BUY L-651,582

L-651,582. An Effective L-type Ca_v Channel Blocker.

Two subtypes of voltage-Gated Ca²⁺ Channels (VGCC, Ca_v) are found in most nonexcitable cells, the T-type (Ca_v3) and the L-Type (Ca_v1)� Ca²⁺ channels.
L-651,582, is an antiproliferative, antiangiogenic, antimetastatic and antiparasitic agent, which is also selective towards numerous mismatch repair-deficient tumor cell lines in vitro. It is a voltage-gated L-type Ca²⁺ channel blocker with an IC₅₀ of 0.5 μg/ml.
Patch clamp measurements of current through L- and T-type channels in guinea pig atrial cells also indicate that L-651,582 is a Ca²⁺ antagonist.
Block of L-type calcium channels is voltage-dependent and the apparent dissociation constant for the high affinity state is 0.2 μg/ml. The IC₅₀ for block of T-type Ca²⁺ channels is 1.4 μg/ml.

Ion Channel Modulators; Voltage - Gated Ca²⁺ Channel Blockers.