Biological ActivityMM 54 is a potent apelin receptor antagonist (Ki = 82 nM; IC50 = 93 nM). Antagonizes the inhibitory affect of [Pyr1]-Apelin-13 on forskolin-induced cAMP accumulation in CHO-K1-APJ cells. Recuces tumor expansion and lengthens survival time in a mouse xenograft model of glioblastoma.
(Modifications: Disulfide bridges: 1-6, 9-14)
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Discovery of a competitive apelin receptor (APJ) antagonist.
Macaluso et al.
Pharmacological targeting of apelin impairs glioblastoma growth.
Harford-Wright et al.
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