2007971-51-7
Chemical Structure
CM-414
- CAS No.: 2007971-51-7
- Formula:C23H29N5O4
- Molecular Weight:439.52
IUPAC Name: 3-(4-ethoxy-3-(1-methyl-7-oxo-3-propyl-4,7-dihydro-1H-pyrazolo[4,3-d]pyrimidin-5-yl)benzyl)-N-hydroxycyclobutane-1-carboxamide
InChIKey: GTSZATFSVLYIRU-UHFFFAOYSA-N
SMILES: O=C1N=C(NC=2C(=NN(C12)C)CCC)C=3C=C(C=CC3OCC)CC4CC(C(=O)NO)C4
Biological Activity: CM-414 is a brain-penetrant phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50s of 60 nM, 91 nM, 310 nM, 322 nM and 490 nM for PDE5, HDAC6, HDAC1, HDAC3 and HDAC2, respectively. CM-414 diminishes brain Aβ and tau phosphorylation (pTau) level in Tg2576 mice. CM-414 can be used for the study of Alzheimer's disease (AD)[1][2].
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CM-414 | CM-414 is a brain-penetrant phosphodiesterase 5 (PDE5) and HDAC inhibitor with IC50s of 60 nM, 91 nM, 310 nM, 322 nM and 490 nM for PDE5, HDAC6, HDAC1, HDAC3 and HDAC2, respectively. CM-414 diminishes brain Aβ and tau phosphorylation (pTau) level in Tg2576 mice. CM-414 can be used for the study of Alzheimer's disease (AD). | |||||||||||||||||||||
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References
- [1]. Obdulia Rabal, et al. Design, Synthesis, and Biological Evaluation of First-in-Class Dual Acting Histone Deacetylases (HDACs) and Phosphodiesterase 5 (PDE5) Inhibitors for the Treatment of Alzheimer's Disease. J Med Chem. 2016 Oct 13;59(19):8967-9004. [Content Brief]
- [2]. Cuadrado-Tejedor M, et al. A First-in-Class Small-Molecule that Acts as a Dual Inhibitor of HDAC and PDE5 and that Rescues Hippocampal Synaptic Impairment in Alzheimer's Disease Mice. Neuropsychopharmacology. 2017 Jan;42(2):524-539. [Content Brief]
