tcsc1361 NP118809

NP118809 is a potent N-type calcium channel blocker, with an IC₅₀ of 0.11 μM; also less potently inhibits L-type calcium channel with an IC₅₀ of 12.2 μM.

IC50 & Target: IC50: 0.11 μM (N-type calcium channel), 12.2 μM (L-type calcium channel)^[1][2]

In Vitro: NP118809 is a potent N-type calcium channel blocker, with an IC₅₀ of 0.11 μM; also inhibits L-type calcium channel with an IC₅₀ of 12.2 μM. NP118809 inhibits the hERG potassium channel in HEK cells, with an IC₅₀ of 7.4 μM^[1].

In Vivo: NP118809 (25 mg/kg, i.p.) shows significant analgesic activity in the phase IIA portions of the rat formalin model^[1]. NP118809 (30 mg/kg, p.o.) results in 80.3% inhibition of mechanical allodynia and 96.3% inhibition of thermal hyperalgesia in the rat spinal nerve ligation model^[2].