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LP-922761 hydrate 

目录号: HY-120179A
产品使用指南

LP-922761 hydrate 是一种有效的,选择性的,具有口服活性的 AAK1 抑制剂,在酶和细胞分析中 IC50 分别为 4.8 nM 和 7.6 nM。LP-922761 hydrate 还抑制 BMP-2 诱导蛋白激酶 (BIKE),IC50 为 24 nM。LP-922761 hydrate 对细胞 GAK,阿片类药物,肾上腺素 α2 或 GABAa 受体无明显活性。

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LP-922761 hydrate Chemical Structure

LP-922761 hydrate Chemical Structure

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Description

LP-922761 hydrate is a potent, selective and orally active adapter protein-2 associated kinase 1 (AAK1) inhibitor with IC50s of 4.8 nM and 7.6 nM in enzyme and cell assays, respectively. LP-922761 hydrate also inhibits BMP-2-inducible protein kinase (BIKE) with an IC50 of 24 nM. LP-922761 hydrate shows less activity at cyclin G-associated kinase (GAK), opioid, adrenergic α2 or GABAa receptors[1].

IC50 & Target

IC50: 4.8 nM (Adapter protein-2 associated kinase 1 (AAK1) in enzyme assays); 7.6 nM (AAK1 in cell assays); 24 nM (BMP-2-inducible protein kinase (BIKE))[1]

In Vivo

In mouse, LP-922761 has a brain to plasma ratio of 0.007, indicating that LP-922761 is essentially restricted to the peripheral compartment[1].

Molecular Weight

414.98

Formula

C₂₁H₂₆N₆O₃.₁/₄H₂O

SMILES

O=C(N(C)CCNC1=NN2C(C=C1)=NC=C2C3=CC=C(C=C3)C(N)=O)OC(C)(C)C.[H]O[H].[1/4]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • 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)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

LP-922761LP922761LP 922761OthersAAK1BIKEperipheralrestrictedpoorlybrain-penetrantInhibitorinhibitorinhibit

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产品名称:
LP-922761 hydrate
目录号:
HY-120179A
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