2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. CVN417

CVN417 是一种口服有效、含有 α6 亚基的 nAChR 拮抗剂，以脉冲依赖的方式调节阶段性多巴胺能神经传递。CVN417 对 nAChR 亚基介导的 Ca(2+) 流出具有抑制作用，IC50s 分别为 0.086 μM (α6)，2.56 μM (α3)，0.657 μM (α4)。CVN417 在啮齿类动物模型中减弱静息震颤，显示出改善帕金森病等疾病运动功能障碍的潜力。

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CVN417 Chemical Structure

CVN417 Chemical Structure

CAS No. : 2919851-73-1

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CVN417 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease[1].

IC50 & Target

IC50: 0.086 μM (nAChR α6), 2.56 μM (nAChR α3), 0.657 μM (nAChR α4)[1]
体外研究
(In Vitro)

CVN417 (10 μM; 0-2 h) 在人肝微粒或肝细胞中表现出较低的代谢周转特性[1]。

CVN417 的体外 ADME 数据[1]

human rat mouse dog
liver microsomes Clint (μL/min/mg) 2.8 31.2 33.3 27.7
hepatocytes (mL/min/106 cells) 3.7 20.8 25.1 32.3

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

CVN417 相关抗体:
体内研究
(In Vivo)

CVN417 (3 mg/kg, 10 mg/kg, 25 mg/kg; 口服) 大鼠震颤模型中震颤下颌运动持续时间呈剂量依赖性减少[1]。

在大鼠中对 CVN417 的药代动力学分析[1]

Route Dose (mg/kg) Cl (mL/min/kg) Vdss (L/kg) AUC0-∞ (ng·h/mL) Cmax (μM) F (%) T1/2 (h) Cbrain,total (2 h) Kp, Kpu/u
i.v. 0.5 38.2 12.3 205
p.o. 10 0.35 775 11 5.9 1.82 4.1, 1.4

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

362.85

Formula

C18H23ClN4O2
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

CVN417 相关分类

  • 摩尔计算器

  • 稀释计算器

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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.

Keywords:

CVN4172919851-73-1CVN 417CVN-417nAChRNicotinic acetylcholine receptorsInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-149483
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