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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 bridge: 1-6,9-14)
|Storage||Store at -20°C|
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.
|Solubility||Soluble to 2 mg/ml in water|
References are publications that support the biological activity of the product.
Macaluso et al (2011) Discovery of a competitive apelin receptor (APJ) antagonist. ChemMedChem 6 1017 PMID: 21560248
Harford-Wright et al (2017) Pharmacological targeting of apelin impairs glioblastoma growth. Brain 140 2939 PMID: 29053791
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