MM 54 (compound 5) is a competitive antagonist at APJ, with an IC 50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation.
体外研究(In Vitro)
MM 54 inhibits more than 95% of apelin binding to APLNR at the dose of 10 μM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
MM 54 (2 mg/kg, ip, bi-weekly for 4 weeks) possesses anti-tumor activity in glioblastoma models with no obvious toxicity. has not independently confirmed the accuracy of these methods. They are for reference only.
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.
[1]. N J Maximilian Macaluso, et al. Discovery of a competitive apelin receptor (APJ) antagonist. ChemMedChem. 2011 Jun 6;6(6):1017-23.[2]. Elizabeth Harford-Wright, et al. Pharmacological targeting of apelin impairs glioblastoma growth. Brain. 2017 Nov 1;140(11):2939-2954.