产品描述:
Atovaquone-d4 is intended for use as an internal standard for the quantification of atovaquone (Item No. 23802) by GC- or LC-MS. Atovaquone is a broad-spectrum antiprotozoal agent that is active against Plasmodium, Toxoplasma, and Babesia, among other protozoa.{39560} It inhibits complex III activity on dihydroorotate in isolated P. falciparum and P. yoelii mitochondria more potently than in rat liver mitochondria (EC50s = 0.95, 0.94, and 510 nM, respectively) and depolarizes the mitochondrial membrane in P. yoelii-infected mouse erythrocytes (EC50 = 260 nM).{39561,39562} Atovaquone also inhibits transport mediated by human breast cancer resistance protein (BCRP) and P-glycoprotein in membrane vesicles (IC50s = 0.23 and 6.8 μM, respectively).{39563} It inhibits the growth of T. gondii in MRC-5 human lung fibroblasts in vitro (IC50 = ~64 nM) and increases mean survival of T. gondii-infected mice from 5.5 to 21.2 days when administered at a dose of 100 mg/kg per day.{39564} Formulations containing atovaquone have been used in the treatment of Pneumocystis pneumonia and toxoplasmosis as well as in combination with proguanil in the treatment of malaria and babesiosis.