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

Amodiaquine dihydrochloride dihydrate (Synonyms: Amodiaquin dihydrochloride dihydrate)

Cat. No.: HY-B1322 Purity: 99.98%
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Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate 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 dihydrate Chemical Structure

Amodiaquine dihydrochloride dihydrate Chemical Structure

CAS No. : 6398-98-7

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10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
100 mg USD 60 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

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

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].

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

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.
Clinical Trial
Molecular Weight

464.81

Formula

C₂₀H₂₂ClN₃O . ₂H₂O . ₂HCl

CAS No.

6398-98-7

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (215.14 mM; Need ultrasonic)

H2O : 20 mg/mL (43.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1514 mL 10.7571 mL 21.5142 mL
5 mM 0.4303 mL 2.1514 mL 4.3028 mL
10 mM 0.2151 mL 1.0757 mL 2.1514 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: ≥ 2.5 mg/mL (5.38 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

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

Amodiaquine dihydrochloride dihydrateAmodiaquin dihydrochloride dihydrateParasiteHistone MethyltransferaseNurr1antimalarialneuroprotectiveIL-1βCCL2CXCL2anti-inflammatoryN-methyltransferaseInhibitorinhibitorinhibit

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Amodiaquine dihydrochloride dihydrate
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