| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 1g |
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| Other Sizes |
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Purity: =99.15%
| Targets |
Voltage-gated sodium channels (NaV1.4, NaV1.2, NaV1.7, NaV1.5, NaV1.8). NaV1.4 and NaV1.2 are most sensitive, NaV1.7 shows intermediate sensitivity, while NaV1.5 and NaV1.8 are insensitive to µ-conopeptide CnIIIC [1]
Selectively inhibits voltage-gated sodium channel subtype NaV1.4 (IC50 = 8.7 nM). Minimal activity against NaV1.1–1.3, 1.5–1.7 (IC50 > 1 μM). [1] |
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| ln Vitro |
Channel Blockade Profile: µ-conopeptide CnIIIC potently blocks human and rodent NaV1.4 channels. At -20 mV, application of 1 µM toxin resulted in nearly irreversible blockade of NaV1.4 current, leaving a residual current of ~5%, indicating partial Na⁺ ion passage through occupied channels. TTX (tetrodotoxin) was excluded from the binding site but trapped within the pore by the toxin. For NaV1.2, NaV1.7, NaV1.5, and NaV1.8 channels, 1 µM toxin induced varying degrees of current reduction, with NaV1.5 and NaV1.8 showing minimal response [1]
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| ln Vivo |
utaneous Delivery via Iontophoresis: In porcine ear and human abdominal skin, iontophoretic delivery of µ-conopeptide CnIIIC (XEP-018) significantly increased skin deposition compared to passive diffusion. At current densities of 0.1, 0.3, and 0.5 mA/cm² for 2 hours, skin deposition reached 22.4 ± 0.4, 34.5 ± 1.4, and 57.4 ± 7.6 µg/cm², respectively (vs. passive controls: 9.8 ± 1.1 µg/cm²). Prolonging treatment to 4 hours further increased deposition to 90.9 ± 30.8 µg/cm² at 0.5 mA/cm². Co-iontophoresis with acetaminophen reduced convective solvent flow, decreasing acetaminophen permeation by ~7-fold, confirming XEP-018’s presence in the skin [2]
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| Enzyme Assay |
Patch-Clamp Electrophysiology: HEK293 or Neuro-2a cells transfected with human NaV channel α-subunits were voltage-clamped using the whole-cell configuration. Cells were superfused with extracellular solution containing 1 µM µ-conopeptide CnIIIC, and currents were recorded at various test potentials (-20 mV for NaV1.4/1.2/1.7/1.5; 10 mV for NaV1.8). Toxin-induced current blockade was analyzed for kinetics (onset/offset) and steady-state inhibition. For NaV1.4, irreversible block with residual current was observed, while other subtypes showed variable sensitivity [1]
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| Cell Assay |
Cell Culture and Transfection: HEK293 cells were cultured in DMEM supplemented with 10% FBS and transfected with plasmids encoding human NaV1.4, NaV1.2, NaV1.7, NaV1.5, or NaV1.8 α-subunits plus β-subunits. After 24–48 hours, transfected cells were used for patch-clamp experiments to measure toxin-induced current changes. Neuro-2a cells expressing NaV1.8 were similarly prepared and tested [1]
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| Animal Protocol |
Porcine Skin Model: Full-thickness porcine ear skin was mounted in Franz diffusion cells. XEP-018 solution (0.1–1 mM) was applied to the epidermal side, with iontophoresis delivered via Ag/AgCl electrodes (anodal or cathodal) at 0.1–0.5 mA/cm² for 15–240 minutes. Skin samples were analyzed for peptide deposition via HPLC or fluorescence microscopy (FITC-labeled XEP-018) [2]
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| ADME/Pharmacokinetics |
Skin Absorption: Iontophoretic delivery enhanced XEP-018 penetration into the epidermis, with deposition increasing linearly with current density and treatment duration. Maximum deposition occurred in the stratum corneum and viable epidermis, with minimal systemic absorption detected in vitro [2]
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| References | |
| Additional Infomation |
Mechanism of Action: µ-conopeptide CnIIIC acts as a pore-blocking antagonist, binding within the NaV channel’s outer vestibule to prevent ion flux. Its specificity for NaV1.4/1.2/1.7 over cardiac NaV1.5 reduces risk of cardiovascular side effects [1]
- Clinical Relevance: The toxin’s dual roles in muscle relaxation (via NaV1.4 blockade) and analgesia (via NaV1.7 modulation) make it a candidate for topical treatment of wrinkles and pain. Iontophoretic delivery offers controlled, localized drug release [2] |
| Molecular Formula |
C92H139N35O28S6
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|---|---|
| Molecular Weight |
2375.7
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| Exact Mass |
2373.89
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| Elemental Analysis |
C, 46.51; H, 5.90; N, 20.64; O, 18.86; S, 8.10
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| CAS # |
936616-33-0
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| Related CAS # |
µ-Conotoxin-CnIIIC acetate
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| Sequence |
{Glp}-Gly-Cys-Cys-Asn-Gly-Pro-Lys-Gly-Cys-Ser-Ser-Lys-Trp-Cys-Arg-Asp-His-Ala-Arg-Cys-Cys-NH2 (Disulfide bridge: Cys3-Cys15, Cys4-Cys21, Cys10-Cys22)
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| SequenceShortening |
{Glp}-GCCNGPKGCSSKWCRDHARCC-NH2 (Disulfide bridge: Cys3-Cys15, Cys4-Cys21, Cys10-Cys22)
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.71±0.1 g/cm3
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| SMILES |
O=C(N[C@]1([H])C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@]2([H])CSSC[C@](C(N[C@H](C(NCC(N3[C@](CCC3)([H])C(N[C@H](C(NCC(N[C@](CSSC[C@H](NC2=O)C(N)=O)([H])C(N[C@H](C(N[C@H](C(N[C@H](C(N4)=O)CCCCN)=O)CO)=O)CO)=O)=O)=O)CCCCN)=O)=O)=O)CC(N)=O)=O)([H])NC([C@H](CSSC1)NC(CNC([C@@H]5CCC(N5)=O)=O)=O)=O)=O)CCCNC(N)=N)=O)C)=O)CC6=CN=CN6)=O)CC(O)=O)=O)CCCNC(N)=N)=O)[C@@H]4CC7=CNC8=CC=CC=C78
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| InChi Key |
PQKXBHZHSUVYIL-XAASTXGFSA-N
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| InChi Code |
InChI=1S/C92H139N35O28S6/c1-43-73(138)113-50(15-8-22-102-91(97)98)79(144)124-64-41-161-160-40-63-88(153)119-55(27-66(95)130)76(141)107-33-70(134)127-24-10-17-65(127)90(155)116-48(13-4-6-20-93)74(139)105-31-68(132)111-60(37-157-156-36-59(72(96)137)123-89(64)154)85(150)122-58(35-129)84(149)121-57(34-128)83(148)114-49(14-5-7-21-94)77(142)117-53(25-44-29-104-47-12-3-2-11-46(44)47)81(146)125-62(39-159-158-38-61(86(151)126-63)112-69(133)32-106-75(140)52-18-19-67(131)110-52)87(152)115-51(16-9-23-103-92(99)100)78(143)120-56(28-71(135)136)82(147)118-54(80(145)109-43)26-45-30-101-42-108-45/h2-3,11-12,29-30,42-43,48-65,104,128-129H,4-10,13-28,31-41,93-94H2,1H3,(H2,95,130)(H2,96,137)(H,101,108)(H,105,139)(H,106,140)(H,107,141)(H,109,145)(H,110,131)(H,111,132)(H,112,133)(H,113,138)(H,114,148)(H,115,152)(H,116,155)(H,117,142)(H,118,147)(H,119,153)(H,120,143)(H,121,149)(H,122,150)(H,123,154)(H,124,144)(H,125,146)(H,126,151)(H,135,136)(H4,97,98,102)(H4,99,100,103)/t43-,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-,58-,59-,60-,61-,62-,63-,64-,65-/m0/s1
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| Chemical Name |
2-((3S,9R,12S,15S,18S,21S,24R,27S,30S,33S,36S,39S,42R,47R,50S,58aS,61R,68R)-33-((1H-imidazol-5-yl)methyl)-21-((1H-indol-3-yl)methyl)-50-(2-amino-2-oxoethyl)-3,18-bis(4-aminobutyl)-68-carbamoyl-27,39-bis(3-guanidinopropyl)-12,15-bis(hydroxymethyl)-36-methyl-1,4,7,10,13,16,19,22,25,28,31,34,37,40,48,51,54,60,66-nonadecaoxo-61-(2-((S)-5-oxopyrrolidine-2-carboxamido)acetamido)tetrapentacontahydro-1H,46H-47,24-(epiminopropanodithiomethano)-9,42-(methanodithioethanoiminomethano)pyrrolo[2,1-t1][1,2]dithia[5,8,11,14,17,20,23,26,29,32,35,38,41,44,47,50,53]heptadecaazacyclohexapentacontin-30-yl)acetic acid
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| Synonyms |
Mu-Conotoxin; XEP-018; CONOTOXIN; ACETY TETRAPEPTIDE-9; Cono Antiwrinkle; 936616-33-0; μ-Conotoxin Cn IIIC
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4209 mL | 2.1046 mL | 4.2093 mL | |
| 5 mM | 0.0842 mL | 0.4209 mL | 0.8419 mL | |
| 10 mM | 0.0421 mL | 0.2105 mL | 0.4209 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.
Products are for research use only; We do not sell to patients
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