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

Amodiaquine dihydrochloride (Synonyms: Amodiaquin dihydrochloride)

Cat. No.: HY-B1322B Purity: >98.0%
Handling Instructions

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

For research use only. We do not sell to patients.

Amodiaquine dihydrochloride Chemical Structure

Amodiaquine dihydrochloride Chemical Structure

CAS No. : 69-44-3

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10 mM * 1  mL in DMSO USD 55 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride 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

428.78

Formula

C₂₀H₂₄Cl₃N₃O

CAS No.

69-44-3

SMILES

[H]Cl.[H]Cl.OC1=CC=C(NC2=CC=NC3=CC(Cl)=CC=C23)C=C1CN(CC)CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (291.52 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3322 mL 11.6610 mL 23.3220 mL
5 mM 0.4664 mL 2.3322 mL 4.6644 mL
10 mM 0.2332 mL 1.1661 mL 2.3322 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.85 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AmodiaquineAmodiaquinParasiteHistone MethyltransferaseNurr1antimalarialneuroprotectiveIL-1βCCL2CXCL2anti-inflammatoryN-methyltransferaseInhibitorinhibitorinhibit

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Amodiaquine dihydrochloride
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HY-B1322B
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