1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. Kv7.2/Kv7.3 activator-2

Kv7.2/Kv7.3 activator-2 是一种可穿透血脑屏障的 Kv7.2/7.3 激活剂 (EC50: 0.25 μM)。Kv7.2/Kv7.3 activator-2 具有良好的光稳定性。Kv7.2/Kv7.3 activator-2 在最大电休克 (MES) 和 sc-戊四氮 (sc-PTZ) 诱发的小鼠急性癫痫模型中具有强效的抗癫痫作用。

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Kv7.2/Kv7.3 activator-2 Chemical Structure

Kv7.2/Kv7.3 activator-2 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Kv7.2/Kv7.3 activator-2 is a BBB-penetrable Kv7.2/7.3 activator (EC50: 0.25 μM). Kv7.2/Kv7.3 activator-2 has good photostability. Kv7.2/Kv7.3 activator-2 has potently antiepileptic effects in maximal electroshock (MES) and sc-pentylenetetrazol (sc-PTZ)-induced acute mice seizure models[1].

IC50 & Target

KCNQ2/Q3

0.25 μM (EC50)

体外研究
(In Vitro)

Kv7.2/Kv7.3 activator-2 (Compound 2c) (10 μM) 的激活效率比 Retigabine (RTG) 高 20%[1]
Kv7.2/Kv7.3 activator-2 (10 μM) 与阳性 Kv7.1 激活剂 ML277 (HY-12343) 相比,对心脏 Kv7.1 通道的影响不明显[1]
Kv7.2/Kv7.3 activator-2 (10 μM) 与 Kv7.2 的 PD 位点结合,关键残基 (W236、F305 和 L299) 在 Kv7.2 通道的激活中起着至关重要的作用[1]
Kv7.2/Kv7.3 activator-2 在预定时间间隔 (0-12 小时) 内经过 254 nm 和 365 nm 的波长照射,其光稳定性优于 RTG[1]

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

药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Mice 30 mg/kg i.v. AUC0-∞ 7922.2 ng·h/mL
Mice 30 mg/kg p.o. AUC0-∞ 3879.5 ng·h/mL
Mice 30 mg/kg i.v. AUC0-t 7905.7 ng·h/mL
Mice 30 mg/kg p.o. AUC0-t 3854.7 ng·h/mL
Mice 30 mg/kg i.v. Cmax 19300 ng/mL
Mice 30 mg/kg p.o. Cmax 4840 ng/mL
Mice 30 mg/kg i.v. CL 63.11 mL/min/kg
Mice 30 mg/kg p.o. CL 123.9 mL/min/kg
Mice 30 mg/kg i.v. MRT0-∞ 0.4 hr
Mice 30 mg/kg p.o. MRT0-∞ 1.2 hr
Mice 30 mg/kg i.v. T1/2 1.97 hr
Mice 30 mg/kg p.o. T1/2 1.00 hr
Mice 30 mg/kg i.v. Tmax 0.083 hr
Mice 30 mg/kg p.o. Tmax 0.100 hr
Mice 30 mg/kg i.v. B/P 0.23 (4h) %
Mice 30 mg/kg p.o. B/P 0.52 (4h) %
Mice 30 mg/kg i.v. B/P 0.56 (2h) %
Mice 30 mg/kg p.o. B/P 0.58 (2h) %
Mice 30 mg/kg i.v. Vz 10.74 L/kg
Mice 30 mg/kg p.o. F 49 %
Mice 30 mg/kg p.o. Vz 10.96 L/kg
体内研究
(In Vivo)

Kv7.2/Kv7.3 activator-2 (Compound 2c) (1-100 mg/kg, 腹腔注射) 对最大剂量电休克 (MES) 诱发的小鼠急性癫痫模型具有剂量依赖性保护作用,ED50 为 4.02 mg/kg,在 100 mg/kg 剂量下保护率达到 100%[1]
Kv7.2/Kv7.3 activator-2 (1-100 mg/kg, 腹腔注射) 以剂量依赖性方式降低 sc-戊四氮 (sc-PTZ) 诱发的最大行为癫痫发作评分,ED50 为 43.17 mg/kg,在 10 mg/kg 剂量下小鼠存活率提高[1]
Kv7.2/Kv7.3 activator-2 (10-50 mg/kg,腹腔注射) 以剂量依赖性方式影响小鼠的运动,小鼠在 50 mg/kg 剂量下表现出运动功能障碍[1]
Kv7.2/Kv7.3 activator-2 (100-679 mg/kg,口服) 对 KM 小鼠的抗癫痫作用具有安全的急性毒性,其 LD50为340.35 mg/kg[1]

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

Animal Model: MES-induced acute seizure KM mice (6 weeks) model
Dosage: 1, 3, 10, 30, 100 mg/kg
Administration: i.p., 30 min before electrically stimulation, and then mice were electrically stimulated and observed their seizure behavior.
Result: Dose-dependently protected against MES-induced acute mice seizure models with an ED50 of 4.02 mg/kg, and protects 100% at 100 mg/kg dose.
Animal Model: sc-PTZ (100 mg/kg, i.p.)- induced acute seizure KM mice (6 weeks) model
Dosage: 1, 3, 10, 30, 50, 100 mg/kg
Administration: i.p., 30 min before sc-PTZ injection, and then recorded. maximum seizure score and measured the latency to generalized tonic-clonic seizures within 30 min.
Result: Dose-dependently reduced sc-PTZ -induced maximal behavioral seizure scores with an ED50 of 43.17 mg/kg, and the survival rate of mice increases at 10 mg/kg dose.
Animal Model: KM mice (6 weeks)
Dosage: 100, 132, 174, 229, 303, 400, 528, and 679 mg/kg
Administration: p.o., and then recorded the health status and mortality of the mice for 14 days post-administration.
Result: had a safe therapeutic window of acute toxicity for antiepileptic effects with an LD50 of 340.35 mg/kg.
分子量

300.42

Formula

C17H20N2OS

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
Kv7.2/Kv7.3 activator-2
目录号:
HY-172887
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