WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor ( IC 50 <0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine (HY-18062)-resist
Température de stockage
Store at -20°C
Expédié en
Ice chest + Ice pads
Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.
Product Description
WR99210 is an orally active and low-toxicity dihydrofolate reductase (DHFR) inhibitor ( IC 50 <0.075 nM). WR99210 shows good antiparasitic activity and is effective against P. falciparum and P. falciparum strains (including Pyrimethamine -resistant P. falciparum strains) as well as T. gondii
In Vitro
WR99210 (0-100 nM; 92 h) is highly effective against T. gondii tachyzoites in tissue culture. WR99210 (0-100 nM; 92 h) shows low cytotoxicity to human foreskin fibroblasts. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Human foreskin fibroblasts ( T. gondii -infected) Concentration: 0-100 nM Incubation Time: 92 h Result: Showed marked inhibition of T. gondii , with an IC 50 value of approximately 50 nM. Cell Cytotoxicity AssayCell Line: Human foreskin fibroblasts Concentration: 0-100 nM Incubation Time: 92 h Result: Lacked of toxicity for fibroblasts.
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male mice ( T. gondii -infected) . Dosage: 1.25 mg/kg Administration: Intraperitoneal injection; single daily for 5 days. Result: Exhibited intraperitoneal parasite numbers were 2 logs less in mice on the day 5.
This compound belongs to the class of organic compounds known as phenol ethers. These are aromatic compounds containing an ether group substituted with a benzene ring.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
