Every lot is tried & tested in a relevant biological assay.
- Crestey, F. et al. (2015) ACS. Chem. Neurosci. 6, 1302.
- Alomone Labs NaV1.1-Compound 3a modulates the current of human NaV1.1 channels stably expressed in HEK/293 cells.A. Superimposed traces of NaV1.1 current upon application of control solution (black), and of 10 µM (grey) and 30 µM (green) NaV1.1-Compound 3a (#CMN-002). Current was elicited by a 50 ms voltage step from the holding potential of -120 mV to 0 mV, delivered every 3 sec. B. Normalized values of the decay time constant τ (diamonds) and peak amplitude (circles) of NaV1.1 current, plotted against rising concentrations of NaV1.1-Compound 3a, demonstrate concentration dependent modulation of the two parameters. At 30 µM NaV1.1-Compound 3a decreases current amplitude, yet significantly increases the decay time constant τ (reduces the rate of inactivation).
NaV1.1-Compound 3a is a modulator of the NaV1.1 channel. This compound increases the activity of NaV1.1 channels although its overall impact remains moderate. It has the ability to increase neuronal excitability in fast-spiking hippocampal interneurons1.
Mutations of NaV channels are associated with a range of complex pathological conditions such as epilepsy, myotonic conditions and cardiac arrhythmias1,2. Loss-of-function mutations in mouse models has shown several phenotypes such as autistic-like behaviors, cognitive deficits, severe epilepsy, and unexpected death1.
NaV1.1-Compound 3a (#CMN-002) is a highly pure, synthetic, and biologically active compound.