Amodiaquine
Based on 12 publication(s) in Google Scholar
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.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.62%
- CAS No.: 86-42-0
- Formule: C20H22ClN3O
- Masse moléculaire:355.86
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Amodiaquine
More- Adv Sci (Weinh). 2026 Jan 26:e15009. [Abstract]
- Pharmacol Res. 2023 May:191:106717. [Abstract]
- BMC Chem. 2025 Jan 30;19(1):28. [Abstract]
- Bioorg Chem. 2024 Jun:147:107412. [Abstract]
- Cell Signal. 2025 Jul:131:111706. [Abstract]
- J Virol. 2024 Feb 20;98(2):e0121623. [Abstract]
- Metab Brain Dis. 2021 Apr;36(4):609-625. [Abstract]
- Biochem Biophys Res Commun. 2020 Feb 19;522(4):862-868. [Abstract]
- Biol Pharm Bull. 2022 Apr 1;45(4):438-445. [Abstract]
- Cell Press Blue. 2026 Apr 22.
- Research Square Print. September 20th, 2022.
- Oxid Med Cell Longev. 2021 Feb 10.
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Bio/Physico-chemical Assay
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Flow Cytometry
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Flow Cytometry
Voir tous les produits spécifiques à Isoform Nuclear Hormone Receptor 4A/NR4A
MoreVoir tous les produits spécifiques à Isoform Parasite
MoreVoir tous les produits spécifiques à Isoform Histone Methyltransferase
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Activité biologique
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Plasmodium |
Nurr1/NR4A2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BHK-21 | CC50 |
52.09 μM
Compound: Amodiaquine
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Cytotoxicity against BHK21 cells after 24 hrs by CellTiter-Glo luminescent assay
Cytotoxicity against BHK21 cells after 24 hrs by CellTiter-Glo luminescent assay
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[PMID: 26771861] |
| CHO | IC50 |
147.157 μM
Compound: Amodiaquine
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Cytotoxicity against CHO cells by MTT assay
Cytotoxicity against CHO cells by MTT assay
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[PMID: 26264839] |
| SH-SY5Y | CC50 |
10 μM
Compound: AQ
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Cytotoxicity against human SH-SY5Y cells after 72 hrs by MTT assay
Cytotoxicity against human SH-SY5Y cells after 72 hrs by MTT assay
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[PMID: 29559198] |
| Vero | CC50 |
>50 μM
Compound: Amodiaquine
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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
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10.1101/2020.03.20.999730 |
| Vero | EC50 |
2.8 μM
Compound: Amodiaquine
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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
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[PMID: 31549836] |
| Vero | IC50 |
5.15 μM
Compound: Amodiaquine
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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
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10.1101/2020.03.20.999730 |
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.
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Cell Line:Primary microglia
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Concentration:10 µM, 15 µM, 20 µM
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Incubation Time:4 hours
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Result:Suppressed LPS-induced expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α and iNOS) in a dose-dependent manner.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male ICR mice (8-10 weeks of age) induced ntracerebral hemorrhage (ICH)[2]
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Dosage:40 mg/kg
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Administration:Intraperitoneal injection; daily; for 3 days
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Result:Diminished perihematomal activation of microglia/macrophages and astrocytes.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 86-42-0
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Appearance Solid
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Masse moléculaire 355.86
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Formule C20H22ClN3O
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Color White to light yellow
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SMILES
OC1=CC=C(NC2=CC=NC3=CC(Cl)=CC=C23)C=C1CN(CC)CC
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Synonyms
Amodiaquin
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (12)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Amodiaquine Enhances Anti-Melanoma Efficacy of Attenuated Salmonella via Targeting Glutathione Reductase in Neutrophils. [Abstract]2026 Jan 26:e15009. PMID: 41588921
Amodiaquine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jan 26:e15009. [Abstract]
IC50 values of AQ (Amodiaquine) for neutrophils.
Amodiaquine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jan 26:e15009. [Abstract]
Effects of AQ (Amodiaquine, 100 mg/kg per mouse, 100 µL per mouse, daily, ip) on neutrophil phagocytosis of VNP-RFP in vitro and in vivo.
Amodiaquine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jan 26:e15009. [Abstract]
Tumor growth curve after VNP combined with AQ (Amodiaquine) treatment.
Amodiaquine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jan 26:e15009. [Abstract]
Distribution of VNP in the mouse heart, liver, spleen, lung, kidney, and tumor after combined treatment with VNP and AQ (Amodiaquine). The dilution ratio of the tissue homogenate is indicated in the corresponding panel.
Amodiaquine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jan 26:e15009. [Abstract]
Changes in the proportion of neutrophils among immune cells in the blood of mice following treatment with VNP combined with AQ (Amodiaquine).
Amodiaquine purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Jan 26:e15009. [Abstract]
The effect of high concentrations of AQ (Amodiaquine, 800 μM) on the interaction between target proteins and AQ (Amodiaquine)-P (20 μM).
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Pharmacol Res
Protective effect of Nr4a2 (Nurr1) against LPS-induced depressive-like behaviors via regulating activity of microglia and CamkII neurons in anterior cingulate cortex. [Abstract]2023 May:191:106717. PMID: 36948326 -
BMC Chem
Development and experimental validation of a machine learning model for the prediction of new antimalarials. [Abstract]2025 Jan 30;19(1):28. PMID: 39885590 -
Bioorg Chem
Identification of FTY720 and COH29 as novel topoisomerase I catalytic inhibitors by experimental and computational studies. [Abstract]2024 Jun:147:107412. PMID: 38696845 -
Cell Signal
Paeoniflorin-6'-O-benzene sulfonate inhibits keratinocyte proliferation by restoring GRK2-JAK1 colocalization in mouse model of psoriasis. [Abstract]2025 Jul:131:111706. PMID: 40037425 -
J Virol
2024 Feb 20;98(2):e0121623. PMID: 38236006 -
Metab Brain Dis
The orphan nuclear receptor Nurr1 agonist amodiaquine mediates neuroprotective effects in 6-OHDA Parkinson's disease animal model by enhancing the phosphorylation of P38 mitogen-activated kinase but not PI3K/AKT signaling pathway. [Abstract]2021 Apr;36(4):609-625. PMID: 33507465 -
Biochem Biophys Res Commun
Combinatorial screening of a panel of FDA-approved drugs identifies several candidates with anti-Ebola activities. [Abstract]2020 Feb 19;522(4):862-868. PMID: 31806372 -
Biol Pharm Bull
Inhibition of Stearoyl-CoA Desaturase 1 Potentiates Anti-tumor Activity of Amodiaquine in Non-small Cell Lung Cancer. [Abstract]2022 Apr 1;45(4):438-445. PMID: 35110426 -
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Solvant et solubilité
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Chun-Hyung Kim, et al. Nuclear receptor Nurr1 agonists enhance its dual functions and improve behavioral deficits in an animal model of Parkinson's disease. Proc Natl Acad Sci U S A. 2015 Jul 14;112(28):8756-61. [Content Brief]
[2]. Keita Kinoshita, et al. A Nurr1 agonist amodiaquine attenuates inflammatory events and neurological deficits in a mouse model of intracerebral hemorrhage. J Neuroimmunol. 2019 May 15;330:48-54. [Content Brief]
[3]. Akira Yokoyama, et al. Effect of amodiaquine, a histamine N-methyltransferase inhibitor, on, Propionibacterium acnes and lipopolysaccharide-induced hepatitis in mice. Eur J Pharmacol. 2007 Mar 8;558(1-3):179-84. [Content Brief]
[4]. M T HOEKENGA. The treatment of acute malaria with single oral doses of amodiaquin, chloroquine, hydroxychloroquine and pyrimethamine. Am J Trop Med Hyg. 1954 Sep;3(5):833-8. [Content Brief]
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 |