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Home / Proteins & Peptide / Proteins

Calciseptine

SKU : BHP21300112

A Specific Blocker of L-Type CaV Channels

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Mfr.No.	SPC-500, SPC-500_0.25 mg, SPC-500_0.5 mg, SPC-500_1 mg, SPC-500_10 mg, SPC-500_5 mg, SPC-500_70 mcg
Description	A Specific Blocker of L-Type CaV Channels
Reconstitution	Centrifuge the vial (10,000 x g for 5 minutes) before adding solvent 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. Gently tap, tilt, and roll the vial to aid dissolution. 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 uM - 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.
Molecular Formula	C299H468N90O87S10
Background	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 alpha1 subunit (7); they were originally divided based on activation voltage current (8). Encoded by the CACNA1C gene, CaV1.2 consists of the three subunits alpha1, a2delta, and beta. 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).
Biological Activity	Calciseptine is a specific antagonist of L-type CaV channels1.
Formulation	Lyophilized from double distilled water (ddH2O). May contain TFA as a residual counter ion.
Molecular Weight	7036 Da
Solubility	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 uM - 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.
Source	Synthetic protein
Accession Number	P22947
Concentration	500 nM
Form	Lyophilized
Notes	Bioassay Tested: yes Steril endotoxin free: no Is Toxin: Yes
Cas Number	178805-91-9
UNSPSC Code	12352202
Lead Time	1-2 Business Days
Modifications	Disulfide bonds between: Cys3-Cys22, Cys17-Cys39, Cys41-Cys52 and Cys53-Cys58
Origin	Dendroaspis polylepis polylepis (Black mamba)

Synonyms	CaS, Calciseptin
Gene Id	CACNA1C
Sequence	RICYIHKASLPRATKTCVENTCYKMFIRTQREYISERGCGCPTAMWPYQTECCKGDRCNK-OH
Target	L-type Ca2+ channels

Country Of Origin	Israel/IL
Purity	>=98% (HPLC)
Storage	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. 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 of solutions: 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.

Applications	Electrophysiology

Reference	H. Schweitz, J. N. Bidard, M. Lazdunski, Toxicon. 28, 84756 (1990). DOI: 10.1016/s0041-0101(09)80007-x J. R. de Weille, H. Schweitz, P. Maes, A. Tartar, M. Lazdunski, Proc. Natl. Acad. Sci. 88, 24372440 (1991). DOI: 10.1073/pnas.88.6.2437 P. Mesirca et al., Nat. Commun. 15, 54 (2024). DOI: 10.1038/s41467-023-43502-w S. Gao et al., Cell. 186, 5363-5374.e16 (2023). DOI: 10.1016/j.cell.2023.10.007 M. C. García, Z. Hernández-Gallegos, J. Escamilla, J. A. Sánchez, J Membr Biol. 184, 1219 (2001). DOI: 10.1007/s00232-001-0080-7 N. Teramoto et al., Pflugers Arch. 432, 46270 (1996). DOI: 10.1007/s004240050158 A. C. Dolphin, J. Physiol. 594, 53695390 (2016). DOI: 10.1113/JP272262 W. A. Catterall, Cold Spring Harb. Perspect. Biol. 3, a003947 (2011). DOI: 10.1101/cshperspect.a003947 F. Hofmann, V. Flockerzi, S. Kahl, J. W. Wegener, Physiol. Rev. 94, 303326 (2014). DOI: 10.1152/physrev.00016.2013 de Weille, J.R. et al. (1991) Proc. Natl. Acad. Sci. U.S.A. 88, 2437.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHP21300112-1	SPC-500_0.25 mg	0.25 mg	$406		Add to Cart
BHP21300112-2	SPC-500_0.5 mg	0.5 mg	$649		Add to Cart
BHP21300112-3	SPC-500_1 mg	1 mg	$1019		Add to Cart
BHP21300112-4	SPC-500_10 mg	10 mg	$4703		Add to Cart
BHP21300112-5	SPC-500_5 mg	5 mg	$3360		Add to Cart
BHP21300112-6	SPC-500_70 mcg	70 mcg	$168		Add to Cart

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