MM 54 |
カタログ番号GC50310 |
MM 54 (化合物 5) は APJ での競合的アンタゴニストであり、IC50 は 93 nM です。 MM 54 は、アペリン結合および APLNR 活性化の強力かつ選択的な阻害剤として機能します。
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Cas No.: 1313027-43-8
Sample solution is provided at 25 µL, 10mM.
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.
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
Average Rating: 5
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