Hm1a
Hm1a is a venom peptide and a selective hNaV1.1 activator with an EC50 of 7.5 nM. Hm1a enhances hNaV1.1 and hNaV1.3 channel currents via delayed inactivation. Hm1a restores action potential firing in Dravet syndrome GABAergic inhibitory interneurons, reduces interictal epileptiform discharges and whole-brain hyperexcitability, lowers seizure frequency, and rescues premature death in Dravet syndrome mice. Hm1a can be used for the research of neurological disease, such as Dravet syndrome.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C170H239N47O54S6
- 分子量:3997.39
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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hNav1.1 7.5 nM (EC50) |
hNav1.3 39.5 nM (EC50) |
Hm1a potently and selectively modulates hNaV1.1 and hNaV1.3 channels with efficacy EC50 values of 7.5 and 39.5 nM in HEK293T cells[1].
Hm1a (50 nM; 2 min) has no functional effect on hNaV1.2, hNaV1.4, hNaV1.5, hNaV1.6, hNaV1.7, or hNaV1.8 channels in HEK293T cells[1].
Hm1a (300 nM) has no functional effect on Kv1.7, Kv10.1, Kv11.1, KCa1.1, KCa2.2, or KCa3.1 channels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Hm1a (0.5 μM; continuous ICV infusion; 0.2 μL/min; up to 5 days) reduces seizure frequency to near zero over 4 days and maintains 90% survival at day 3 in Dravet syndrome mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Scn1a (R1407X) Dravet syndrome mice (N2 backcross generation on C57BL/6J background; aged postnatal day 18-26)[1]
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Dosage:0.5 μM
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Administration:ICV infusion; 0.1-0.2 μL/min; 1 h
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Result:Reduced mean interictal spike frequency from 27.6 spikes/h to 11.7 spikes/h.
Achieved a significant reduction in peak 0.5-2 Hz activity via power spectrum analysis.
Induced a spike-free period of ~1 hour following infusion cessation.
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Animal Model:Scn1a (R1407X) Dravet syndrome mice (N2 backcross generation on C57BL/6J background; aged postnatal day 18-26)[1]
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Dosage:0.5 μM
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Administration:continuous ICV infusion; 0.2 μL/min; up to 5 days
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Result:Reduced mean seizure count from 3.50 seizures/day at day 0 to near 0 seizures/day by day 4.
Led 67% of treated mice to have significantly reduced or completely abolished seizures after 3 days.
Maintained 90% survival of treated mice to day 3, compared to 0% survival of vehicle-treated controls.
化学情報
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分子量 3997.39
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分子式 C170H239N47O54S6
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配列
Glu-Cys-Arg-Tyr-Leu-Phe-Gly-Gly-Cys-Ser-Ser-Thr-Ser-Asp-Cys-Cys-Lys-His-Leu-Ser-Cys-Arg-Ser-Asp-Trp-Lys-Tyr-Cys-Ala-Trp-Asp-Gly-Thr-Phe-Ser (Disulfide bridge: Cys2-Cys16; Cys9-Cys21; Cys15-Cys28)
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シーケンスの短縮
ECRYLFGGCSSTSDCCKHLSCRSDWKYCAWDGTFS (Disulfide bridge: Cys2-Cys16; Cys9-Cys21; Cys15-Cys28)
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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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Hm1a 関連分類
HY-P5183 関連分類
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