ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy.
IC50&Target
HDAC6
3 nM (IC50)
体外研究
Treatment with ACY-1083 (30 and 300 nM) significantly improves cell viability in a dose-dependent manner.
Cell Viability Assay
Cell Line:
Mouse hippocampal (HT22) cells
Concentration:
30 and 300 nM
Incubation Time:
Result:
Significant improvement in cell viability.
体内研究
ACY-1083 (i.p.; 10 mg/kg; for 7 days) effectively relieves Cisplatin-induced mechanical allodynia in C57BL/6J mice
ACY-1083 (oral doses of 3 mg/kg ACY-1083 for 7 days) reverses Paclitaxel-induced mechanical allodynia in adult male SD rats.
Mice dosed with 5 mg/kg ACY-1083 by intraperitoneal (i.p.) injection have a maximum plasma concentration (Cmax) of 936 ng/mL, a half-life (T1/2) of 3.5 hours, and a biologically active plasma exposure of 8 hours after dosing.
Animal Model:
Adult male C57BL/6J mice of 8-10 weeks of age
Dosage:
3 or 10 mg/kg
Administration:
Administered i.p. injection; daily; for 7 days
Result:
The 10 mg/kg relieved Cisplatin (2.3 mg/kg)-induced mechanical allodynia, whereas the 3 mg/kg dose did not.
Animal Model:
Adult male Sprague Dawley rats
Dosage:
3 mg/kg
Administration:
Two daily doses were given orally for 7 days.
Result:
Reversed Paclitaxel (6 mg/kg or 12 mg/kg)-induced mechanical allodynia.
分子式
C17H18F2N4O2
分子量
348.35
CAS号
1708113-43-2
运输条件
Room temperature in continental US; may vary elsewhere.