Biological Activity
Potent apelin receptor antagonist (Ki = 82 nM; IC50 = 93 nM). Antagonizes the inhibitory affect of [Pyr1]-Apelin-13 on forskolin-induced cAMP accumulation in CHO-K1-APJ cells.
Technical Data
| M. Wt | 1737.15 |
| Formula | C70H121N29O15S4 |
| Sequence |
CRPRLCKHCRPRLC (Modifications: Disulfide bridge: 1-6,9-14) |
| Storage | Store at -20°C |
| CAS Number | 1313027-43-8 |
| PubChem ID | 122705991 |
| InChI Key | BMJYNYGARUVBJU-CSRTWURCSA-N |
| Smiles | [H]N[C@H]1CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(N)=N)NC1=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC1=CNC=N1)C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(N)=N)NC1=O)C(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solubility | Soluble to 2 mg/ml in water |
Preparing Stock Solutions
The following data is based on the product molecular weight 1737.15. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 0.58 mL | 2.88 mL | 5.76 mL |
| 5 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 10 mM | 0.06 mL | 0.29 mL | 0.58 mL |
| 50 mM | 0.01 mL | 0.06 mL | 0.12 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Macaluso et al (2011) Discovery of a competitive apelin receptor (APJ) antagonist. ChemMedChem 6 1017 PMID: 21560248
Keywords: MM 54, supplier, MM54, potent, apelin, receptors, antagonists, antagonism, Apelin, Receptors, Apelin, Receptors, Tocris Bioscience
