Cyclotraxin B

环孢菌素B

S-1203586-72-4 | Cyclotraxin B acetate | (3S,6R,11R,17S,20S,23S,26S,32S,35S)-6-amino-20-(4-aminobutyl)-3-(2-amino-2-oxoethyl)-17-(2-carboxyethyl)-23-[(1R)-1-hydroxyethyl]-26-[(4-hydroxyphenyl)methyl]-32-(2-methylsulfanylethyl)-2,5,13,16,19,22,25,28,31,34-

C288514-10mg

10mg

≥98%

Cyclotraxin B 是一种环肽，是一种高效且选择性的 TrkB 抑制剂，且不会改变 BDNF 的结合。Cyclotraxin B 非竞争性地抑制 BDNF 诱导的 TrkB 活性，IC50 值为 0.30 nM。Cyclotraxin B 可以穿越血脑屏障，并具有止痛和抗焦虑的行为作用。 Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects。

TrkB受体拮抗剂；抑制BDNF诱导的TrkB活性（IC50 = 0.30 nM）。变构改变TrkB受体构象，但不改变BDNF结合。预防BDNF引起的小鼠冷异常性疼痛。还显示在小鼠中表现出推定的抗焦虑特性。

CNPMGYTKEGC(Modifications: Disulfide bridge between 1 - 11)