| Identification | Back Directory | [Name]
ACY-1083 | [CAS]
1708113-43-2 | [Synonyms]
ACY-1083
ACY 1083,ACY1083
5-Pyrimidinecarboxamide, 2-[(4,4-difluoro-1-phenylcyclohexyl)amino]-N-hydroxy- | [Molecular Formula]
C17H18F2N4O2 | [MDL Number]
MFCD32062694 | [MOL File]
1708113-43-2.mol | [Molecular Weight]
348.35 |
| Chemical Properties | Back Directory | [density ]
1.38±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 100 mg/mL (287.07 mM) | [form ]
Solid | [pka]
7.74±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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[1]. | [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 (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[1] | | 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[1] | | 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. |
| [IC 50]
HDAC6: 3 nM (IC50) | [References]
[1] Krukowski K, et al. HDAC6 inhibition effectively reverses chemotherapy-induced peripheral neuropathy. Pain. 2017 Jun;158(6):1126-1137. DOI:10.1097/j.pain.0000000000000893
[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. DOI:10.1097/TA.0000000000002119 |
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