ACY-1083

ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC 50 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 In Vitro Treatment with ACY-1083 (30 and 300 nM) significantly improves cell viability in a dose-dependent manner. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: Mouse hippocampal (HT22) cells Concentration: 30 and 300 nM Incubation Time: Result: Significant improvement in cell viability. In Vivo 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 (C max ) of 936 ng/mL, a half-life (T 1/2 ) of 3.5 hours, and a biologically active plasma exposure of 8 hours after dosing. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Oil IC50& Target:HDAC6 3 nM (IC 50 )

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