Ziconotide Acetate | CAS 107452-89-1 | N-Type Calcium Channel Antagonist (Research Use Only) | Knowlux

Product Description

Ziconotide Acetate, CAS 107452-89-1, is a synthetic 25-amino-acid peptide corresponding to omega-conotoxin MVIIA, originally isolated from the venom of the marine cone snail Conus magus, supplied by Knowlux for laboratory research use. The peptide is constrained by three intramolecular disulfide bridges and is C-terminally amidated. The molecular formula is C102H172N36O32S7 (free peptide) and the molecular weight is 2639.13 g/mol. Each lot is released with a lot-specific COA, MSDS and analytical traceability.

CAS and Salt Form Clarification: CAS 107452-89-1 is the free peptide registry for Ziconotide and is the identifier applied to both the free peptide and the acetate salt across ChemicalBook, MedChemExpress, Selleck, and Chinese supplier listings. The acetate salt is not consistently assigned a separate CAS in commercial catalogues; the counter-ion is declared on the lot COA. MedChemExpress lists the acetate salt as C102H172N36O32S7.xC2H4O2 without a discrete acetate CAS. A trifluoroacetate (TFA) salt is also commercially available and is assigned a distinct formula (C116H179F21N36O46S7, MW 3437.3) by TargetMol, reflecting the TFA counter-ion mass. Knowlux specifies the salt basis and counter-ion content per lot. Buyers should confirm whether the quoted material is acetate salt, TFA salt, or free peptide before procurement, as the counter-ion affects mass balance and apparent molarity.

Structural Complexity Note: Ziconotide contains six cysteine residues forming three disulfide bonds with the connectivity Cys1-Cys16, Cys8-Cys20, and Cys15-Cys25. This triple-disulfide architecture is the defining structural feature of the omega-conotoxin family and is essential for biological activity. Correct disulfide pairing is a critical quality attribute that cannot be inferred from a single HPLC purity figure. The peptide also contains a methionine residue (Met12) that is susceptible to oxidation to methionine sulfoxide, an impurity that can compromise potency. Buyers should request disulfide mapping or partial-reduction MS data, and methionine sulfoxide content data, where assay performance depends on channel blockade.

Product Parameters

Product Details

1. Overview

Ziconotide is a synthetic form of omega-conotoxin MVIIA, a 25-residue peptide originally identified in the venom of Conus magus. It is a potent and selective antagonist of N-type voltage-gated calcium channels (CaV2.2), which are concentrated on presynaptic nerve terminals in the dorsal horn of the spinal cord. Blockade of these channels reduces calcium influx and inhibits the release of pronociceptive neurotransmitters including glutamate, calcitonin gene-related peptide (CGRP), and substance P, thereby interrupting pain signal transmission. In clinical medicine, Ziconotide is approved for intrathecal analgesia in severe chronic pain. The material supplied under this specification is research-grade and is not intended for human administration. Knowlux supplies this compound strictly for laboratory investigation of CaV2.2 channel pharmacology, synaptic transmission, and neuropathic pain mechanisms.

2. Receptor Pharmacology and Selectivity

Ziconotide binds N-type calcium channels (CaV2.2) with exceptionally high affinity. Reported equilibrium dissociation constants (Kd) in rat brain membranes range from 1.1 to 18 pM, and functional inhibition IC50 values in the same system range from 2 to 55 pM. In heterologous expression systems, potency varies with the holding potential: IC50 values of 1.3 +/- 0.1 uM at -50 mV and 10.2 +/- 0.6 uM at -80 mV have been reported in tsA-201 cells expressing CaV2.2. In rat superior cervical ganglion neurons, blockade of high-voltage-activated calcium currents occurs with an IC50 of 32 nM, and inhibition of depolarization-induced norepinephrine release is observed at IC50 values of 1.2 nM (peripheral sympathetic efferents) and 5.5 nM (hippocampus). These values are assay- and system-dependent and are provided for scientific reference only. The selectivity of Ziconotide for CaV2.2 over other voltage-gated calcium channel subtypes (CaV1, CaV2.1, CaV2.3, CaV3) is a key pharmacological property that distinguishes it from non-selective calcium channel blockers.

3. Research Applications

Published pharmacological characterizations and documented protocols describe the following research applications:

• CaV2.2 (N-type) channel binding and functional blockade assays (patch clamp, calcium imaging, neurotransmitter release)

• Synaptic transmission and spinal dorsal horn pain signaling studies

• Neuropathic and chronic pain mechanism research in animal models

• Selectivity profiling against other voltage-gated calcium channel subtypes

• Disulfide-rich peptide folding, oxidation, and analytical characterization (a model system for polycyclic conotoxins)

• Reference standard development for HPLC and LC-MS analytical methods

These descriptions are derived from published research and are provided for scientific reference only. They do not constitute clinical guidance or dosing recommendations.

Quality Control

Solubility and Handling

Solubility: Ziconotide Acetate is freely soluble in water. MedChemExpress reports H2O solubility of 100 mg/mL, DMSO solubility of 25 mg/mL, and PBS solubility of 50 mg/mL, all requiring sonication. ChemicalBook describes the compound as freely soluble in water and practically insoluble in methyl tert-butyl ether. BenchChem notes that Ziconotide is a hydrophilic molecule that is freely soluble in water. The high aqueous solubility reflects the peptide's highly basic character (isoelectric point approximately 11.2) and distinguishes it from the more lipophilic conotoxins and hydrophobic research peptides. For stock preparation, water or PBS is the preferred solvent; DMSO is feasible at 25 mg/mL for applications requiring anhydrous conditions. Prepare solutions fresh and aliquot to avoid repeated freeze-thaw cycles.

Handling Precautions: Use powder-handling containment (glove box or fume hood with particulate control). Avoid inhalation of fine powder. ChemicalBook assigns GHS06 (Danger, H301+H331, toxic if swallowed or inhaled) and UN 3172 (Toxic organic compounds, n.o.s.) for this material. Wear nitrile gloves, lab coat, and eye protection. The Met12 residue is susceptible to oxidation; BenchChem technical guidance notes that dilute solutions of omega-conopeptides are highly unstable due to Met12 oxidation and recommends addition of 50 ug/mL L-methionine as a stabilizing agent where prolonged solution storage is unavoidable. Ziconotide is most stable at pH 3.0 to 5.0; avoid neutral to alkaline conditions for extended periods.

Storage and Stability

Storage guidance for Ziconotide Acetate diverges in a pattern consistent with its disulfide- and methionine-containing structure. MedChemExpress specifies 2 years at -80C and 1 year at -20C for powder under nitrogen, with solutions stable for 6 months at -80C or 1 month at -20C. Selleck, Biorbyt, and InvivoChem specify 3 years at -20C for powder, with InvivoChem additionally listing 2 years at 4C. BenchChem recommends -20C for powder and notes that shipping with ice packs preserves disulfide-bond integrity; however, Selleck states that stability testing supports room-temperature shipping without cooling measures for short transit periods. The divergence between -20C and -80C recommendations is likely attributable to differences in the stability-indicating methods used to support each shelf-life claim; -80C under nitrogen is the conservative archival condition, while -20C is adequate for routine working inventories within the supplier-specified window. For reconstituted solutions, stability is substantially shorter and pH-dependent: Ziconotide is most stable at pH 3.0 to 5.0, and dilute solutions are prone to Met12 oxidation. Prepare solutions fresh, aliquot, and avoid repeated freeze-thaw cycles. Protect from light and moisture throughout storage.

Documentation Support

Per lot: COA, MSDS, certificate of origin, HPLC chromatogram, and mass spectrometry data. Disulfide connectivity data, methionine sulfoxide content, acetate content, water content, and peptide content available on request. Custom specifications and third-party inspection can be arranged on a project basis.

About Knowlux

Knowlux Biotechnology is a GMP-oriented manufacturer and supplier of peptides, APIs and fine-chemical research compounds, operating from Hubei, China. We serve research groups, CDMOs and distributors in more than 40 countries, and support contract synthesis, custom packaging and technical documentation requests.

Compliance Statement

FOR RESEARCH USE ONLY. NOT FOR HUMAN USE. NOT FOR DIAGNOSTIC OR THERAPEUTIC USE.

This product is supplied for laboratory research use only. It is not for human or animal administration, not for diagnostic or therapeutic use, not for retail sale, and not for personal use. Ziconotide is an approved medicinal product in certain jurisdictions for specific clinical indications (severe chronic pain via intrathecal administration); however, the material offered under this specification is research-grade and is not intended for clinical use. The purchaser is responsible for verifying product specifications against their specific research requirements and for compliance with all applicable institutional, local, and national regulations governing research chemical acquisition, storage, and use. Research context statements are for scientific reference only and do not constitute medical advice, promotional claims, or dosing guidance.

Data Verification Notes: The molecular formula C102H172N36O32S7 and molecular weight 2639.13 g/mol are confirmed by MedChemExpress, GL Biochem, ChemicalBook (Chengdu Shengnuo), Adooq, and Hoelzel/Bachem. The sequence CKGKGAKCSRLMYDCCTGSCRSGKC-NH2 with disulfide bridges Cys1-Cys16, Cys8-Cys20, and Cys15-Cys25 is consistent across MedChemExpress, GL Biochem, Adooq, and BenchChem. The CAS 107452-89-1 is applied to both the free peptide and the acetate salt in commercial listings; MedChemExpress represents the acetate as C102H172N36O32S7.xC2H4O2 without a discrete acetate CAS. The TFA salt (C116H179F21N36O46S7, MW 3437.3) is a distinct salt form assigned by TargetMol and is noted for reference. The Kd and IC50 values (Kd 1.1-18 pM; IC50 2-55 pM in rat brain membranes; IC50 1.3 uM and 10.2 uM at -50 mV and -80 mV in tsA-201 cells; IC50 32 nM in rat SCG neurons) are from Bertin Bioreagent and BenchChem compilations and are assay-dependent. The pH stability range (3.0-5.0) and the Met12 oxidation liability are from BenchChem technical documentation. The GHS06 hazard classification (H301+H331, UN 3172) is from ChemicalBook (Chengdu Shengnuo). Storage shelf-life divergence (-20C versus -80C) is reported as-is; the -80C under nitrogen condition is presented as the conservative archival option.

Formatting Note: All formulas, sequences, and comparison operators use plain ASCII notation to prevent character corruption on the platform. The micro symbol has been rendered as "u" in "uM" and "ug/mL" to avoid non-ASCII character risk. Section headings, table alignment, and spacing follow the approved product detail pattern. No trailing spaces or non-breaking characters are used; tables use consistent pipe alignment.