Guangxitoxin 1E
Guangxitoxin 1E is a potent and selective blocker of KV2.1 and KV2.2 channels. Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM. KV2 channels underlie delayed-rectifier potassium currents in various neurons.
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- CAS. Nr.: 1233152-82-3
- Formel: C178H248N44O45S7
- Molecular Weight:3948.61
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Speicherung:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
IC50: 1-3 nM (KV2 channels); 24-54 nM (KV4.3 channels)[2]
Guangxitoxin 1E inhibits KV2 with an IC50 of 1-3 nM but has no significant effect on KV1.2, KV1.3, KV1.5, KV3.2 and BK potassium channels, nor on calcium and sodium channels CaV1.2, CaV2.2, NaV1.5, NaV1.7, NaV1.8, whereas the IC50 for KV4.3 channels is 24-54 nM[2].
In mouse β-cells, Guangxitoxin 1E inhibits 90% of IDR and, as for KV2.1, shifts the voltage dependence of channel activation to more depolarized potentials, a characteristic of gating-modifier peptides. Guangxitoxin 1E broadens theβ-cell action potential, enhances glucose-stimulated intracellular calcium oscillations, and enhances insulin secretion from mouse pancreatic islets in a glucose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1233152-82-3
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Appearance Solid
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Molecular Weight 3948.61
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Formel C178H248N44O45S7
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Color White to off-white
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Sequence
Glu-Gly-Glu-Cys-Gly-Gly-Phe-Trp-Trp-Lys-Cys-Gly-Ser-Gly-Lys-Pro-Ala-Cys-Cys-Pro-Lys-Tyr-Val-Cys-Ser-Pro-Lys-Trp-Gly-Leu-Cys-Asn-Phe-Pro-Met-Pro (Disulfide bridge:Cys4-Cys19;Cys11-Cys24;Cys18-Cys31)
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Sequence Shortening
EGECGGFWWKCGSGKPACCPKYVCSPKWGLCNFPMP (Disulfide bridge:Cys4-Cys19;Cys11-Cys24;Cys18-Cys31)
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
H2O : ≥ 1 mg/mL (0.25 mM)
* "≥" means soluble, but saturation unknown.
Reinheit & Dokumentation
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Data Sheet (294 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Hönigsperger C, et al. Physiological roles of Kv2 channels in entorhinal cortex layer II stellate cells revealed by Guangxitoxin-1E. J Physiol. 2017 Feb 1;595(3):739-757. [Content Brief]
[2]. Herrington J, et al. Blockers of the delayed-rectifier potassium current in pancreatic beta-cells enhance glucose-dependent insulin secretion. Diabetes. 2006 Apr;55(4):1034-42. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Guangxitoxin 1E Related Classifications
HY-P1427 Related Classifications
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