Name: CM-414
Rating: 5 (10 reviews)

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HIT ID:HIT214318353
Cas No:1624792-70-6
常用名:CM-414
别名:CM414, CM 414
IUPAC:(1s,3s)-3-[(4-ethoxy-3-{1-methyl-7-oxo-3-propyl-1H,4H,7H-pyrazolo[4,3-d]pyrimidin-5-yl}phenyl)methyl]-N-hydroxycyclobutane-1-carboxamide
IUPAC:(1s,3s)-3-[(4-ethoxy-3-{1-methyl-7-oxo-3-propyl-1H,4H,7H-pyrazolo[4,3-d]pyrimidin-5-yl}phenyl)methyl]-N-hydroxycyclobutane-1-carboxamide
InChI key:GTSZATFSVLYIRU-GASCZTMLSA-N

分子式:C23H29N5O4
分子量:439.516
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:CCCc1nn(C)c2c1[nH]c(nc2=O)-c1cc(C[C@H]2C[C@H](C2)C(=O)NO)ccc1OCC |wU:18.19,20.24,(-2.73,-5.8,;-2.25,-4.33,;-.74,-4.01,;-.27,-2.55,;-1.17,-1.3,;-.27,-.06,;-.74,1.41,;1.2,-.53,;1.2,-2.07,;2.53,-2.84,;3.86,-2.07,;3.86,-.53,;2.53,.24,;2.53,1.78,;5.2,-2.84,;5.2,-4.38,;6.53,-5.15,;6.53,-6.69,;5.2,-7.46,;4.8,-8.95,;3.31,-8.55,;3.71,-7.06,;1.98,-9.32,;.64,-8.55,;1.98,-10.86,;3.31,-11.63,;7.87,-4.38,;7.87,-2.84,;6.53,-2.07,;6.53,-.53,;5.2,.24,;5.2,1.78,)|
SMILES:CCCc1nn(C)c2c1[nH]c(nc2=O)-c1cc(C[C@H]2C[C@H](C2)C(=O)NO)ccc1OCC |wU:18.19,20.24,(-2.73,-5.8,;-2.25,-4.33,;-.74,-4.01,;-.27,-2.55,;-1.17,-1.3,;-.27,-.06,;-.74,1.41,;1.2,-.53,;1.2,-2.07,;2.53,-2.84,;3.86,-2.07,;3.86,-.53,;2.53,.24,;2.53,1.78,;5.2,-2.84,;5.2,-4.38,;6.53,-5.15,;6.53,-6.69,;5.2,-7.46,;4.8,-8.95,;3.31,-8.55,;3.71,-7.06,;1.98,-9.32,;.64,-8.55,;1.98,-10.86,;3.31,-11.63,;7.87,-4.38,;7.87,-2.84,;6.53,-2.07,;6.53,-.53,;5.2,.24,;5.2,1.78,)|

CM-414 is a dual inhibitor of HDACs and PDE5 for the Treatment of Alzheimer’s Disease (IC50 values of 60 nM, 310 nM, 490 nM, 322 nM, and 91 nM against PDE5, HDAC1, HDAC2, HDAC3, and HDAC6, respectively). Chronic treatment of Tg2576 mice with CM-414 diminished brain Aβ and tau phosphorylation (pTau) levels, increased the inactive form of GSK3β, reverted the decrease in dendritic spine density on hippocampal neurons, and reversed their cognitive deficits, at least in part by inducing the expression of genes related to synaptic transmission.

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