MPiN
MPiN is a KV1.3 potassium channel inhibitor. The IC50 values of MPiN for inhibiting Kv1.3 currents are 1.1 μM (at -90 mV) and 0.6 μM (at -35 mV). MPiN exhibits in vivo efficacy in a mouse psoriasis model. MPiN can be used for the research of psoriasis.
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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。
- CAS 番号: 108975-37-7
- 分子式: C17H21NO
- 分子量:255.35
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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
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
1.1 μM
|
Inhibition of human KV1.3 channel currents in HEK293T cells held at -90 mV (predominantly closed state) assessed via whole-cell patch-clamp electrophysiology assay with acute perfusion of MPiN.
Inhibition of human KV1.3 channel currents in HEK293T cells held at -90 mV (predominantly closed state) assessed via whole-cell patch-clamp electrophysiology assay with acute perfusion of MPiN.
|
2026.07.06.736759 |
| HEK-293T | IC50 |
0.6 μM
|
Inhibition of human KV1.3 channel currents in HEK293T cells held at -35 mV (predominantly inactivated state) assessed via whole-cell patch-clamp electrophysiology assay with acute perfusion of MPiN.
Inhibition of human KV1.3 channel currents in HEK293T cells held at -35 mV (predominantly inactivated state) assessed via whole-cell patch-clamp electrophysiology assay with acute perfusion of MPiN.
|
2026.07.06.736759 |
体外実験
MPiN (10 μM) potently and reversibly inhibits human KV1.3 channels expressed in HEK293T cells, with higher inhibitory potency for inactivated channels (IC50 = 0.6 μM) than for closed channels (IC50 = 1.1 μM)[1].
MPiN (10 μM; 5 min) selectively inhibits human KV1.3 channels expressed in HEK293T cells, and acts only after the channels open[1].
MPiN (5-20 μM) allosterically promotes voltage sensor activation of human KV1.3 channels expressed in HEK293T cells, while inhibiting channel currents and inducing a hyperpolarizing shift in the activation curve without altering steady-state inactivation[1].
MPiN binds to a novel extracellular pocket formed by the PP1-PP2 turret loop, pore helix, and outer S5/S6 helices on human KV1.3[1].
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:BALB/c (male, 5-6 weeks old, imiquimod-induced psoriasis model)[1]
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Dosage:25 mg/kg
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Administration:i.p.; once daily for 10 days
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Result:Significantly reduced total Psoriasis Area and Severity Index scores.
Reduced spleen index.
Suppressed serum TNF-α levels.
Attenuated epidermal thickening.
化学情報
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CAS 番号 108975-37-7
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分子量 255.35
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分子式 C17H21NO
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SMILES
OC1=C(CN2CCCCC2C)C3=CC=CC=C3C=C1
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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)