FR900359

一种环状缩肽，存在于A.crenata中，是Gαq、Gα11和Gα14的抑制剂（IC50分别为13.18、10.47和10nM）；在1µM的BRET测定中，相对于一组额外的Gα亚基（包括Gαs和Gαi），对这些Gα亚基的选择性高于一组额外的Gα亚基；诱导预收缩的分离小鼠尾动脉松弛，抑制用阿司匹林培养的清洗分离人血小板中U-46619诱导的血小板聚集；诱导细胞周期停滞在G1期，减少B16黑色素瘤细胞的增殖和血清诱导的迁移；以2.5µg/只的剂量抑制由屋尘螨诱发的过敏性哮喘小鼠模型中的气道高反应性。A cyclic depsipeptide that has been found in A. crenata and is an inhibitor of Gαq, Gα11, and Gα14 (IC50s = 13.18, 10.47, and 10 nM, respectively); selective for these Gα subunits over a panel of additional Gα subunits over a panel of additional Gα subunits, including Gαs and Gαi, in BRET assays at 1 µM; induces relaxation of precontracted isolated mouse tail arteries and inhibits U-46619-induced platelet aggregation in washed isolated human platelets cultured with aspirin; induces cell cycle arrest at the G1 phase and reduces proliferation and serum-induced migration of B16 melanoma cells; inhibits airway hyperresponsiveness in a mouse model of house dust mite-induced allergic asthma at 2.5 µg/animal.分子式C49H75N7O15分子量1002.2CCC(N[C@@H]([C@H](O)C(C)C)C(O[C@@H]([C@@]1([H])C(N([C@@](C(O[C@@H]([C@@H](C(O[C@@H](C(N(C(C(N[C@H](C(N([C@H](C(N1)=O)C)C)=O)C)=O)=C)C)=O)CC2=CC=CC=C2)=O)NC(C)=O)C(C)C)=O)([H])[C@@H](C)OC)C)=O)C(C)C)=O)=O