PD 173212

Non Antibodies

N-type Ca2+ channels

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

599, 9

A Novel Blocker of N-type CaV Channels

Centrifuge the vial before adding solvent (10, 000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity

41116134

PD 173212 is a dipeptidyl-amine that acts as an N-type voltage-gated Ca2+ channel blocker1. PD 173212 inhibited N-type channels in IMR-32 cells with IC50 = 36 nM as measured by Ca2+ imaging of K+ stimulated cells and only had small effects on other channels at much higher concentrations1.

Yes

Native voltage-gated Ca2+ channels (VGCC, CaV) are pharmacologically classified into at least five different subclasses (L-, N-, P-, Q-, and R-type), the characteristics of which are determined by the pore-forming α1 subunit. The subunit CaV2.2 (α1B) forms N-type Ca2+ channels, which are located primarily on presynaptic nerve terminals of central and peripheral neurons1.PD 173212 is a dipeptidyl-amine that acts as a N-type CaV channels blocker. It is the most active small molecule for N-type calcium channel blockade as it inhibits this channel with an IC50 of 36 nM in IMR-32 cells, as measured by using fluorescent technique2. PD 173212 blocks also other CaV channels but to a lesser extent and only at higher concentrations2. In vivo, it prevents tonic seizures in the audiogenic seizure model.