Molecular Formula | C32H32N2O |
Molar Mass | 460.61 |
Density | 1.142±0.06 g/cm3(Predicted) |
Boling Point | 618.9±55.0 °C(Predicted) |
pKa | 5.99±0.10(Predicted) |
Storage Condition | Sealed in dry,Room Temperature |
In vitro study | NP118809 is a potent N-type calcium channel blocker, with an IC 50 of 0.11 μM; also inhibits L-type calcium channel with an IC 50 of 12.2 μM. NP118809 inhibits the hERG potassium channel in HEK cells, with an IC 50 of 7.4 μM. |
In vivo study | NP118809 (25 mg/kg, i.p.) shows significant analgesic activity in the phase IIA portions of the rat formalin model. 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. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.171 ml | 10.855 ml | 21.71 ml |
5 mM | 0.434 ml | 2.171 ml | 4.342 ml |
10 mM | 0.217 ml | 1.086 ml | 2.171 ml |
5 mM | 0.043 ml | 0.217 ml | 0.434 ml |
biological activity | NP118809 is an effective n-type calcium channel (N-type calcium channel) blocker with an IC50 value of 0.11 μM; At the same time, it can weakly inhibit l-type calcium channel (L-type calcium channel) with an IC50 value of 12.2 μM. |
target | N-Type Ca 2 + Channel 0.11 μM (IC 50 ) L-type calcium channel 12.2 μM (IC 50 ) |
in vitro study | NP118809 is a potent N-type calcium channel blocker, with an IC 50 of 0.11 μ M; Also inhibits L-type calcium channel with an IC 50 of 12.2 μ M. NP118809 inhibits the hERG potassium channel in HEK cells, with an IC 50 of 7.4 μ m. |
in vivo study | NP118809 (25 mg/kg, I. p.) shows significant analgesic activity in the phase IIA portions of the rat formalin model. 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. |