2. Vitamin D Related/Nuclear Receptor Anti-infection Epigenetics
  3. Nuclear Hormone Receptor 4A/NR4A Parasite Histone Methyltransferase
  4. Amodiaquine

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.

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Amodiaquine

Amodiaquine Chemical Structure

CAS No. : 86-42-0

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Based on 11 publication(s) in Google Scholar

Other Forms of Amodiaquine:

Amodiaquine Related Antibodies

Top Publications Citing Use of Products

Voir tous les produits spécifiques à Isoform Nuclear Hormone Receptor 4A/NR4A:

Voir toutes les isoformes
Nur77/NR4A1 Nurr1/NR4A2

Voir tous les produits spécifiques à Isoform Parasite:

Voir toutes les isoformes
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

Voir tous les produits spécifiques à Isoform Histone Methyltransferase:

Voir toutes les isoformes
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 NSD3/WHSC1L1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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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

Plasmodium

 

Nurr1/NR4A2

 

Cellular Effect
Cell Line Type Value Description References
BHK-21 CC50
52.09 μM
Compound: Amodiaquine
Cytotoxicity against BHK21 cells after 24 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against BHK21 cells after 24 hrs by CellTiter-Glo luminescent assay
[PMID: 26771861]
CHO IC50
147.157 μM
Compound: Amodiaquine
Cytotoxicity against CHO cells by MTT assay
Cytotoxicity against CHO cells by MTT assay
[PMID: 26264839]
SH-SY5Y CC50
10 μM
Compound: AQ
Cytotoxicity against human SH-SY5Y cells after 72 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells after 72 hrs by MTT assay
[PMID: 29559198]
Vero CC50
>50 μM
Compound: Amodiaquine
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
10.1101/2020.03.20.999730
Vero EC50
2.8 μM
Compound: Amodiaquine
Antiviral activity against Zika virus PLCal_ZV infected in African green monkey Vero cells assessed as reduction in viral titer after 1 hr by plaque assay
Antiviral activity against Zika virus PLCal_ZV infected in African green monkey Vero cells assessed as reduction in viral titer after 1 hr by plaque assay
[PMID: 31549836]
Vero IC50
5.15 μM
Compound: Amodiaquine
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
10.1101/2020.03.20.999730
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].

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

Amodiaquine Related Antibodies

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].

MedChemExpress (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.
Essai clinique
Masse moléculaire

355.86

Formule

C20H22ClN3O
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : 66.67 mg/mL (187.35 mM; ultrasonic and adjust pH to 3 with 1M HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8101 mL 14.0505 mL 28.1009 mL
5 mM 0.5620 mL 2.8101 mL 5.6202 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureté et documentation
Références

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8101 mL 14.0505 mL 28.1009 mL 70.2523 mL
5 mM 0.5620 mL 2.8101 mL 5.6202 mL 14.0505 mL
10 mM 0.2810 mL 1.4050 mL 2.8101 mL 7.0252 mL
15 mM 0.1873 mL 0.9367 mL 1.8734 mL 4.6835 mL
20 mM 0.1405 mL 0.7025 mL 1.4050 mL 3.5126 mL
25 mM 0.1124 mL 0.5620 mL 1.1240 mL 2.8101 mL
30 mM 0.0937 mL 0.4683 mL 0.9367 mL 2.3417 mL
40 mM 0.0703 mL 0.3513 mL 0.7025 mL 1.7563 mL
50 mM 0.0562 mL 0.2810 mL 0.5620 mL 1.4050 mL
60 mM 0.0468 mL 0.2342 mL 0.4683 mL 1.1709 mL
80 mM 0.0351 mL 0.1756 mL 0.3513 mL 0.8782 mL
100 mM 0.0281 mL 0.1405 mL 0.2810 mL 0.7025 mL
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Amodiaquine Related Classifications

Help & FAQs
  • 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:

Amodiaquine86-42-0AmodiaquinNuclear Hormone Receptor 4A/NR4AParasiteHistone MethyltransferaseNuclear Hormone Receptor 4ANerve Growth Factor IB-like ReceptorNurr1antimalarialneuroprotectiveIL-1βCCL2CXCL2anti-inflammatoryN-methyltransferaseInhibitorinhibitorinhibit

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