1. Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  2. Potassium Channel Cytochrome P450
  3. ML252

ML252 是钾离子通道 (potassium channel) 的选择性抑制剂,靶向 KCNQ2 (Kv7.2. IC50=69 nM). ML252 也抑制细胞色素 Cytochrome P450IC50 分别为 6.1 nM (CYP1A2),18.9 nM (CYP2C9),3.9 nM (CYP3A4),19.9 nM (CYP2D6)。

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ML252 Chemical Structure

ML252 Chemical Structure

CAS No. : 1392494-64-2

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规格 价格 是否有货 数量
5 mg ¥1999
3 - 4 周
10 mg ¥3197
3 - 4 周
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  • 生物活性

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生物活性

ML252 is a selective inhibitor of potassium channel, targeting to KCNQ2 channel (Kv7.2) (IC50=69 nM). ML252 also inhibits Cytochrome P450 with IC50s of 6.1 nM (CYP1A2), 18.9 nM (CYP2C9), 3.9 nM (CYP3A4), 19.9 nM (CYP2D6), respectively[1][2].

IC50 & Target[1][2]

CYP1A2

6.1 μM (IC50)

CYP2C9

18.9 μM (IC50)

CYP2D6

19.9 μM (IC50)

CYP3A4

3.9 μM (IC50)

体外研究
(In Vitro)

ML252 (1 μM;0-48 h) 在大鼠肝脏小体中的内在清除率和随后预测的肝脏清除率分别为 1720 mL/min/kg 和 67.3 mL/min/kg[1]
ML252 (0.1-0 μM) 在 0.3 μM 开始抑制 CHO-KCNQ2 细胞系的 KCNQ2 电流,在 1 μM 时,完全抑制电流[1]
ML252 (30 μM; 48 h) 对 CHO 细胞无急性毒性[1]

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

体内研究
(In Vivo)

ML252 具有不适合口服的代谢稳定性[2]
ML252 (10 mg/kg,3 mg/mL;腹腔注射;单剂量;1 h 后测定) 在大鼠模型中的 B:P 比值为1.9,大脑绝对水平为 672 nM[1]

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

分子量

308.42

Formula

C20H24N2O

CAS 号
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 *
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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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ML252
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HY-18063
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