Spadin (trifluoroacetate salt)

K2P2.1/TREK1抑制剂（在表达K2P2.1/TREK1的COS-7细胞匀浆中Ki=10nM）；对应于人类分拣蛋白的12-28位氨基酸；与C13NJ小胶质细胞中的分拣蛋白结合（Ki=8nM）；抑制表达K2P2.1/TREK1的COS-7细胞中花生四烯酸诱导的电流（IC50=70.7nM）；减少小鼠强迫游泳测试中的静止时间。An inhibitor of K2P2.1/TREK1 (Ki = 10 nM in homogenates from COS-7 cells expressing K2P2.1/TREK1); corresponds to amino acids 12-28 of human sortilin; binds to sortilin in C13NJ microglial cells (Ki = 8 nM); inhibits arachidonic acid-induced currents in COS-7 cells expressing K2P2.1/TREK1 (IC50 = 70.7 nM); decreases immobility time in the forced swim test in mice.分子式C96H142N26O22 • XCF3COOH分子量2012.3O=C(N[C@H](C(N1CCC[C@H]1C(N[C@H](C(N2CCC[C@H]2C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC3=CNC4=C3C=CC=C4)C(N[C@@H](CO)C(NCC(N5CCC[C@H]5C(N[C@@](C(NCC(N[C@@H](C(C)C)C(N[C@@H](CO)C(N[C@@H](CC6=CNC7=C6C=CC=C7)C(NCC(N[C@H](C(N[C@@H](CCCNC(N)=N)C(O)=O)=O)CC(C)C)=O)=O)=O)=O)=O)=O)([H])[C@@H](C)CC)=O)=O)=O)=O)=O)=O)=O)CC(C)C)=O)=O)C)[C@H](CC8=CC=C(O)C=C8)N[H].OC(C(F)(F)F)=O