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.
For research use only. We do not sell to patients.
- CAS No.: 86-42-0
- Formula: C20H22ClN3O
- Molecular Weight:355.86
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Amodiaquine
More- Adv Sci (Weinh). 2026 Jan 26:e15009. [Abstract]
- Pharmacol Res. 2023 May:191:106717. [Abstract]
- Bioorg Chem. 2024 Jun:147:107412. [Abstract]
- BMC Chem. 2025 Jan 30;19(1):28. [Abstract]
- J Virol. 2024 Feb 20;98(2):e0121623. [Abstract]
- Cell Signal. 2025 Jul:131:111706. [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.
All Nuclear Hormone Receptor 4A/NR4A Isoforms
MoreAll Parasite Isoforms
MoreAll Histone Methyltransferase Isoforms
More
Biological Activity
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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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Molecular Weight 355.86
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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 -
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 -
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 -
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 -
J Virol
2024 Feb 20;98(2):e0121623. PMID: 38236006 -
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 -
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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Solvent & Solubility
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)
Purity & Documentation
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Data Sheet (281 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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Handling Instructions (2659 KB)
References
[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 |
Amodiaquine Related Classifications
HY-B1322A Related Classifications
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