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NP-118809 (39-1B4) is a potent N-type calcium channel blockers (IC50= 0.11 uM) which has good selectivity over L-type calcium channels. NP-118809 exhibites increased N-type channel blockade (IC50=0.11 uM) and is 111-fold more selective for N-type channels (L-type calcium channel IC50=12.2 uM). NP118809 further exhibits a number of favorable preclinical characteristics as they relate to overall pharmacokinetics and minimal off-target activity including the hERG potassium channel.
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Source | Bioorg Med Chem Lett (2010). Figure 3. NP118809 |
| Method | i.p. | |
| Cell Lines | rat | |
| Concentrations | 25 mg/kg | |
| Incubation Time | - | |
| Results | Figure 2 shows that up on intraperitoneal (ip) administration both NP118809 and NP078585 (25 mg/kg) both exhibited significant analgesic activity in the phase IIA portions of the rat formalin model. |
| Molecular Weight | 460.61 |
| Formula | C32H32N2O |
| CAS Number | 41332-24-5 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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