2. Autophagy
  3. LRRK2
  4. LRRK2-IN-14

LRRK2-IN-14 (Compound 8) 是一种口服有效的 LRRK2 抑制剂。LRRK2-IN-14 对 LRRK2 (G2019S) 细胞活性影响的 IC50 为 6.3 nM。LRRK2-IN-14 对 hERG 有抑制效果 (IC50 = 22 μM)。具有血脑屏障穿透性。

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LRRK2-IN-14 Chemical Structure

LRRK2-IN-14 Chemical Structure

CAS No. : 2942328-06-3

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LRRK2-IN-14 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

LRRK2-IN-14 (Compound 8) is an orally active LRRK2 inhibitor. LRRK2-IN-14 has an IC50 of 6.3 nM for LRRK2(G2019S) cell activity.LRRK2-IN-14 has an inhibitory effect on hERG (IC50=22 μM). LRRK2-IN-14 has blood-brain barrier permeability[1].

体外研究
(In Vitro)

LRRK2-IN-14 (1 μM; 30 min) 在肝微粒体中的代谢稳定性较高 (79.3%)[1]。

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

LRRK2-IN-14 相关抗体:
体内研究
(In Vivo)

LRRK2-IN-14 (30 mg/kg; p.o.; single dose) 在 ICR 小鼠中抑制了大脑中 G2019S 突变的 LRRK2 的磷酸化[1]。


在 ICR 小鼠中的药代动力学分析[1]

Route Dose (mg/kg) C0 (ng/mL) Cmax (ng/mL) Tmax (h) t1/2 (h) Vdss (mL/kg) Clobs (mL/min/kg) AUC0-last (ng·h/mL) AUC0-INF (ng·h/mL) MRT0-INF (h) F (%)
i.v. 5 4101 / / 0.905 1233 16.3 5122 5181 1.27 /
p.o. 5 / 2803 0.083 0.709 / / 3657 3672 1.22 70.9
brain 5 / 837 0.292 0.648 / / 1230 1233 1.14 /

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

Animal Model: ICR mice[1]
Dosage: 30 mg/kg
Administration: p.o.; single dose
Result: Reduced phosphorylated LRRK2 levels to 34%.
分子量

381.35

Formula

C17H18F3N5O2
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

LRRK2-IN-14 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

LRRK2-IN-142942328-06-3LRRK2Leucine-rich repeat kinase 2ICR miceNeurological DiseaseInhibitorinhibitorinhibit

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