ACY-1083

Product NameACY-1083
CAS1708113-43-2
MFC17H18F2N4O2
MW348.35
EINECS
MOL File1708113-43-2.mol

Chemical Properties

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

Usage And Synthesis

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 (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.

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

ACY-1083 Supplier

ACY-1083 manufacturers

Related Product Information

Send Inquriy