MM 54 (compound 5) 是 APJ 的竞争性拮抗剂，IC50 为 93 nM。 MM 54 作为 apelin 结合和 APLNR 激活的有效和选择性抑制剂。
货号:ajcx27322
CAS:1313027-43-8
分子式:C70H121N29O15S4
分子量：1737.15
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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