TGN-020 sodium is a selective Aquaporin 4 (AQP4) inhibitor with an IC50 of 3.1 μM[1][2]. TGN-020 sodium is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[3]. TGN-020 sodium alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats[4].
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[3].
TGN-020 sodium (0.02 mg/μL; two microliter intravitreal injections) can suppress retinal edema in STZ-induced diabetic rats (nine-week-old male Wistar rats) retinas[2].
TGN-020 sodium (100?mg/kg; ip; single dose immediately followed SCI) promotes functional recovery at days 3, 7, 14, 21, and 28, as well as reduces the degree of edema and inhibits the expression of AQP4, GFAP, PCNA at days 3 after SCI[4].
TGN-020 sodium inhibits the glial scar formation and upregulates GAP-43 expression in adult female Sprague-Dawley rats (180-220?g, 9-10?weeks old) with SCI[4].
[1]. Vincent J Huber, et al. Identification of aquaporin 4 inhibitors using in vitro and in silico methods. Bioorg Med Chem. 2009 Jan 1;17(1):411-7.
[2]. Shou Oosuka, et al. Effects of an Aquaporin 4 Inhibitor, TGN-020, on Murine Diabetic Retina. Int J Mol Sci. 2020 Mar 27;21(7):2324.
[3]. An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562.
[4]. Jian Li, et al. TGN-020 alleviates edema and inhibits astrocyte activation and glial scar formation after spinal cord compression injury in rats. Life Sci. 2019 Apr 1;222:148-157.