α-Dendrotoxin  (Synonyms: α-DTX)

α-Dendrotoxin (α-DTX) is a voltage-gated K⁺ channel blocker and an acid-sensing ion channel (ASIC) inhibitor. α-Dendrotoxin blocks K_v1.1, K_v1.2, K_v1.6 and D-type (I_D) 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^[1][2][3].

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.

α-Dendrotoxin (0.08-0.24 nmol/mouse; i.c.v.) induces dose-dependent tonic-clonic seizures in CD1 mice, with a CD₉₇ of 0.21 nmol/mouse for hindlimb tonic extension^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

7048.01

C₃₀₅H₄₇₂N₉₈O₈₄S₆

74504-53-3

{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)

{Pyr}-PRRKLCILHRNPGRCYDKIPAFYYNQKKKQCERFDWSGCGGNSNRFKTIEECRRTCIG (disulfide bridge:Cys7-Cys57,Cys16-Cys40,Cys32-Cys53)

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• [1]. Báez A, et al. α-Dendrotoxin inhibits the ASIC current in dorsal root ganglion neurons from rat. Neurosci Lett. 2015;606:42-47.

  [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.

  [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]