| Name | 1-[(4-chlorophenyl)methyl]-5-(trifluoromethyl)benzimidazol-2-amine |
|---|---|
| Synonyms |
ns 638
NS638 NS-638 |
| Description | NS-638 is a small nonpeptide molecule with Ca2+-channel blocking properties. K+-stimulated intracellular Ca2+-elevation is blocked with an IC50 value of 3.4 μM. |
|---|---|
| Related Catalog | |
| Target |
IC50: 3.4 μM (K+-stimulated intracellular Ca2+-elevation) [1] |
| In Vitro | NS-638 dose dependently inhibits K+-stimulated [45 Ca2+]-uptake in chick cortical synaptosomes and 2-amino-3-(3-hydroxy-5-methylisoxazol-4-yl)propionic acid (AMPA)- stimulated [3H]GABA-release from cultured cortical neurons with IC50 values of 2.3 and 4.3 μM, respectively. K+-stimulated intracellular Ca2+-elevation in cultured cerebellar granule cells is equipotently blocked with an IC50 value of 3.4 μM. At this concentration no effect on Ca2+-induced contractions in K+-depolarized guinea pig taenia coli is observed. NS-638 reversibly blocks N- and L-type Ca2+-channels in cultured chick dorsal root ganglion cells in the concentration range of 1-30 μM[1]. |
| In Vivo | In the mouse middle cerebral artery occlusion model, NS-638 administered i.p. (50 mg kg-1) at 1 h and 6 h post-ischemia, and once a day for the next two days, results in a 48% reduction in total infarct volume. It does not show protection against ischemic neuronal damage in the gerbil model of bilateral carotid artery occlusion[1]. |
| Cell Assay | The effect of NS-638 on neuronal Ca2+-channels is evaluated using whole cell patch clamp techniques[1]. |
| Animal Admin | Mice: In the mouse middle cerebral artery occlusion model, NS-638 is administered i.p. (50 mg kg-1) at 1 h and 6 h post-ischemia, and once a day for the next two days[1]. |
| References |
| Density | 1.45g/cm3 |
|---|---|
| Boiling Point | 476.3ºC at 760mmHg |
| Molecular Formula | C15H11ClF3N3 |
| Molecular Weight | 325.71600 |
| Flash Point | 241.8ºC |
| Exact Mass | 325.05900 |
| PSA | 44.57000 |
| LogP | 4.26910 |
| Appearance | white solid |
| Vapour Pressure | 3.09E-09mmHg at 25°C |
| Index of Refraction | 1.609 |
| Storage condition | -20℃ |