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| Product Name: | MM 54 | | Synonyms: | MM 54;L-Cysteine, L-cysteinyl-L-arginyl-L-prolyl-L-arginyl-L-leucyl-L-cysteinyl-L-lysyl-L-histidyl-L-cysteinyl-L-arginyl-L-prolyl-L-arginyl-L-leucyl-, cyclic (1→6),(9→14)-bis(disulfide);Cys9-Cys14);H-Cys-Arg-Pro-Arg-Leu-Cys-Lys-His-Cys-Arg-Pro-Arg-Leu-Cys-OH(Disulfide bridge：Cys1-Cys6;MM 54 （TFA salt） | | CAS: | 1313027-43-8 | | MF: | C70H121N29O15S4 | | MW: | 1737.17 | | EINECS: | | | Product Categories: | | | Mol File: | 1313027-43-8.mol |  |
| | MM 54 Chemical Properties |
| density | 1.59±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Solid | | pka | 2.95±0.70(Predicted) | | color | White to off-white | | Water Solubility | Soluble to 2 mg/ml in water | | Sequence | Cys-Arg-Pro-Arg-Leu-Cys-Lys-His-Cys-Arg-Pro-Arg-Leu-Cys (Disulfide bridge:Cys1-Cys6; Cys9-Cys14) |
| | MM 54 Usage And Synthesis |
| Uses | 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]. | | 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].
| Animal Model: | Tumour-bearing nude-mice[2]. | | Dosage: | 2 mg/kg. | | Administration: | Intraperitoneal injection, bi-weekly for 4 weeks. | | Result: | Reduced tumor progression (glioblastoma). |
| | storage | Store at -20°C | | References | [1] N J Maximilian Macaluso, et al. Discovery of a competitive apelin receptor (APJ) antagonist. ChemMedChem. 2011 Jun 6;6(6):1017-23. DOI:10.1002/cmdc.201100069
[2] Elizabeth Harford-Wright, et al. Pharmacological targeting of apelin impairs glioblastoma growth. Brain. 2017 Nov 1;140(11):2939-2954. DOI:10.1093/brain/awx253 |
| | MM 54 Preparation Products And Raw materials |
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