Biological Activity
AC1-IN-1 is a potent and selective Adenylyl cyclase type 1 (AC1) inhibitor with an IC50 of 0.54 μM. AC1-IN-1 displays modest antiallodynic effects in a mouse model of inflammatory pain. AC1-IN-1 has CNS activity[1].
AC1-IN-1 (compound 38; HEK293 cells; 30 μM, 1 hours) shows nontoxic to this human cell line[1].
AC1-IN-1 (5.6 mg/kg; i.v.) displays modest, yet statistically significant, antiallodynic effects at 1 h post-treatment compared to the 0 min (allodynic) time point[1].
References
[1]. Scott JA, et al. Optimization of a Pyrimidinone Series for Selective Inhibition of Ca2+/Calmodulin-Stimulated Adenylyl Cyclase 1 Activity for the Treatment of Chronic Pain. J Med Chem. 2022; 65(6):4667-4686.
