BAY-6096, a potent, selective, and highly water-soluble α2B antagonist with IC50 = 14 nM. Key aspects of the optimization were the introduction of a permanently charged pyridinium moiety to achieve very good aqueous solubility and the inversion of an amide to prevent genotoxicity. BAY-6096 dose-dependently reduced blood pressure increases in rats induced by an α2B agonist, demonstrating the role of α2B receptors in vascular constriction in rats.
MedKoo Cat#: 123014
Name: BAY-6096
CAS#: 2313483-41-7
Chemical Formula: C21H23ClN6O2
Exact Mass: 426.1600
Molecular Weight: 426.91
Elemental Analysis: C, 59.08; H, 5.43; Cl, 8.30; N, 19.69; O, 7.50
The following data is based on the product molecular weight 426.91 Batch specific molecular weights may vary from batch to batch due to the degree 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 | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
