NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)

NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal);

NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) (compound 40) 是 Ape13 的大环类似物,一种有效的 APJ 激动剂 (Ki=5.7 nM)。NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) 表现出有利的 Gα12 偏向信号传导和延长的体内半衰期。

NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal)amp;;

NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) Chemical Structure

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生物活性

NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) (compound 40), a macrocyclic analogue of Ape13, is a potent APJ agonist (Ki=5.7 nM). NH2-c[X-R-L-S-X]-K-G-P-(D-2Nal) exhibits a favorable Gα12-biased signaling and an increased in vivo half-life[1].

IC50 Target

APJ[1]

分子量

1020.18

Formula

C49H73N13O11

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Tran K, et, al. Size-Reduced Macrocyclic Analogues of [Pyr 1]-apelin-13 Showing Negative Gα 12 Bias Still Produce Prolonged Cardiac Effects. J Med Chem. 2022 Jan 13;65(1):531-551.