1. Anti-infection
    Epigenetics
  2. Parasite
    Histone Methyltransferase
  3. Amodiaquine

Amodiaquine (Synonyms: Amodiaquin)

目录号: HY-B1322A
产品使用指南

Amodiaquine (Amodiaquin) 是一种4-氨基喹啉类抗疟剂,是一种有效的具有口服活性的组胺 N-甲基转移酶 (histamine N-methyltransferase) 抑制剂。Amodiaquine 也是一种 Nurr1 激动剂,可特异性结合 Nurr1 的配体结合域,EC50 为 ~20 μM。抗炎作用。

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Amodiaquine Chemical Structure

Amodiaquine Chemical Structure

CAS No. : 86-42-0

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Description

Amodiaquine (Amodiaquin), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect[1][2][3][4].

IC50 & Target

EC50: ~20 μM (Nurr1-LBD (ligand binding domain))[1]
Histamine N-methyltransferase[3]

In Vitro

Amodiaquine (10-20 μM; 4 hours) treatment suppresses LPS-induced expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α and iNOS) in a dose-dependent manner[1].
Amodiaquine (5 μM; 24 hours) significantly inhibits neurotoxin (6-OHDA-induced cell death in primary dopamine cells as examined by the number of TH+ neurons and dopamine uptake. The neuroprotective effect of Amodiaquine is also observed in rat PC12 cells[1].

RT-PCR[1]

Cell Line: Primary microglia
Concentration: 10 µM, 15 µM, 20 µM
Incubation Time: 4 hours
Result: Suppressed LPS-induced expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α and iNOS) in a dose-dependent manner.
In Vivo

Amodiaquine (40 mg/kg; intraperitoneal injection; daily; for 3 days; male ICR mice) treatment diminishes perihematomal activation of microglia/macrophages and astrocytes. Amodiaquine also suppresses ICH-induced mRNA expression of IL-1β, CCL2 and CXCL2, and ameliorated motor dysfunction of mice[2].

Animal Model: Male ICR mice (8-10 weeks of age) induced ntracerebral hemorrhage (ICH)[2]
Dosage: 40 mg/kg
Administration: Intraperitoneal injection; daily; for 3 days
Result: Diminished perihematomal activation of microglia/macrophages and astrocytes.
Molecular Weight

355.86

Formula

C₂₀H₂₂ClN₃O

CAS No.

86-42-0

中文名称

阿莫地喹

SMILES

OC1=CC=C(NC2=CC=NC3=CC(Cl)=CC=C23)C=C1CN(CC)CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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  • 稀释计算器

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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:

AmodiaquineAmodiaquinParasiteHistone MethyltransferaseNurr1antimalarialneuroprotectiveIL-1βCCL2CXCL2anti-inflammatoryN-methyltransferaseInhibitorinhibitorinhibit

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