrimethamine (specific activity: 7.08 MBq/ mol) was injected intravenously into the tail vein of the control and infected rats. Static whole body images of the rats were acquired under the gamma camera at 5 min, 45 min, 2 h, 6 h, and 24 h following the intravenous administration of the radioactivity (3.7 MBq/rat) [2]. The 10-day treatment with 10mg/kg/day of fluconazole combined with 40/1mg/kg/day sulfadiazine and pyrimethamine resulted in 93% survival of CF1 mice acutely infected with the highly virulent T. gondii RH strain, versus 36% of mice treated with just sulfadiazine and pyrimethamine [4].Toxicity: Sulfadoxine/pyrimethamine is well tolerated as treatment and when used as intermittent preventive treatment in pregnant African women. Sulfadoxine/pyrimethamine is no longer used as prophylaxis because it may cause toxic epidermal necrolysis and Stevens Johnson syndrome [5].
Welcome to hebei Shuoxi biotechnology co., LTD. Shuoxi is a fast developing pharmaceutical intermediates enterprise located in shijiazhuang, capital of hebei province.
Shuoxi analysis research and development center also provides custom synthesis service.
Hebei Shuoxi biotechnology co., LTD can provide customized synthetic chemicals in different quantities in laboratories, factories and industrial scale.
We have more than 10 years experience in this field.
We can offer competitive price for every customer and guarantee the quality of our products.
3. We pay attention to the needs of each customer and build a good relationship with them.
4. We have long-term business relations with Canada, Mexico, Brazil, UK, Russia, Germany, USA, India, South Africa, Malta, Egypt, Armenia, Australia, Philippines, Belgium, Netherlands, Denmark and other countries.
If you have any other questions for me. Please feel free to contact me.
We only produce and sell products that are legal in China. All products are sold only to laboratory research.