Identification | Back Directory | [Name]
MM 54 | [CAS]
1313027-43-8 | [Synonyms]
MM 54 Cys9-Cys14) H-Cys-Arg-Pro-Arg-Leu-Cys-Lys-His-Cys-Arg-Pro-Arg-Leu-Cys-OH(Disulfide bridge:Cys1-Cys6 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) | [Molecular Formula]
C70H121N29O15S4 | [MOL File]
1313027-43-8.mol | [Molecular Weight]
1737.17 |
Chemical Properties | Back Directory | [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) |
Hazard Information | Back Directory | [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 |
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Company Name: |
BOC Sciences
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Tel: |
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Website: |
https://www.bocsci.com |
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