FPL 64176 是一种非二氢吡啶类L型钙通道激动剂,EC50值为 16 nM。
产品描述
FPL 64176 is a L-type calcium channels activator.
体外活性
FPL-64176, on schistosomes cultured ex vivo and in an in vivo murine model of infection.?Unlike DHPs, FPL-64176 evokes rapid and sustained contractile paralysis of adult Schistosoma mansoni reminiscent of the anthelmintic praziquantel.?This is accompanied by tegument disruption and an arrest of mitotic activity in somatic stem cells and germ line tissues.?Interestingly, this strong ex vivo phenotype was temperature dependent, with FPL-64176 treatment being less potent at 37 C than 23 C. However, FPL-64176 caused intra-tegument lesions at the basement membrane of worms cultured ex vivo under both conditions,?as well as an in vivo hepatic shift of parasites from the mesenteric vasculature of infected mice to the liver[1].
体内活性
Gene expression profiling of worms harvested following in vivo FPL-64176 exposure reveals differences in transcripts associated with muscle and extracellular matrix function, as well as female reproduction, which is consistent with the worm phenotypes observed following ex vivo drug treatment[1].
Cas No.
120934-96-5
分子式
C22H21NO3
分子量
347.41
别名
FPL 64176;FPL64176
储存和溶解度
DMSO:55 mg/ml (158.31 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years