TGN-020 选择性水通道蛋白 4 (AQP4) 抑制剂

TGN-020 是一种选择性水通道蛋白 4 (AQP4) 抑制剂，IC₅₀ 为 3.1 μM。TGN-020 是一种 PROTAC linker，属于 alkyl chain 类，可用于合成 PROTAC 分子。TGN-020 减轻大鼠脊髓压迫损伤后的水肿并抑制神经胶质瘢痕的形成。

产品描述：    

TGN-020 is a selective Aquaporin 4 (AQP4) inhibitor with an IC50 of 3.1 μM[1][2]. TGN-020 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs[3].TGN-020 alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats[4].


IC50 & Target     ：Alkyl-Chain


体外实验：

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].

体内实验：

TGN-020 (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 (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. TGN-020 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].

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