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Home / Proteins & Peptide / Proteins

alpha-Conotoxin Vc1.1

SKU : BHP21300307

A Potent Antagonist of alpha9alpha10 nAChR, a Weak Antagonist of other nAChRs and an Agonist of GABAB receptors

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Mfr.No.	STV-500, STV-500_0.1 mg, STV-500_0.5 mg, STV-500_1 mg, STV-500_10 mg, STV-500_5 mg
Description	A Potent Antagonist of alpha9alpha10 nAChR, a Weak Antagonist of other nAChRs and an Agonist of GABAB receptors
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	C71H103N23O25S4
Background	alpha-Conotoxin Vc1.1 (Vc1.1) is a 16 amino acid synthetic version of a conopeptide, which was first discovered from a PCR screen of cDNA from the venom ducts of the tropical marine snail, Conus victoriae1. Vc1.1 adopts the archetypal three-dimensional structure of a-conotoxins, which consists of a helical region stabilized by two disulfide bonds. The alpha-conotoxin family members are defined, in part, by their pharmacological targets, the nicotinic acetylcholine receptors (nAChRs). Vc1.1 is a neuronal nAChR antagonist that displays selectivity for the alpha9alpha10 subtype2. A subset of alpha-conotoxins have been shown to inhibit high-voltage-activated (HVA) calcium channel currents via activation of the gamma-aminobutyric acid (GABA) receptor B (GABABR). GABABRs are G-protein-coupled receptors (GPCRs) for GABA, the main inhibitory neurotransmitter in the brain. GABABRs are promising targets for the treatment of various neurological and psychiatric disorders, including pain, depression, and drug addiction. Vc1.1 was the first alpha-conotoxin shown to inhibit HVA calcium channels (CaV2.2 and CaV2.3) via GABABR activation3,4.Vc1.1 alleviates neuropathic pain in three human neuropathic pain rat models and accelerates the functional recovery of injured neurons5. This toxin has been tested in human clinical trials for the treatment of neuropathic pain, where it exhibited both clean safety and side effect profiles. In addition to its antinociceptive and antihyperalgesic actions in neuropathic pain models, Vc1.1 inhibits human DRG neurons via activation of the GABABR, which are the primary transducers at the start of the pain processing pathway6.
Biological Activity	A specific antagonist of alpha9alpha10 nAChR that also selectively modulate high-voltage-activated (HVA) calcium channel acting as agonists via G-protein -coupled GABAB receptors 1,2.
Formulation	Lyophilized from double distilled water (ddH2O). May contain TFA as a residual counter ion.
Molecular Weight	1807 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 peptide
Accession Number	P69747
Concentration	20 nM - 1 uM
Form	Lyophilized
Notes	Bioassay Tested: yes Steril endotoxin free: no Is Toxin: Yes
Cas Number	740980-24-9
UNSPSC Code	12352202
Lead Time	1-2 Business Days
Modifications	Disulfide bonds between: Cys2-Cys8, Cys3-Cys16 Cys16- C-terminal amidation
Origin	Conus victoriae (Queen Victoria cone)

Synonyms	ACV1, Vc1.1, Alpha-Conotoxin Vc1.1
Gene Id	CHRNA9, CHRNA10, CHRNA6, CHRNA3, CHRNB2, CHRNB3, CACNA1B, CACNA1E, CHRNB4, GABBR1, GABBR2
Sequence	GCCSDPRCNYDHPEIC-NH2
Target	alpha9alpha10 nAChRs, GABA(B) receptors, Neuronal nAChR, Cav2.2, Cav2.3

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	Sandall, D.W. et al. (2003) Biochemistry, 42, 6904. Vincler, M. et al. (2006) PNAS, 103(47), 17780. Callaghan, B. et al. (2008) J. Neurosci., 28, 10943. Sadeghi, M. et al. (2018) ACS Chem. Biol., 13, 1577. Satkunanathan, N. et al. (2005) Brain Res., 1059, 149. Castro, J. et al. (2017) Gut, 66, 1083. Callaghan, B. et al. (2008) J. Neurosci., 28, 10943.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHP21300307-1	STV-500_0.1 mg	0.1 mg	$281		Add to Cart
BHP21300307-2	STV-500_0.5 mg	0.5 mg	$765		Add to Cart
BHP21300307-3	STV-500_1 mg	1 mg	$1071		Add to Cart
BHP21300307-4	STV-500_10 mg	10 mg	$4523		Add to Cart
BHP21300307-5	STV-500_5 mg	5 mg	$3206		Add to Cart

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