1624792-73-9
1624792-73-9 structure
- Name: trans CM-414
- Chemical Name: trans CM-414
- CAS Number: 1624792-73-9
- Molecular Formula: C23H29N5O4
- Molecular Weight: 439.516
- Create Date: 2020-01-20 14:08:56
- Modify Date: 2024-02-04 23:48:35
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A first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM); does not inhibit class IIa HDAC isoforms, MMP-3, MMP-10, and PDE9 (IC50>10 uM), has modest or weak activity for HDAC8/11/10 (IC50=640/550/2400 nM); diminishes brain Aβ and pTau levels, increases the inactive form of GSK3β, reverts the decrease in dendritic spine density on hippocampal neurons, and reverses the cognitive deficits in Tg2576 mice.
| Name | trans CM-414 |
|---|
| Description | A first-in-class, dual inhibitor of PDE5 and HDAC that inhibits HDAC1/2/3/6 (IC50=310/490/322/91 nM, respectively) and PDE5 (IC50=60 nM); does not inhibit class IIa HDAC isoforms, MMP-3, MMP-10, and PDE9 (IC50>10 uM), has modest or weak activity for HDAC8/11/10 (IC50=640/550/2400 nM); diminishes brain Aβ and pTau levels, increases the inactive form of GSK3β, reverts the decrease in dendritic spine density on hippocampal neurons, and reverses the cognitive deficits in Tg2576 mice. |
|---|---|
| References | References 1. Cuadrado-Tejedor M, et al. Neuropsychopharmacology. 2017 Jan;42(2):524-539. View Related Products by Target HDAC |
| Molecular Formula | C23H29N5O4 |
|---|---|
| Molecular Weight | 439.516 |