| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
Purity: =99.90%
| Targets |
N-type calcium channel
Ziconotide acetate targets N-type voltage-gated calcium channels. By blocking these channels, the compound reduces calcium influx into neurons, thereby decreasing neurotransmitter release at synapses. The N-type calcium channels are located on the primary afferent neurons in the pain pathway. By blocking these channels, Ziconotide acetate produces potent analgesic effects. The compound's high selectivity for N-type channels over other calcium channel subtypes contributes to its therapeutic efficacy. |
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| ln Vitro |
Ziconotide acetate only partially suppresses high-voltage-activated calcium currents in differentiated human neuroblastoma IMR32 cells, rat superior cervical ganglion neurons, and rat hippocampus neurons because most native cells have a range of distinct calcium channels. Additionally, ziconotine acetate decreases calcium currents that arise from HEK cells, tsa-201 cells, and Xenopus laevis oocytes expressing the α1B subunit[1]. By limiting the production of pronociceptive neurotransmitters in the spinal cord's dorsal horn, ziconide acetate inhibits the transmission of pain signals, which is how it exerts its antinociceptive action[1].
In vitro, Ziconotide acetate is a potent and selective blocker of N-type calcium channels. It reduces calcium currents that result from expression of the α1B subunit in HEK cells, tsa-201 cells, and Xenopus laevis oocytes. In most native cells, Ziconotide acetate only partially reduces high-voltage-activated calcium currents due to the presence of multiple calcium channel types. The compound reduces synaptic transmission by inhibiting neurotransmitter release. Standard in vitro assays include patch-clamp electrophysiology on cells expressing N-type calcium channels and measurement of neurotransmitter release. |
| ln Vivo |
In a mouse model of experimental autoimmune encephalomyelitis (EAE), ziconotate (it; 25-100 pmol/site; 5 μL; on the 4th, 10th, 15th, 20th, and 24th days) acetate decreases IL-1β and IL-23 levels in the CNS and splenic production of IL-17 25 days after MOG35-55-elicited EAE[2].
In vivo, Ziconotide acetate is used clinically as an analgesic for severe chronic pain. It is administered intrathecally (into the spinal fluid) to bypass the blood-brain barrier and achieve local effects in the spinal cord. By blocking N-type calcium channels on primary afferent neurons, the compound reduces synaptic transmission and produces potent analgesia. Ziconotide acetate is approved for the treatment of severe chronic pain in patients who are intolerant or refractory to other treatments. |
| Enzyme Assay |
For non-cell-based receptor binding assays, Ziconotide acetate can be evaluated using membrane preparations from cells expressing N-type calcium channels (α1B subunit). Radioligand binding displacement experiments are performed using a radiolabeled conotoxin or other N-type channel ligand. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand at appropriate conditions. Bound radioligand is separated from free by rapid filtration. Nonspecific binding is determined in the presence of excess unlabeled ligand. IC50 values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing N-type calcium channels (e.g., HEK cells expressing the α1B subunit) are cultured in appropriate media. Patch-clamp electrophysiology is performed in voltage-clamp mode to record calcium currents. Cells are treated with various concentrations of Ziconotide acetate, and the reduction in calcium current amplitude is measured. IC50 values are calculated from concentration-response curves. For neurotransmitter release assays, synaptosomes or neuronal cultures are treated with the compound, and neurotransmitter release is measured using biochemical or electrochemical methods.
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| Animal Protocol |
Animal/Disease Models: Female C57BL/6mice (18-22 g, 6- 8 weeks old) injected with myelin oligodendrocytes glycoprotein[2]
Doses: 25 pmol/site, 50 pmol/site, 100 pmol/site Route of Administration: Intrathecal injection; on the 4th, 10th, 15th, 20th, and 24th days Experimental Results: Dramatically decreased the mechanical hypersensitivity in animals with EAE. For in vivo animal studies, Ziconotide acetate is typically administered intrathecally to rodents. In pain models (e.g., formalin test, hot plate test, neuropathic pain models), nociceptive responses are measured following compound administration. The compound's analgesic efficacy is assessed by comparing responses in treated and control animals. Pharmacokinetic studies involve measuring compound concentrations in cerebrospinal fluid and plasma. Dosing regimens vary depending on the specific model and desired exposure levels. Ziconotide acetate is administered intrathecally in clinical settings. |
| ADME/Pharmacokinetics |
Ziconotide acetate is a peptide with a molecular formula of C104H176N36O34S7. It is administered intrathecally for the treatment of severe chronic pain. The compound is a potent and selective blocker of N-type calcium channels. It reduces synaptic transmission by inhibiting neurotransmitter release. The compound is available for research use only and is a controlled substance. It should be stored according to the manufacturer's recommendations.
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| Toxicity/Toxicokinetics |
The toxicity profile of Ziconotide acetate includes potential neurologic and psychiatric adverse effects due to its mechanism of action in the central nervous system. Common adverse effects may include dizziness, nausea, confusion, and gait disturbances. The compound is a controlled substance and is only available for research use or under strict clinical supervision. Standard toxicological evaluation would include assessment of neurologic, psychiatric, and cardiovascular effects. The compound is not for human consumption outside of approved clinical use.
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| References | |
| Additional Infomation |
See also: Ziconopeptide Acetate (note moved to).
Ziconotide acetate (SNX-111 acetate) is a peptide that is a potent and selective blocker of N-type calcium channels. It reduces synaptic transmission and is used clinically as an analgesic for severe chronic pain. It is administered intrathecally to produce local effects in the spinal cord. Ziconotide acetate is a synthetic version of a peptide originally found in the venom of the marine cone snail Conus magus. It is approved for the treatment of severe chronic pain in patients who are intolerant or refractory to other treatments. |
| Molecular Formula |
C104H176N36O34S7
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|---|---|
| Molecular Weight |
2699.18605232239
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| Exact Mass |
2698.122
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| CAS # |
914454-03-8
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| Related CAS # |
Ziconotide;107452-89-1;Ziconotide TFA
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| PubChem CID |
72941949
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| Sequence |
Cys-Lys-Gly-Lys-Gly-Ala-Lys-Cys-Ser-Arg-Leu-Met-Tyr-Asp-Cys-Cys-Thr-Gly-Ser-Cys-Arg-Ser-Gly-Lys-Cys-NH2 (Disulfide bridge:Cys1-Cys16;Cys8-Cys20;Cys15-Cys25)
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| SequenceShortening |
CKGKGAKCSRLMYDCCTGSCRSGKC-NH2 (Disulfide bridge:Cys1-Cys16;Cys8-Cys20;Cys15-Cys25)
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
43
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| Hydrogen Bond Acceptor Count |
48
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| Rotatable Bond Count |
40
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| Heavy Atom Count |
181
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| Complexity |
5510
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| Defined Atom Stereocenter Count |
22
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| SMILES |
C(=O)(O)C.C(C1C=CC(O)=CC=1)[C@@H]1NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H]2NC([C@@H](NC([C@@H](NC(CNC([C@@H](NC(CNC([C@@H](NC([C@H](CSSC[C@H]3C(N[C@H](C(NCC(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(NCC(N[C@H](C(N[C@@H](CSSCC(C(N3)=O)NC(=O)[C@H](CC(=O)O)NC1=O)C(=O)N)=O)CCCCN)=O)=O)CO)=O)CCCNC(N)=N)=O)CSSC2)=O)CO)=O)=O)[C@H](O)C)=O)N)=O)CCCCN)=O)=O)CCCCN)=O)=O)C)=O)CCCCN)=O
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| InChi Key |
LBACTXHPMJIKTR-XZSNVYKZSA-N
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| InChi Code |
InChI=1S/C102H172N36O32S7.C2H4O2/c1-50(2)34-63-91(161)127-62(26-33-171-5)90(160)129-64(35-53-22-24-54(143)25-23-53)92(162)130-65(36-78(148)149)93(163)135-72-48-175-173-45-69(80(108)150)133-86(156)58(18-8-12-29-105)121-76(146)39-117-85(155)66(41-139)131-88(158)61(21-15-32-114-102(111)112)126-96(166)70-46-176-177-47-71(97(167)132-68(43-141)95(165)125-60(87(157)128-63)20-14-31-113-101(109)110)134-89(159)59(19-9-13-30-106)123-81(151)51(3)119-74(144)37-115-83(153)56(16-6-10-27-103)120-75(145)38-116-84(154)57(17-7-11-28-104)124-82(152)55(107)44-172-174-49-73(137-98(72)168)99(169)138-79(52(4)142)100(170)118-40-77(147)122-67(42-140)94(164)136-70;1-2(3)4/h22-25,50-52,55-73,79,139-143H,6-21,26-49,103-107H2,1-5H3,(H2,108,150)(H,115,153)(H,116,154)(H,117,155)(H,118,170)(H,119,144)(H,120,145)(H,121,146)(H,122,147)(H,123,151)(H,124,152)(H,125,165)(H,126,166)(H,127,161)(H,128,157)(H,129,160)(H,130,162)(H,131,158)(H,132,167)(H,133,156)(H,134,159)(H,135,163)(H,136,164)(H,137,168)(H,138,169)(H,148,149)(H4,109,110,113)(H4,111,112,114);1H3,(H,3,4)/t51-,52+,55-,56-,57-,58-,59-,60-,61-,62-,63-,64-,65-,66-,67-,68-,69-,70-,71-,72-,73-,79-;/m0./s1
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| Chemical Name |
acetic acid;2-[(1R,4S,7S,13S,16R,21R,24S,27S,30S,33S,36S,39S,42R,45S,48S,54S,60S,63R,68R,71S,77S)-63-amino-13,45,54,60-tetrakis(4-aminobutyl)-4,36-bis(3-carbamimidamidopropyl)-16-carbamoyl-71-[(1R)-1-hydroxyethyl]-7,39,77-tris(hydroxymethyl)-27-[(4-hydroxyphenyl)methyl]-48-methyl-33-(2-methylpropyl)-30-(2-methylsulfanylethyl)-2,5,8,11,14,23,26,29,32,35,38,41,44,47,50,53,56,59,62,69,72,75,78,85-tetracosaoxo-18,19,65,66,81,82-hexathia-3,6,9,12,15,22,25,28,31,34,37,40,43,46,49,52,55,58,61,70,73,76,79,84-tetracosazatricyclo[40.37.4.221,68]pentaoctacontan-24-yl]acetic acid
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| Synonyms |
Ziconotide (acetate)
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: 100 mg/mL
DMSO: 25 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (Infinity mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.3705 mL | 1.8524 mL | 3.7048 mL | |
| 5 mM | 0.0741 mL | 0.3705 mL | 0.7410 mL | |
| 10 mM | 0.0370 mL | 0.1852 mL | 0.3705 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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