ACY-1083

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

ACY-1083 是一种选择性、脑穿透性 HDAC6 抑制剂 (IC50: 3 nM)。它对 HDAC6 的选择性比所有其他类别的 HDAC 亚型高 260 倍。

ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor (IC50: 3 nM). It is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy.(In Vitro):ACY-1083 (30 and 300 nM) dose-dependently improves cell viability.(In Vivo):In C57BL/6J mice, ACY-1083 (10 mg/kg; i.p.) effectively relieves Cisplatin-induced mechanical allodynia. In adult male SD rats, ACY-1083 (3 mg/kg; orally) reverses Paclitaxel-induced mechanical allodynia. ACY-1083(5 mg/kg; i.p.) shows a Cmax of 936 ng/mL, a half-life (T1/2) of 3.5h, and a biologically active plasma exposure of 8 hours.

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.

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.

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Cell Cycle/DNA Damage

HDAC

antibacterial

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1708113-43-2

348.354

C17H18F2N4O2

>98% (HPLC)

In Vitro:?DMSO : 200 mg/mL (574.14 mM)

ONC(=O)c1cnc(NC2(CCC(F)(F)CC2)c2ccccc2)nc1

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(-20℃)

With Ice Pack

≥ 2 years