| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Targets the APJ receptor (APLNR, Apelin receptor) as a competitive antagonist. APJ is a class A G protein-coupled receptor (GPCR) that plays a key role in various physiological processes, including cardiovascular function and energy metabolism. Blocking APJ signaling is a strategy for inhibiting tumor growth and angiogenesis.
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| ln Vitro |
At a dosage of 10 µM, MM 54 blocks almost 95% of apelin binding to APLNR[2].
In vitro, at a concentration of 10 uM, MM 54 inhibits more than 95% of apelin binding to APLNR, demonstrating its high potency in blocking the ligand-receptor interaction. This inhibitory activity is characterized by an IC50 of 93 nM, making it a highly effective tool for studying APJ receptor biology in cell-based systems. |
| ln Vivo |
In glioblastoma models, MM 54 (2 mg/kg, ip, biweekly for 4 weeks) exhibits anti-tumor action without evident toxicity[2].
In vivo, MM 54 (2 mg/kg) administered via intraperitoneal (i.p.) injection bi-weekly for four weeks possesses anti-tumor activity in glioblastoma models, significantly inhibiting tumor growth with no obvious toxicity reported. It behaves as a potent and selective inhibitor of apelin binding and APLNR activation, validating its utility for in vivo pharmacology studies. |
| Enzyme Assay |
In vitro radioligand binding assays for APJ are performed using membranes from cells overexpressing the human APJ receptor. The membranes are incubated with a fixed concentration of a radiolabeled apelin peptide (e.g., [¹2⁵I]apelin-13) and varying concentrations of MM 54 for a specific period. Bound radioactivity is separated by filtration through glass fiber filters and counted using a scintillation counter to determine the IC50.
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| Cell Assay |
Functional cell-based assays to assess APJ antagonism typically measure the inhibition of apelin-induced cAMP accumulation or calcium mobilization. HEK293 cells stably expressing human APJ are pre-loaded with a calcium-sensitive fluorescent dye. The cells are pre-incubated with MM 54 before stimulation with a specific APJ agonist. The resulting change in fluorescence is measured using a plate reader to calculate the IC50 of the antagonist.
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| Animal Protocol |
Animal/Disease Models: Tumour-bearing nude-mice[2].
Doses: 2 mg /kg. Route of Administration: intraperitoneal (ip) injection, bi-weekly for 4 weeks. Experimental Results: decreased tumor progression (glioblastoma). In the glioblastoma xenograft model, nude mice bearing subcutaneous tumors are treated with MM 54. The compound is administered at a dose of 2 mg/kg via intraperitoneal injection twice a week for four weeks. During the study, tumor volume is measured regularly with calipers. At the endpoint, tumors are excised and weighed. Body weight and overall health are also monitored to assess compound toxicity. |
| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for MM 54, such as half-life, oral bioavailability, and clearance, are not publicly available. As a synthetic peptide, its in vivo stability is likely limited, which is why it is commonly administered via intraperitoneal injection in animal studies rather than orally. Its molecular weight is 1737.16 g/mol, and it is formulated for injection as a solution.
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| Toxicity/Toxicokinetics |
No specific toxicity data for MM 54 is publicly available. In the reported glioblastoma study, the compound showed "no obvious toxicity" at the administered dose of 2 mg/kg when given bi-weekly for four weeks, as indicated by general health monitoring in the animals. No further toxicological assessments are described in the literature.
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| References | |
| Additional Infomation |
MM 54 is a research-grade chemical tool, not an approved drug. It is a valuable tool for investigating the pathophysiological roles of the apelin/APJ system, particularly in cancer, cardiovascular diseases, and metabolic disorders. The compound is being studied for its potential to inhibit glioblastoma growth and could have broader applications in other APJ-expressing tumor types.
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| Molecular Formula |
C70H121N29O15S4
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|---|---|
| Molecular Weight |
1737.15504622459
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| Exact Mass |
1735.847
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| CAS # |
1313027-43-8
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| PubChem CID |
122705991
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| Sequence |
Cys-Arg-Pro-Arg-Leu-Cys-Lys-His-Cys-Arg-Pro-Arg-Leu-Cys (Disulfide bridge:Cys1-Cys6; Cys9-Cys14)CRPRLCKHCRPRLC (Disulfide bridge:Cys1-Cys6; Cys9-Cys14)
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| SequenceShortening |
CRPRLCKHCRPRLC (Disulfide bridge:Cys1-Cys6; Cys9-Cys14)
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| Appearance |
White to off-white solid powder
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| LogP |
-8.9
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| Hydrogen Bond Donor Count |
23
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| Hydrogen Bond Acceptor Count |
26
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| Rotatable Bond Count |
33
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| Heavy Atom Count |
118
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| Complexity |
3520
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| Defined Atom Stereocenter Count |
14
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| SMILES |
S1C[C@@H](C(N[C@@H](CCC/N=C(\N)/N)C(N2CCC[C@H]2C(N[C@H](C(N[C@H](C(N[C@H](C(=O)O)CS1)=O)CC(C)C)=O)CCC/N=C(\N)/N)=O)=O)=O)NC([C@H](CC1=CN=CN1)NC([C@H](CCCCN)NC([C@@H]1CSSC[C@@H](C(N[C@@H](CCC/N=C(\N)/N)C(N2CCC[C@H]2C(N[C@H](C(N[C@H](C(N1)=O)CC(C)C)=O)CCC/N=C(\N)/N)=O)=O)=O)N)=O)=O)=O
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| InChi Key |
BMJYNYGARUVBJU-CSRTWURCSA-N
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| InChi Code |
InChI=1S/C70H121N29O15S4/c1-36(2)27-45-57(104)95-48(32-116-115-31-39(72)53(100)90-43(16-9-23-84-69(77)78)64(111)98-25-11-18-51(98)62(109)88-41(55(102)92-45)14-7-21-82-67(73)74)60(107)87-40(13-5-6-20-71)54(101)94-47(29-38-30-81-35-86-38)59(106)96-49-33-117-118-34-50(66(113)114)97-58(105)46(28-37(3)4)93-56(103)42(15-8-22-83-68(75)76)89-63(110)52-19-12-26-99(52)65(112)44(91-61(49)108)17-10-24-85-70(79)80/h30,35-37,39-52H,5-29,31-34,71-72H2,1-4H3,(H,81,86)(H,87,107)(H,88,109)(H,89,110)(H,90,100)(H,91,108)(H,92,102)(H,93,103)(H,94,101)(H,95,104)(H,96,106)(H,97,105)(H,113,114)(H4,73,74,82)(H4,75,76,83)(H4,77,78,84)(H4,79,80,85)/t39-,40-,41-,42-,43-,44-,45-,46-,47-,48-,49-,50-,51-,52-/m0/s1
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| Chemical Name |
(3S,6R,11R,14S,17S,20S)-6-[[(2S)-2-[[(2S)-6-amino-2-[[(3S,6R,11R,14S,17S,20S)-6-amino-3,17-bis[3-(diaminomethylideneamino)propyl]-14-(2-methylpropyl)-2,5,13,16,19-pentaoxo-8,9-dithia-1,4,12,15,18-pentazabicyclo[18.3.0]tricosane-11-carbonyl]amino]hexanoyl]amino]-3-(1H-imidazol-5-yl)propanoyl]amino]-3,17-bis[3-(diaminomethylideneamino)propyl]-14-(2-methylpropyl)-2,5,13,16,19-pentaoxo-8,9-dithia-1,4,12,15,18-pentazabicyclo[18.3.0]tricosane-11-carboxylic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ≥ 100 mg/mL (57.56 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (1.44 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (1.44 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (1.44 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5757 mL | 2.8783 mL | 5.7565 mL | |
| 5 mM | 0.1151 mL | 0.5757 mL | 1.1513 mL | |
| 10 mM | 0.0576 mL | 0.2878 mL | 0.5757 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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