| Bioactivity | WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor (IC50P. falciparum and P. falciparum strains (including Pyrimethamine (HY-18062)-resistant P. falciparum strains) as well as T. gondii[1][2][3]. | ||||||
| Target | IC50: <0.075 nM (DHFR). | ||||||
| Invitro | WR99210 (0-100 nM; 92 h) is highly effective against T. gondii tachyzoites in tissue culture[1].WR99210 (0-100 nM; 92 h) shows low cytotoxicity to human foreskin fibroblasts[1]. Cell Viability Assay[1] Cell Line: | ||||||
| In Vivo | WR99210 (1.25 mg/kg; i.p.; single daily for 5 days) is highly effective against T. gondii tachyzoites in a mouse model[1]. Animal Model: | ||||||
| Name | WR99210 | ||||||
| CAS | 47326-86-3 | ||||||
| Formula | C14H18Cl3N5O2 | ||||||
| Molar Mass | 394.68 | ||||||
| Appearance | Solid | ||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||
| Storage |
*该产品在溶液状态不稳定，建议您现用现配，即刻使用。 |
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| Reference | [1]. Mui EJ, et al. Triazine Inhibits Toxoplasma gondii tachyzoites in vitro and in vivo. Antimicrob Agents Chemother. 2005 Aug;49(8):3463-7. [2]. Hastings MD, et al. Pyrimethamine and WR99210 exert opposing selection on dihydrofolatereductase from Plasmodium vivax. Proc Natl Acad Sci U S A. 2002 Oct 1;99(20):13137-41. [3]. Kiara SM, et al. In vitro activity of antifolate and polymorphism in dihydrofolate reductase of Plasmodium falciparum isolates from the Kenyan coast: emergence of parasites with Ile-164-Leu mutation. Antimicrob Agents Chemother. 2009 Sep;53(9):3793-8. |