α-Dendrotoxin
α-Dendrotoxin (α-DTX) is a voltage-gated K+ channel blocker and an acid-sensing ion channel (ASIC) inhibitor. α-Dendrotoxin blocks Kv1.1, Kv1.2, Kv1.6 and D-type (ID) voltage-gated K+ channels, and reversibly inhibits slowly inactivating potassium currents. α-Dendrotoxin induces epilepsy-related behaviors in mice. α-Dendrotoxin can be used in studies related to tonic-clonic seizures.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 74504-53-3
- Formel: C305H472N98O84S6
- Molecular Weight:7048.01
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
Kv1.1 |
Kv1.2 |
Kv1.6 |
In Vitro
α-Dendrotoxin (0.1-10 μM; 25 s sustained application, 0.1-3 μM; 5 s co-application, 30-100 nM; sustained application for outward current inhibition, 100 nM-1 μM; co-application for outward current inhibition) reversibly inhibits acid-sensing ion channel (ASIC) peak currents in cultured rat dorsal root ganglion neurons with an IC50 of 0.8 μM when applied in a sustained manner, and abolishes post-acid pulse transient outward currents in these neurons at nanomolar to micromolar concentrations, while co-application with acid has no effect on ASIC currents[1].
α-Dendrotoxin (1-2 µM) increases excitability of large layer 5 pyramidal neurons from rat neocortex by hyperpolarizing the action potential firing threshold by 4-8 mV and reducing the threshold current for action potential initiation by 46%, without altering action potential half-width[3].
α-Dendrotoxin (2 µM) inhibits 6% of the total slow potassium current in nucleated outside-out patches from somata of large layer 5 pyramidal neurons from rat neocortex[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:CD1 mice (male, 18-24 g)[2]
-
Dosage:0.08 nmol/mouse; 0.2 nmol/mouse; 0.21 nmol/mouse; 0.24 nmol/mouse
-
Administration:i.c.v.
-
Result:Elicited compulsive grooming, jaw opening, forelimb and hindlimb myoclonus, Straub tail, and opisthotonus.
Induced wild running, falling down, hindlimb myoclonus, hindlimb tonic extension, and frequent death in most mice at 0.2 and 0.24 nmol/mouse.
Reached a CD97 (dose inducing tonic extension in 97% of mice) of 0.21 nmol/mouse.
Caused tonic-clonic seizures in all mice treated with 0.21 nmol/mouse, and killed 9 out of 10 mice following tonic extension.
Chemical Information
-
CAS. Nr. 74504-53-3
-
Molecular Weight 7048.01
-
Formel C305H472N98O84S6
-
Synonyms
α-DTX
-
Sequence
{Pyr}-Pro-Arg-Arg-Lys-Leu-Cys-Ile-Leu-His-Arg-Asn-Pro-Gly-Arg-Cys-Tyr-Asp-Lys-Ile-Pro-Ala-Phe-Tyr-Tyr-Asn-Gln-Lys-Lys-Lys-Gln-Cys-Glu-Arg-Phe-Asp-Trp-Ser-Gly-Cys-Gly-Gly-Asn-Ser-Asn-Arg-Phe-Lys-Thr-Ile-Glu-Glu-Cys-Arg-Arg-Thr-Cys-Ile-Gly (disulfide bridge:Cys7-Cys57,Cys16-Cys40,Cys32-Cys53)
-
Sequence Shortening
{Pyr}-PRRKLCILHRNPGRCYDKIPAFYYNQKKKQCERFDWSGCGGNSNRFKTIEECRRTCIG (disulfide bridge:Cys7-Cys57,Cys16-Cys40,Cys32-Cys53)
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
-
Two-electrode voltage clamp in Xenopus oocytes
Two-electrode voltage clamp measures whole-oocyte membrane current from Xenopus oocytes expressing exogenous ion channels, receptors, or transporters; one intracellular microelectrode senses membrane voltage, and the second injects current so the amplifier can hold the membrane at command voltages while recording the compensating current as the functional readout. The method is suited to Xenopus oocytes because their large size supports microinjection and intracellular electrode impalement, but the large membrane area can limit voltage-clamp speed and accuracy, especially for large or fast currents.
Reinheit & Dokumentation
Verweise
[1]. Báez A, et al. α-Dendrotoxin inhibits the ASIC current in dorsal root ganglion neurons from rat. Neurosci Lett. 2015;606:42-47. [Content Brief]
[2]. Fischer W, et al. Anticonvulsant profile of flunarizine and relation to Na(+) channel blocking effects. Basic Clin Pharmacol Toxicol. 2004 Feb;94(2):79-88. [Content Brief]
[3]. Bekkers JM, et al. Modulation of excitability by alpha-dendrotoxin-sensitive potassium channels in neocortical pyramidal neurons. J Neurosci. 2001;21(17):6553-6560. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)