产品
编 号:F205550
分子式:C17H18F2N4O2
分子量:348.35
产品类型
结构图
CAS No: 1708113-43-2
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产品详情
生物活性:
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.
体内研究:
ACY-1083 (i.p.; 10 mg/kg; for 7 days) effectively relieves Cisplatin-induced mechanical allodynia in C57BL/6J miceACY-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.
体外研究:
Treatment with ACY-1083 (30 and 300 nM) significantly improves cell viability in a dose-dependent manner.