NPD-001 is a potent TbrPDEB1 inhibitor. NPD-001 is 10-fold more potent on hPDE4 (hPDE4B1 IC50 = 0.6 nM) than on TbrPDEB1 (IC50 = 4 nM). Trypanosomal phosphodiesterases B1 and B2 (TbrPDEB1 and TbrPDEB2) play an important role in the life cycle of Trypanosoma brucei, the causative parasite of human African trypanosomiasis (HAT), formerly known as African sleeping sickness. Knock down of both enzymes leads to cell cycle arrest and is lethal to the parasite. References: Veerman J, van den Bergh T, Orrling KM, Jansen C, Cos P, Maes L, Chatelain E, Ioset JR, Edink EE, Tenor H, Seebeck T, de Esch I, Leurs R, Sterk GJ. Synthesis and evaluation of analogs of the phenylpyridazinone NPD-001 as potent trypanosomal TbrPDEB1 phosphodiesterase inhibitors and in vitro trypanocidals. Bioorg Med Chem. 2016 Apr 1;24(7):1573-81. doi: 10.1016/j.bmc.2016.02.032. Epub 2016 Feb 26. PubMed PMID: 26935942.

纯度：≥98%

CAS：469863-16-9