A competitive, highly selective beta-1-adrenoceptor antagonist (more than 40-fold selective for beta-1 than beta-2; Ki1 and beta-2, respectively). The most beta-1-selective chemical of the beta-blockers tested so far. Used for treatment of essential hypertension and highly cardioselective. Induces mild vasodialation via a nitric oxide- and cGMP-depedent pathways (EC50 = 11.36uM in renal arteries).
Formula:C22H25F2NO4 • HCl
Solubility:DMSO
Primary Target:→1-adrenoceptor
Primary Target Ki:0.88 and 44 for →1 and →2, respectively
Molar Mass:441.9
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.