Stromatoxin 1
Stromatoxin 1 is a peptide potassium channel inhibitor that can be isolated from tarantulas. Stromatoxin 1 selectively inhibits Kv2.1/2.2, Kv4.2, and Kv2.1/6.3 or Kv2.1/9.3 channels, reduces KV and fast-inactivating IA currents, and inhibits peak and persistent K+ currents. Stromatoxin 1 enhances cell excitability through electrophysiological changes such as shortening of afterhyperpolarization and the refractory period, thereby increasing intracellular calcium, promoting glucose-stimulated insulin secretion from rodent β cells/islets, and enhancing contraction of human detrusor smooth muscle. Stromatoxin 1 improves conduction fidelity in uninjured sensory neurons. Stromatoxin 1 can be used in research related to neuropathic pain.
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- CAS. Nr.: 741738-59-0
- Formel: C156H237N49O48S7
- Molecular Weight:3791.31
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
K(V)2.1, K(V)2.2, K(V)4.2, and K(V)2.1/9.3[1]
In Vitro
Stromatoxin 1 has a weak effect on the action potential of human pancreatic β cells, with the peak voltage remaining at -21 mV both in the absence and presence of blockers[4].
Stromatoxin 1 (1 μM; 1 h) does not significantly affect glucose-induced insulin secretion in intact human pancreatic islets[4].
Stromatoxin 1 (100 nM) reduces AHPD50 by 18%, shortens the refractory period, and increases the probability of AP conduction during repetitive stimulation in naïve rat L4/L5 DRG neurons[3].
Stromatoxin 1 selectively inhibits slowly inactivating Kv2.1/2.2-mediated K+ currents in human pancreatic β cells, reducing the sustained current by 45% and the peak current by 15%[4].
Stromatoxin 1 (100 nM; 60 min) depolarizes the resting membrane potential of rat whisker follicle Merkel cells from -48 mV to -40 mV without affecting action potential properties, membrane capacitance, or input resistance[5].
Stromatoxin 1 (100 nM) inhibits voltage step-induced KV currents in freshly isolated human DSM cells at positive voltages (+10 to +30 mV)[6].
Stromatoxin 1 (100 nM; 20 min) increases intracellular Ca2+ levels in freshly isolated human DSM cells[6].
Stromatoxin 1 (100 nM; 10 min) increases the amplitude and force of spontaneous phasic contractions in isolated human DSM strips without significantly altering contraction frequency, duration, or muscle tone[6].
Stromatoxin 1 (100 nM; 30 min) enhances EFS-induced contractions in human DSM isolated strips across the 3.5-30 Hz stimulation range[6].
Stromatoxin 1 (100 nM) inhibits a component of whole-cell Kv currents in guinea pig DSM cells and alters activation kinetics, and the ScTx1-sensitive current exhibits biophysical properties consistent with Kv2.1-containing channels[7].
Stromatoxin 1 (100 nM; 10 min) does not change the resting membrane potential of guinea pig DSM cells[7].
Stromatoxin 1 (100 nM) increases spontaneous and EFS-induced contractions of guinea pig DSM strips, has only a slight effect on the amplitude of carbachol-induced phasic contractions, and has no effect on KCl-induced contractions[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 741738-59-0
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Molecular Weight 3791.31
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Formel C156H237N49O48S7
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Sequence
Asp-Cys-Thr-Arg-Met-Phe-Gly-Ala-Cys-Arg-Arg-Asp-Ser-Asp-Cys-Cys-Pro-His-Leu-Gly-Cys-Lys-Pro-Thr-Ser-Lys-Tyr-Cys-Ala-Trp-Asp-Gly-Thr-Ile-NH2 (Disulfide bridge: Cys2-Cys16, Cys9-Cys21, Cys15-Cys28)
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Sequence Shortening
DCTRMFGACRRDSDCCPHLGCKPTSKYCAWDGTI-NH2 (Disulfide bridge: Cys2-Cys16, Cys9-Cys21, Cys15-Cys28)
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)