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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- CAS No.: 2007971-51-7
- 화학식: C23H29N5O4
- 분자량:439.52
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
IC50 & Target
[1]|
PDE5 60 nM (IC50) |
HDAC6 91 nM (IC50) |
HDAC1 310 nM (IC50) |
HDAC3 322 nM (IC50) |
HDAC2 490 nM (IC50) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2007971-51-7
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분자량 439.52
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화학식 C23H29N5O4
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SMILES
O=C1N=C(NC=2C(=NN(C12)C)CCC)C=3C=C(C=CC3OCC)CC4CC(C(=O)NO)C4
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)