SR 33805 oxalate

Non Antibodies

L-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

654, 77

A Specific Blocker of L-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

SR 33805, a fantofarone derivative, is a potent Ca2+ channel antagonist1. It binds allosterically to the α1-subunit of L-type Ca2+ channels (Kd = 20 pM), at a site distinct from other types of blockers2. It potently inhibits the Ca2+ channel in primary mouse cardiac myocytes cultures with IC50 values ranging from 4 to 33 nM3.

Yes

Two types of voltage-gated Ca2+ channels (VGCC, CaV) are found in most nonexcitable cells, T-type and the L-type Ca2+ channels1-2.SR 33805, a fantofarone derivative, is a potent Ca2+ channel antagonist3. It binds allosterically to the a1-subunit of L-type Ca2+ channels (Kd = 20 pM), at a site distinct from other types of blockers4. It potently inhibits the Ca2+ channel, and hence prevents Ca2+ influx, in primary mouse cardiac myocytes cultures with IC50 values ranging from 4.1 to 33 nM5.SR 33805 shows selectivity for vascular smooth muscle, inducing vasorelaxation without producing inotropic or chronotropic effects6. It inhibits PDGF-stimulated smooth muscle cell proliferation and the associated rise in intracellular Ca2+ concentration with IC50 values of 0.2 µM and 0.3 µM, respectively7.Despite its strong Ca2+-antagonistic properties, SR33805 increases cardiac cell contractile activity as a consequence of its Ca2+-sensitizing effects. These effects are attributable to both an increase in the maximal Ca2+-activated force and a length-dependent Ca2+-sensitization3.