Calciseptine

Non Antibodies

Proteins

Israel

Storage as Solution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles. - Storage before Reconstitution: The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture. - Storage after Reconstitution: The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Lyophilized

CaS, Calciseptin - A Specific Blocker of L-Type CaV Channels

A Specific Blocker of L-Type Ca_V Channels

12352202

Disulfide bonds between: Cys³-Cys²², Cys¹⁷-Cys³⁹, Cys⁴¹-Cys⁵² and Cys⁵³-Cys⁵⁸

Calciseptine is a specific antagonist of L-type CaV channels1.

no

Calciseptine is a peptide toxin originally isolated from black mamba (Dendroaspis polylepsis) venom (1, 2). A three-finger toxin, calciseptine consists of 60 amino acids with 4 disulfide bridges (2). It is a specific L-type CaV channel blocker selective for CaV1.2 (3). Calciseptine binds to the shoulder of the CaV1.2 pore domain and traps the channel in a non-conductive conformation (4).Calciseptine blocks spontaneous or K+-induced contraction of cardiac and smooth muscle cells (2). However, in skeletal muscle, it increases L-type currents, modulating Ca2+ permeation (5). Using a patch clamp, calciseptine was shown to specifically block L-type CaV channel currents in neuronal cells in culture, with IC50 values of 15-500 nM (2). It was also shown to reduce the open probability and availability of the L-type channel in guinea pig portal vein smooth muscle cells, using outside-out patch clamping (6).CaV1.2 is one of 10 voltage-gated calcium channels (VGCCs), which are divided into three families based on the pore-forming α1 subunit (7); they were originally divided based on activation voltage current (8). Encoded by the CACNA1C gene, CaV1.2 consists of the three subunits α1, a2δ, and β. This channel is expressed by smooth and cardiac muscle, pancreas, neurons, and fibroblasts. It is involved in central nervous system function and neuroendocrine regulation, cardiac and smooth muscle contractibility, and multiple other physiological processes (9).