产品描述
Pafuramidine is an orally bioavailable prodrug of furamidine. It has activity against Pneumocystis pneumonia (IC50 value: 4.5 nM)
体外活性
The results of this investigation suggest that DB75 inhibits mitochondrial function. Yeast cells relying upon mitochondrial metabolism for energy production are especially sensitive to DB75 [1].
体内活性
DB289, a novel orally active prodrug of DB75, is undergoing phase IIb clinical trials for early-stage human African trypanosomiasis, Pneumocystis jiroveci carinii pneumonia, and malaria [1]. Clearance of DB289 approximated the liver plasma flow and its large volume of distribution was consistent with extensive tissue binding. Plasma protein binding of DB289 was 97 to 99% in four animal species and humans, but that of DB75 was noticeably less and more species- and concentration-dependent [2]. Despite excellent oral activity against early-stage sleeping sickness, oral administration of DB289 exhibited limited efficacy in mouse models of late-stage disease [3].
Cas No.
186953-56-0
分子式
C20H20N4O3
分子量
364.4
别名
DB289;Pafuramidine
储存和溶解度
DMSO:33.33 mg/mL (91.47 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years