ACY-1083 是一种可渗透脑的选择性 HDAC6 抑制剂，IC₅₀ 为 3 nM，ACY-1083 对 HDAC6 的选择性比其他类别的 HDAC 亚型高 260 倍。ACY-1083 可有效逆转化疗引起的周围神经病变。

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.

Oil

HDAC6 3 nM (IC50)

Treatment with ACY-1083 (30 and 300 nM) significantly improves cell viability in a dose-dependent manner. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Viability Assay

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[1]. Krukowski K, et al. HDAC6 inhibition effectively reverses chemotherapy-induced peripheral neuropathy. Pain. 2017 Jun;158(6):1126-1137.
[2]. Vahagn C Nikolian, et al. Isoform 6-selective histone deacetylase inhibition reduces lesion size and brain swelling following traumatic brain injury and hemorrhagic shock. J Trauma Acute Care Surg. 2019 Feb;86(2):232-239.

In Vitro: DMSO : 200 mg/mL (574.14 mM; Need ultrasonic)配制储备液