2,5-dimethylcelecoxib

Non Antibodies

KCNQ 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

395, 4

A KCNQ Channel Opener

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

2, 5-dimethylcelecoxib is a KCNQ channel opener in smooth muscle cells1.

Yes

KV7 (KCNQ) channels are voltage-gated potassium channels. These channels are mainly responsible for the cardiac and auditory IKs current and the neuronal M-current but can be found in other tissues as well. Voltage-gated potassium channels are tetramers of α-subunits, which surround a K+-selective pore1. The five different KCNQ subtypes have distinct assembly preferences encoded by a C-terminal cytoplasmic assembly domain, the A-domain tail. This domain is a self-assembling, parallel, four-stranded coiled coil2.2, 5-Dimethylcelecoxib (DMC) is a synthetic opener of KCNQ channels in smooth muscle cells. It is a derivative of Celecoxib without its COX-2 inhibitory function. In asthma and other lung diseases, airways become hyperconstricted because of the secretion of various endogenous substances. DMC causes an increase in KCNQ currents and restores current amplitudes in guinea pig ASMC (air smooth muscle cells). This effect is also seen after the application of bronchoconstrictors such as methacholine and histamine, suggesting that DMC can regulate and dilate airway diameter in bronchoconstricting diseases3. DMC is a potent activator of apoptotic pathways and also suppresses production of prostaglandins in vitro by inhibiting cytokine-triggered upregulation of microsomal PGE-synthase-1. These properties may be valuable in the research of cancer4.