NAADP receptor modulator-1

NAADP receptor modulator-1 is a cell-permeable NAADP receptor modulator. NAADP receptor modulator-1 competes with NAADP for binding sites and inhibits NAADP-induced Ca²⁺ release^[1]. In Vitro:NAADP receptor modulator-1 (Compound 3) (0-30 μM) potently and selectively inhibits NAADP-induced Ca²⁺ release in egg homogenates of Lytechinus pictus sea urchins, with an IC₅₀ of 15 μM; it acts as a partial agonist at concentrations >100 μM^[1].
NAADP receptor modulator-1 shows weak competitive activity against [³²P]NAADP binding in Lytechinus pictus egg homogenates, with an IC₅₀ of 90 μM^[1].
NAADP receptor modulator-1 (10 mM) can cross the cell membrane of intact Lytechinus pictus sea urchin egg cells, and completely inhibits NAADP-induced Ca²⁺ release when administered extracellularly^[1].
When applied extracellularly, NAADP receptor modulator-1 (1 mM) potently attenuates CCK-induced Ca²⁺ oscillations in mouse pancreatic acinar cells, while exerting minimal effects on acetylcholine-induced Ca²⁺ responses^[1].
NAADP receptor modulator-1 (10 mM; extracellular incubation) completely abolishes NAADP-induced Ca²⁺ transients in intact sea urchin eggs^[1].