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.
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- CAS 番号: 74504-53-3
- 分子式: C305H472N98O84S6
- 分子量:7048.01
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
Kv1.1 |
Kv1.2 |
Kv1.6 |
体外実験
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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD1 mice (male, 18-24 g)[2]
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Dosage:0.08 nmol/mouse; 0.2 nmol/mouse; 0.21 nmol/mouse; 0.24 nmol/mouse
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Administration:i.c.v.
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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.
化学情報
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CAS 番号 74504-53-3
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分子量 7048.01
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分子式 C305H472N98O84S6
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別名
α-DTX
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配列
{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)
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シーケンスの短縮
{Pyr}-PRRKLCILHRNPGRCYDKIPAFYYNQKKKQCERFDWSGCGGNSNRFKTIEECRRTCIG (disulfide bridge:Cys7-Cys57,Cys16-Cys40,Cys32-Cys53)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)