MM 54

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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 54

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].

Shanghai Jinpan Biotech Co Ltd 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].

Shanghai Jinpan Biotech Co Ltd 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.

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