SR 33805 oxalate.
A Specific L-type Cav Channel Blocker.
Two types of voltage-gated�Ca2+ channels (VGCC, Cav) are found in most nonexcitable cells, T-type and the L-type Ca2+ channels.
SR 33805, a fantofarone derivative, is a potent Ca2+ channel antagonist. It binds allosterically to the alpha1-subunit of L-type Ca2+ channels (Kd = 20 pM), at a site distinct from other types of blocker. 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 nM.
SR 33805 shows selectivity for vascular smooth muscle, inducing vasorelaxation without producing inotropic or chronotropic effects. 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, respectively.
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+-sensitization.
Alomone Labs is pleased to offer SR 33805 oxalate (#S-105).
Ion Channel Modulators; Voltage - Gated Ca2+ Channel Blockers
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