NS-4591

Product details

• Chemical name: 4,5-dichloro-1,3-diethyl-1,3-dihydro-benzoimidazol-2-one.
• CAS number: 273930-52-2
• Molecular formula: C11H12Cl2N2O.
• Purity: >98% (HPLC)
• Concentration: 0.01-5 μM.
• Form: Lyophilized powder.
• Solubility: 100 mM DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
• Reconstitution: 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. For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water at a concentration of at least 0.1 mg/mL. 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. It is recommended to prepare fresh solutions in working buffers just before use. For long-term storage of diluted solutions, we recommend adding 0.1% BSA. Repeat freeze-thawing may result in loss of activity.
• Shipping: 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.
• Target: KCa3.1, KCa2 channels
• Source: Synthetic
• Activity: NS-4591 is a potent SK4 channel activator; 30 nM doubled KCa3.1 currents in HEK cells1.

Scientific background

Calcium activated potassium (KCa) channels include three types of small-conductance channels, KCa2.1, KCa2.2 and KCa2.3, and the intermediate conductance channel KCa3.1. Both small- and intermediate-conductance KCa channels play important roles in many processes involving Ca2+-dependent signaling in both electrically excitable and non-excitable cells1.NS-4591 is a potent synthetic activator of KCa3.1 and KCa2 channels. It has an effective concentration of 0.01-5 μM. NS-4591 does not seem to affect KCa1.1 or NaV channels but does cause a small reduction in CaV currents and a prominent reduction in delayed rectifier KV channel. In whole-cell patch-clamp experiments conducted, NS-4591 doubled IK-mediated currents at a concentration of 45±6 nM while 530±100 nM was required for doubling of SK3-mediated currents. The effect of NS-4591 was also examined in acutely dissociated bladder primary afferent neurons and NS-4591 was shown to inhibit the number of action potentials generated by suprathreshold depolarizing pulses. NS-4591 reduces the amplitude of detrusor twitches in a concentration dependent manner. in vivo experiments in rats and cats have demonstrated that 30 mg/kg inhibits bladder hyper activity induced by capsaicin and acetic acid. NS-4591 might prove to be an important agent for the treatment of bladder hyperactivity.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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