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RA-2 is a pan-negative-gating modulator of KCa2/3 channels. It acts by inhibiting EDH-type relaxation in coronary arteries.

RA-2 is a negative-gating modulator of KCa2/3 channels with an IC50 of 17 nM. RA-2 inhibits bradykinin-induced endothelium-derived hyperpolarization (EDH)-type relaxation in U46619-precontracted rings. RA-2 can help to define the physiologic and pathomechanistic roles of KCa2/3 in the vasculature, central nervous system, and during inflammation[1].

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[1] Oliván-Viguera A, et al. A novel pan-negative-gating modulator of KCa2/3 channels, fluoro-di-benzoate, RA-2, inhibits endothelium-derived hyperpolarization-type relaxation in coronary artery and produces bradycardia in vivo. Mol Pharmacol. 2015;87(2):338- DOI:10.1124/mol.114.095745