1375466-18-4
1375466-18-4 structure
- Name: ACY-775
- Chemical Name: ACY-775
- CAS Number: 1375466-18-4
- Molecular Formula: C17H19FN4O2
- Molecular Weight: 330.36
- Catalog: Research Areas Cardiovascular Disease
- Create Date: 2018-01-14 21:56:36
- Modify Date: 2024-01-07 08:09:43
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ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6) with an IC50 of 7.5 nM.
| Name | ACY-775 |
|---|---|
| Synonyms |
Benzamide, 4-(dimethylamino)-N-[5-[(2-mercaptoacetyl)amino]pentyl]-
4-(Dimethylamino)-N-{5-[(sulfanylacetyl)amino]pentyl}benzamide |
| Description | ACY-775 is a potent and selective inhibitor of the of histone deacetylase 6 (HDAC6) with an IC50 of 7.5 nM. |
|---|---|
| Related Catalog | |
| Target |
HDAC6:7.5 nM (IC50) HDAC1:2123 nM (IC50) HDAC2:2570 nM (IC50) HDAC3:11223 nM (IC50) |
| In Vitro | In vehicle-treated cells, α-tubulin is mainly presented in the deacetylated form, while histone 3 is clearly acetylated. Upon treatment with ACY-775, a clear enhancement of the acetylation of α-tubulin is visible, while histone acetylation remains unaltered. Acetylation of α-tubulin is visualized by immunofluorescence and the intensity in the neurites of the neurons is quantified and normalized to the length of the fluorescent signal. In vehicle-treated DRG neurons, acetylated α-tubulin is already present. Upon treatment with ACY-775 the signal intensity of acetylated α-tubulin increases significantly. Significant increase in motility of mitochondria and also the total number of mitochondria within the neurites are observed compare with vehicle-treated DRG neurons. A significantly higher number of retrogradely transport mitochondria is observed in DRG neurons treated with ACY-775 compare with vehicle-treated cells[1]. |
| In Vivo | Biodistribution profiles of ACY-738, ACY-775, and tubastatin A are examined after acute dosing at 5 or 50 mg/kg over 2 h. At t=30 min after acute 50 mg/kg injection, respective plasma levels of ACY-738 and ACY-775 are 515 ng/mL (1.9 μM) and 1359 ng/mL (4.1 μM). Elimination from plasma is rapid, with plasmatic half-life of 12 min and concentration below 10 ng/mL after 2 h. Nevertheless, areas under concentration time curves for brain and plasm calculated over 2 h for both ACY-738 and ACY-775 lead to ratios >1. When ACY-738 (5 mg/kg) or ACY-775 (50 mg/kg) are administered repeatedly in wild-type mice at 24 h, 4 h, and 30 min before killing, significant increases in α-tubulin acetylation are observed in all tested brain regions[2]. |
| Cell Assay | Undifferentiated RN46A-B14 cells, a line of immortalized rat raphe neuronal precursors, are grown. They are treated with 2.5 μM ACY-738, ACY-775, tubastatin A, 0.6 μM TSA or vehicle (0.1% DMSO) for 4 h. Samples are processed using histone extraction kit and quantified using protein assay. |
| Animal Admin | Mice are tested for immobility in the TST. At 30 min or 2 h after i.p. injection of ACY-738 (5, 50 mg/kg), ACY-775 (5, 50 mg/kg), and citalopram (0.5, 2, 20 mg/kg), a combination of the previous, or vehicle, mice are attached to the test rig and time immobile over 6 min is recorded. For open-field activity mice are injected with ACY-738 or ACY-775 at 5, 10, or 50 mg/kg or vehicle and allowed to explore. Activity is recorded[2]. |
| References |
| Density | 1.1±0.1 g/cm3 |
|---|---|
| Boiling Point | 589.7±45.0 °C at 760 mmHg |
| Molecular Formula | C17H19FN4O2 |
| Molecular Weight | 330.36 |
| Flash Point | 310.4±28.7 °C |
| LogP | 1.54 |
| Vapour Pressure | 0.0±1.7 mmHg at 25°C |
| Index of Refraction | 1.566 |
| Storage condition | 2-8℃ |