α-Conotoxin Vc1.1 TFA

Cat No.:V81790 Purity: ≥98%
α-Conotoxin Vc1.1 TFA is a disulfide peptide extracted from Conus victoriae and a selective nAChR antagonist.
α-Conotoxin Vc1.1 TFA Chemical Structure Product category: nAChR
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
α-Conotoxin Vc1.1 TFA is a disulfide peptide extracted from Conus victoriae and a selective nAChR antagonist. α-Conotoxin Vc1.1 TFA inhibits α3α5β2, α3β2 and α3β4 with IC50s of 7.2 μM, 7.3 μM and 4.2 μM respectively. It has less inhibitory effect on other nAChR subtypes and can be used for the study of neuropathic pain.
Biological Activity I Assay Protocols (From Reference)
Targets
IC50: 7.2 μM (α3α5β2), 7.3 μM (α3β2) and 4.2 μM (α3β4)[1]
ln Vitro
Using a PCR search of cDNAs from Conus victoriae venom ducts, the α-Conotoxin Vc1.1 was initially identified. In isolated bovine chromaffin cells, α-Conotoxin Vc1.1 preferentially targets peripheral nAChR subtypes over central subtypes and suppresses nicotine-evoked membrane currents in a concentration-dependent manner. Vc1.1's three-dimensional structure is supported by the I-III, II-IV disulfide connection observed in other alpha-conotoxins, and it consists of a short alpha-helix spanning residues Pro6 to Asp11. The cysteine spacing in α-Conotoxin Vc1.1's sequence indicates that it belongs to the 4/7 subclass of α-conotoxins, which also contains the well-researched conotoxins MII, EpI, and PnIB[1].
ln Vivo
In addition to suppressing pain behaviors, α-Conotoxin Vc1.1 (0.18–18 μg/μL) intramuscular injection given daily for seven days to male Sprague-Dawley rats also speeds up the functional recovery of injured neurons[1]. Result: Suppressed pain behaviors and accelerates functional recovery of injured neurones. Animal Model: Outbred male Sprague-Dawley rats (3-4 months old; 250-350 g) bearing chronic constriction injury (CCI)[1]. Dosage: 0.18 μg/μL, 1.8 μg/μL, or 18 μg/μL; Administration: Intramuscular injection; daily; for 7 days.
Animal Protocol
Animal/Disease Models: Outbred male SD (Sprague-Dawley) rats (3-4 months old; 250-350 g) bearing with chronic constriction injury (CCI)[1]
Doses: 0.18 μg/μL, 1.8 μg/μL or 18 μg/μL
Route of Administration: intramuscular (im)injection ; daily; for 7 days
Experimental Results: Suppressed pain behaviors and also accelerates functional recovery of injured neurones.
References
[1]. Richard J Clark, et al. The Synthesis, Structural Characterization, and Receptor Specificity of the Alpha-Conotoxin Vc1.1. J Biol Chem. 2006 Aug 11;281(32):23254-63.
[2]. Narmatha Satkunanathan, et al. Alpha-conotoxin Vc1.1 Alleviates Neuropathic Pain and Accelerates Functional Recovery of Injured Neurones. Brain Res. 2005 Oct 19;1059(2):149-58.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C73H104F3N23O27S4
Molecular Weight
1921.00
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)
Solubility Data
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 0.5206 mL 2.6028 mL 5.2056 mL
5 mM 0.1041 mL 0.5206 mL 1.0411 mL
10 mM 0.0521 mL 0.2603 mL 0.5206 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.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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