Molecular Formula | C14H14N4O2 |
Molar Mass | 270.29 |
Density | 1.433±0.06 g/cm3(Predicted) |
Solubility | DMSO: ≥ 32 mg/mL |
pKa | 7.75±0.10(Predicted) |
Storage Condition | -20℃ |
In vivo study | ACY-738 induces a dramatic increase in α-tubulin acetylation in the mouse brain, stimulating the mouse to produce exploratory behavior in a new, unfamiliar environment. ACY-738 has similar antidepressant activity. The elimination of ACY-738 in plasma is rapid with a half-life of 12 minutes. After 2 hours, the concentration is below 10 ng/ml. ACY-738 can be rapidly distributed to the brain, so that the central nervous system drug exposure and other surrounding tissue similar. In NZB/W mice, ACY-738 reduced several features in systemic lupus erythematosus disorders by modulating B cell development in the bone marrow. ACY-738 can increase the percentage of B cells at early stages of development, while decreasing their percentage of cells at late pre-B cell stages. It regulates dysfunctional developmental checkpoints in systemic lupus erythematosus, thereby regulating the development of B cells in bone marrow cells. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.7 ml | 18.499 ml | 36.998 ml |
5 mM | 0.74 ml | 3.7 ml | 7.4 ml |
10 mM | 0.37 ml | 1.85 ml | 3.7 ml |
5 mM | 0.074 ml | 0.37 ml | 0.74 ml |
biological activity | ACY-738 inhibits HDAC6 at low nanomolar concentration, IC50 is 1.7 nM. Its selectivity for HDAC6 is 60-1500 times higher than other class I HDACs. |
target | TargetValue HDAC6 (Cell-free) 1.7 nM |
Target | Value |
HDAC6 (Cell-free) | 1.7 nM |
in vivo study | ACY-738 induce a sharp increase in acetylation of α-tubulin in mouse brain, stimulating mice to produce inquiry behavior in a new and unfamiliar environment. ACY-738 have antidepressant activity similar to that. The elimination rate of ACY-738 in plasma is rapid, with a half-life of 12 minutes. After 2 hours, its concentration was less than 10 ng/ml. ACY-738 can be quickly distributed into the brain, making the drug exposure in the central nervous system similar to other surrounding tissues. In NZB/W mice, ACY-738 reduce several features in systemic lupus erythematosus by regulating the development of B cells in the bone marrow. ACY-738 can increase the percentage of B cells in the early developmental stage and decrease their percentage in the late pre-B cell stage. It regulates dysfunctional developmental checkpoints in systemic lupus erythematosus, thereby regulating the development of B cells in bone marrow cells. |