NS-638

SKU: orb1226171

Description

A nonpeptide calcium channel blocker that dose dependently inhibits AMPA-stimulated [3H]GABA-release from cultured cortical neurons with IC50 of 4.3 uM; blocks K(+)-stimulated intracellular Ca(2+)-elevation in cultured cerebellar granule cells with IC50 of 3.4 uM, reversibly blocks N- and L-type Ca(2+)-channels in cultured chick dorsal root ganglion cells (1-30 uM); exhibits anti-ischemic properties in vivo.

Key Properties

• CAS Number: 150493-34-8
• MW: 325.7161496
• Purity: >98% (HPLC)
• Formula: C₁₅H₁₁ClF₃N₃
• SMILES: FC(C1=CC=C2C(N=C(N)N2CC3=CC=C(Cl)C=C3)=C1)(F)F
• Target: Calcium Channel
• Solubility: DMSO: ≥ 34 mg/mL

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NS638 | NS 638

Quick Database Links

Gene Symbol

Calcium Channel