1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. CVN293

CVN293 是一种选择性的,能够透过血脑屏障的钾离子 (K+) 通道 KCNK13 抑制剂,对 hKCNK13 和 mKCNK13 的 IC50 值分别为 41 nM 和 28 nM。CVN293 有效抑制小胶质细胞中 NLRP3 炎症小体介导的促炎细胞因子 IL-1β 的产生。

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CVN293 Chemical Structure

CVN293 Chemical Structure

CAS No. : 2815296-08-1

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CVN293 is a selective and brain permeable potassium ion (K+) channel KCNK13 inhibtor with IC50s of 41 nM and 28 nM for hKCNK13 and mKCNK13, respectively. CVN293 potently inhibits the NLRP3-inflammasome mediated production of the proinflammatory cytokine IL-1β in microglia[1].

IC50 & Target[1]

hKCNK13

41 nM (IC50)

mKCNK13

28 nM (IC50)

hKCNK6

>30000 nM (IC50)

hKCNK2

>30000 nM (IC50)

体外研究
(In Vitro)

CVN293 (0.05、0.5、5 μM) 对 NLRP3 炎症小体介导的 LPS 引发的小鼠小胶质细胞产生 IL-1β 具有浓度依赖性抑制作用[1]

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

体内研究
(In Vivo)

Pharmacokinetic Parameters of CVN293 in male Sprague-Dawley rat, dog and cynomolgus monkey[1].

IV (0.5 mg/kg; rat) PO (3 mg/kg; rat) IV (1 mg/kg; dog) PO (10 mg/kg; dog) IV (1 mg/kg; cynomolgus monkey) PO (3 mg/kg; cynomolgus monkey)
Tmax (h) 1.0 1.25 1.0
Cmax (ng/mL) 468 241 165
AUC0-∞ (ng•h/mL) 222 1236 438 630 782 546
t1/2 (h) 1.0 2.0 0.5 2.6 1.1 1.9
CLp (mL/min/kg) 35 38 22
Vss (L/kg) 1.85 1.42 1.45
F (%) 87 41 24

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

分子量

311.27

Formula

C14H10FN7O

CAS 号
Unlabeled CAS

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
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  • 稀释计算器

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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)
× = ×
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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:
CVN293
目录号:
HY-158155
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