NS-638

SKU: orb1304083

Description

NS-638 is a calcium channel blocker that inhibits potassium-stimulated intracellular calcium elevation with an IC50 of 3.4 µM. This small molecule is a useful research tool for studying calcium signaling pathways in cardiovascular and neurological research, applicable in both in vitro and in vivo experimental models.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 150493-34-8
• MW: 325.72
• Purity: 99.00% (May vary between batches)
• Formula: C₁₅H₁₁ClF₃N₃
• SMILES: Nc1nc2cc(ccc2n1Cc1ccc(Cl)cc1)C(F)(F)F
• Target: Calcium Channel
• Solubility: DMSO:55 mg/mL (168.86 mM)

Bioactivity

• Target IC50:
  Ca2+ channel:3.4 μM
• In Vivo:
  In the mouse model of middle cerebral artery occlusion, NS-638 administration (50 mg/kg, i.p.) at 1 hour and 6 hours after ischemia, followed by daily dosing for two subsequent days, leads to a 48% decrease in overall infarct volume. However, it fails to demonstrate neuroprotective effects in the gerbil model of bilateral carotid artery occlusion against ischemic neuronal damage.
• 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 (IC50: 2.3 and 4.3 μM), respectively. K+-stimulated intracellular Ca2+-elevation in cultured cerebellar granule cells is equipotently blocked (IC50: 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 (1-30 μM).
• Cell Research:
  NS-638 is prepared in 1% DMSO and 1% ethanol. The effect of NS-638 on neuronal Ca2+-channels is evaluated using whole cell patch clamp techniques.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Ca channels, Ca2+ channels, Calcium Channel, CalciumChannel, NS638, NS-638, NS 638, Inhibitor, K+-stimulated intracellular Ca2+-elevation, inhibit

Compound Identifiers

PubChem CID

127722