2. Neuronal Signaling
  3. AAK1
  4. AAK1-IN-5

AAK1-IN-5 是一种具有高选择性、可透过血脑屏障以及口服活性的接头蛋白2相关激酶1 (adaptor protein-2-associated kinase 1, AAK1) 抑制剂 (AAK1 IC50=1.2 nM, Filt Ki=0.05 nM, cell IC50=0.5 nM)。AAK1-IN-5 具有研究神经性疼痛的潜力。

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AAK1-IN-5 Chemical Structure

AAK1-IN-5 Chemical Structure

CAS No. : 1815613-44-5

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AAK1-IN-5 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

AAK1-IN-5 is a highly selective, CNS-penetrable, and orally active adaptor protein-2-associated kinase 1 (AAK1) inhibitor (AAK1 IC50 of 1.2 nM, Filt Ki of 0.05 nM, and cell IC50 of 0.5 nM). AAK1-IN-4 has the potential for the research for neuropathic pain[1].

IC50 & Target

IC50: 1.2 nM (AAK1)[1].
Ki: 0.05 nM (AAK1)[1]
体外研究
(In Vitro)

AAK1-IN-5 (compound 58) (0.5 μM, 0-10 min) has a good metabolic stability, with half-life values of over 120 min in human and mouse liver microsomes, and 76.0, 17.6, 26.0 min in rat, cynomolgus monkey, and dog, respectively[1].

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

AAK1-IN-5 相关抗体:
体内研究
(In Vivo)

AAK1-IN-5 (compound 58) can reduce hyperalgesia in SD rats (chronic constriction injury) efficiently with good efficacy observed at doses of 1 and 3 mg/kg[1].

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

Animal Model: Male Sprague-Dawley rats (chronic constriction injury, CCI)[1]
Dosage: 1-3 mg/kg
Administration: p.o., 0-5.5 hours
Result: Reduced hyperalgesia in CCI rats efficiently with good efficacy observed at doses of 1 and 3 mg/kg.
分子量

385.40

Formula

C19H23F4N3O
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

AAK1-IN-5 相关分类

  • 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.

Keywords:

AAK1-IN-51815613-44-5AAK1Adaptor-associated Kinase 1AP2-associated kinase 1PeptidesProteinsNeurophysiologySelectivityCNSOralNeuropathic PainInhibitorinhibitorinhibit

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