Identification | Back Directory | [Name]
1(2H)-Phthalazinone, 2-cycloheptyl-4a,5,8,8a-tetrahydro-4-[4-methoxy-3-[4-[4-(2H-tetrazol-5-yl)phenoxy]butoxy]phenyl]-, (4aR,8aS)-rel- | [CAS]
469863-16-9 | [Synonyms]
NPD001 NPD-001 NPD 001 1(2H)-Phthalazinone, 2-cycloheptyl-4a,5,8,8a-tetrahydro-4-[4-methoxy-3-[4-[4-(2H-tetrazol-5-yl)phenoxy]butoxy]phenyl]-, (4aR,8aS)-rel- | [Molecular Formula]
C33H40N6O4 | [MOL File]
469863-16-9.mol | [Molecular Weight]
584.71 |
Chemical Properties | Back Directory | [Melting point ]
153-155 °C | [Boiling point ]
768.9±70.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
4.48±0.10(Predicted) | [color ]
White to off-white |
Hazard Information | Back Directory | [Biological Activity]
NPD-001 is a potent Trypanosoma brucei phosphodiesterases TbrPDEB1 and TbrPDEB2 inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits human PDEs (phosphodiesterases). NPD-001 shows good anti trypanosomal activity, with an IC50 of 80 nM[1]. | [References]
[1]. Veerman J, et al. 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. |
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