R892 is a selective bradykinin B1 receptor antagonist that demonstrates significant antagonistic activity with pA2 values of 8.8 and 8.6 for human and rabbit B1 receptors, respectively. With an ID50 of 2.8 nM for B1 receptors and >600 nM for B2 receptors, R892 exhibits a strong selectivity profile and lacks agonistic properties. Furthermore, R892 is resistant to degradation by aminopeptidase and kininase II (ACE), showcasing its metabolic stability. This compound serves as a valuable tool for research applications investigating bradykinin receptor signaling and related physiological functions.
R892 is a selective bradykinin B1 receptor antagonist that demonstrates significant antagonistic activity with pA2 values of 8.8 and 8.6 for human and rabbit B1 receptors, respectively. With an ID50 of 2.8 nM for B1 receptors and >600 nM for B2 receptors, R892 exhibits a strong selectivity profile and lacks agonistic properties. Furthermore, R892 is resistant to degradation by aminopeptidase and kininase II (ACE), showcasing its metabolic stability. This compound serves as a valuable tool for research applications investigating bradykinin receptor signaling and related physiological functions.
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