Biological Activity
Highly potent and very selective non-peptide angiotensin AT1 receptor antagonist (IC50 values are 0.7 and > 10000 nM for AT1 and AT2 receptors respectively). Potently inhibits angiotensin II-induced contractions in isolated rabbit aorta (IC50 = 0.2 nM) and reduces blood pressure in hypertensive rats.
Compound Libraries
EMD 66684 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 547.05 |
| Formula | C28H30N8O2.HCl |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1216884-39-7 |
| PubChem ID | 56972165 |
| InChI Key | YMFXGXGDHBXTPY-UHFFFAOYSA-N |
| Smiles | Cl.CCCCC1=NC2=C(N1CC1=CC=C(C=C1)C1=C(C=CC=C1)C1=NN=NN1)C(=O)N(CC(=O)N(C)C)C=C2 |
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
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 27.35 | 50 | |
| ethanol | 27.35 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 547.05. 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 | 1.83 mL | 9.14 mL | 18.28 mL |
| 5 mM | 0.37 mL | 1.83 mL | 3.66 mL |
| 10 mM | 0.18 mL | 0.91 mL | 1.83 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.37 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Mederski et al (1994) Non-peptide angiotensin II receptor antagonists: synthesis and biological activity of a series of novel 4,5-dihydro-4-oxo-3H-imidazo[4,5-c]pyridine derivatives. J.Med.Chem. 37 1632 PMID: 8201597
Mederski et al (1995) 4,5-Dihydro-4-oxo-3H-imidazo[4,5-c]pyridines: potent arylacetic acid-derived AT1 antagonists with improved affinity for the AT2 receptor. Bioorg.Med.Chem.Lett. 5 2665 PMID:
Keywords: EMD 66684, supplier, Potent, selective, non-peptide, AT1, antagonists, Receptors, Angiotensin, EMD66684, Angiotensin, AT1, Receptors, Angiotensin, AT1, Receptors, Tocris Bioscience
