الصفحة الرئيسية>>Peptides>>ω-Conotoxin GVIA

ω-Conotoxin GVIA

رقم الكتالوجGC13886

ω ؛ -Conotoxin GVIA هو مثبط لقناة N-type Ca2+.

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ω-Conotoxin GVIA التركيب الكيميائي

Cas No.: 106375-28-4

الحجم السعر المخزون الكميّة
1mg
308٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of ω-Conotoxin GVIA

ω-Conotoxin GVIA is a cone snail toxin that selectively blocks N-type channels in neurons [1].

ω-Conotoxin GVIA binds to human neocortical, rat hippocampal, and chick brain synaptic plasma membranes (IC50s = 4.6, 60, and 150 pM, respectively, in radioligand binding assays) [3,4,5].

ω-Conotoxin GVIA markedly reduced the amplitude of the tetanic contractions of the tibialis anterior muscle in mice, but tetanic facilitation was not impaired. The muscle contractions elicited by direct electrical stimulation were not significantly modified by ω-Conotoxin GVIA. ω-Conotoxin GVIA did not had any significant changes in systemic blood pressure [5].

References:
[1]. H.D. Mansvelder, J.C. Stoof, K.S. Kits. Dihydropyridine block of ω-agatoxin IVA- and ω-conotoxin GVIA-sensitive Ca2+ channels in rat pituitary melanotropic cells.Eur. J. Pharmacol., 311 (1996), pp. 293-304
[2]. Feuerstein, T.J., Dooley, D.J., and Seeger, W. Inhibition of norepinephrine and acetylcholine release from human neocortex by ω-conotoxin GVIA. J. Pharmacol. Exp. Ther. 252(2), 778-785 (1990).
[3]. Lampe, R.A., Lo, M.M., Keith, R.A., et al. Effects of site-specific acetylation on ω-conotoxin GVIA binding and function. Biochemistry 32(13), 3255-3260 (1993).
[4]. Sato, K., Park, N.G., Kohno, T., et al. Role of basic residues for the binding of ω-conotoxin GVIA to N-type calcium channels. Biochem. Biophys. Res. Commun. 194(3), 1292-1296 (1993).
[5]: Rossoni G, Berti F, La Maestra L, Clementi F. ω-Conotoxin GVIA binds to and blocks rat neuromuscular junction. Neuroscience Letters. 1994;176:185-188.

Protocol of ω-Conotoxin GVIA

Cell experiment [1]:

Cell lines

Rat pituitary melanotropic cells

Preparation Method

ω-Conotoxin GVIA was administered via a gravity-driven Y-tube system or pressure jet. The recording chamber was continuously perfused at a rate of ~ 1.5ml/min, driven by air pressure, and the bath volume was kept constant by continuous suction. Electrophysiological testing was performed. 

Reaction Conditions

1 or 10 µM

Applications

1 µM ω-Conotoxin GVIA blocked the high voltage-activated current by 25.5±3.6%. The block at 10µM ω-Conotoxin GVIA was 22.9±2.5% (not significantly different from the block by 1µM;n = 3), indicating thatω-Conotoxin GVIA yields a saturating effect.

Animal experiment [2]:

Animal models

male COBS CD (SD) rats

Preparation Method

After intravenous injection of different doses of ω-Conotoxin GVIA (1--2 nmol/kg) in rats, the sciatic nerve of the rats was stimulated and the blood pressure of the rats was measured through the carotid artery.

Dosage form

Intravenous injection, 1--2 nmol/kg

Applications

Intravenous injection caused a progressive loss of tension development of tibialis muscle indirectly evoked by the electrical stimulation of the sciatic nerve, ω-Conotoxin GVIA (1 nmol/kg i.v.) reduced the strength of muscle contraction by 75% in about 27 min (from 39.5 + 1.8 g to 9.9 + 0.4 g).

References:
[1]: H.D. Mansvelder, J.C. Stoof, K.S. Kits. Dihydropyridine block of ω-agatoxin IVA- and ω-conotoxin GVIA-sensitive Ca2+ channels in rat pituitary melanotropic cells.Eur. J. Pharmacol., 311 (1996), pp. 293-304
[2]: Rossoni G, Berti F, La Maestra L, Clementi F. ω-Conotoxin GVIA binds to and blocks rat neuromuscular junction. Neuroscience Letters. 1994;176:185-188.

Chemical Properties of ω-Conotoxin GVIA

Cas No. 106375-28-4 SDF
Canonical SMILES C[C@](O)([H])[C@@](/N=C(O)/[C@](/N=C(O)/[C@]1([H])C[C@](O)([H])CN12)([H])CC3=CC=C(O)C=C3)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N\[C@@](/C(O)=N\[C@@](C(O)=N)([H])CC4=CC=C(O)C=C4)([H])CSSC[C@@](N=C(O)[C@](N=C(O)[C@](N=C(O)[C@](N=C(O)[C@](N=C(O)[C@]5([H])C[
Formula C120H182N38O43S6 M.Wt 3037.35
الذوبان Soluble to 1 mg/ml in Water Storage Desiccate at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of ω-Conotoxin GVIA

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 0.3292 mL 1.6462 mL 3.2923 mL
5 mM 0.0658 mL 0.3292 mL 0.6585 mL
10 mM 0.0329 mL 0.1646 mL 0.3292 mL
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