MM 54

MM 54;

MM 54 (compound 5) 是竞争性的 APJ 拮抗剂,其 IC50 值为 93 nM。MM 54作为一种有效的和选择性的 apelin 结合和 APLNR 激活的抑制剂。

MM 54amp;;

MM 54 Chemical Structure

CAS No. : 1313027-43-8

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生物活性

MM 54 (compound 5) is a competitive antagonist at APJ, with an IC50 of 93 nM. MM 54 behaves as a potent and selective inhibitor of apelin binding and APLNR activation[1][2].

体外研究
(In Vitro)

MM 54 inhibits more than 95% of apelin binding to APLNR at the dose of 10 µM[2].

MCE 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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Tumour-bearing nude-mice[2].
Dosage: 2 mg/kg.
Administration: Intraperitoneal injection, bi-weekly for 4 weeks.
Result: Reduced tumor progression (glioblastoma).

分子量

1737.17

Formula

C70H121N29O15S4

CAS 号

1313027-43-8

Sequence Shortening

CRPRLCKHCRPRLC (Disulfide bridge:Cys1-Cys6; Cys9-Cys14)

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.

参考文献
  • [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.