| Size | Price | Stock | Qty |
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| 100mg |
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| Other Sizes |
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Purity: ≥98%
Amodiaquin hydrochloride (trade names Camoquin, Flavoquine) is a potent and orally bioactive inhibitor of the Ebola virus, acts by targeting the viral protein 35 (VP35). It is also a 4-aminoquinoline class of antimalarial agent and anti-inflammatory agent that inhibits 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. Amodiaquine has been shown to be more effective than chloroquine in treating chloroquine-resistant Plasmodium falciparum malaria infections and may give more protection than chloroquine when used as weekly prophylaxis. Amodiaquine, like chloroquine, is generally well tolerated. Amodiaquine is a histamine N-methyltransferase inhibitor. It is on the World Health Organization's List of Essential Medicines, the most important medications needed in a basic health system.
| ln Vitro |
The expression of LPS-induced pro-inflammatory cytokines (IL-1β, interleukin 6, TNF-α, and iNOS) is inhibited in a dose-regulated manner by amodiaquine dihydrochloride (10–20 μM; 4 hours) administration [1]. μM; 24 hr) markedly reduced the amount of neurotoxic (6-OHDA) that caused cell death in primary dopamine cells, as indicated by the quantity of TH+ neurons and dopamine chow. Amodiaquine was also found to have neuroprotective properties in tea PC12 cells using the use of RT-PCR.
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| ln Vivo |
Amodiaquine (40 mg/kg; intraperitoneal; daily; for 3 days; stable ICR tumors) treatment decreased the peritumor activation of stellate stellate cells and tiny stellate cells/macrophages. Amodiaquine also ameliorates motor impairment in mice and suppresses ICH-induced mRNA expression of IL-1β, CCL2, and CXCL2 [2].
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| Cell Assay |
RT-PCR[1]
Cell Types: primary microglia Tested Concentrations: 10μM, 15μM, 20μM Incubation Duration: 4 hrs (hours) Experimental Results: Inhibition of LPS-induced pro-inflammatory cytokines (IL-1β, interleukin-6, TNF - 1]. α and iNOS) in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Male ICR mice (8-10 weeks old) induced intracerebral hemorrhage (ICH) [2]
Doses: 40 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; lasted for 3 days Experimental Results: Microglia around the hematoma / diminished activation of macrophages and astrocytes. |
| 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.
[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. [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. [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. [5]. John R Horton, et al. Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. J Mol Biol. 2005 Oct 21;353(2):334-344. |
| Additional Infomation |
Amodiaquine Hydrochloride is the hydrochloride salt of amodiaquine, an orally active 4-aminoquinoline derivative with antimalarial and anti-inflammatory properties. Similar in structure and activity to chloroquine, amodiaquine is effective against some chloroquine-resistant strains, particularly Plasmodium falciparum, the most deadly malaria parasite. Although the mechanism of plasmodicidal action has not been fully elucidated, like other quinoline derivatives, amodiaquine likely is able to inhibit heme polymerase activity in the body. This results in accumulation of free heme, which is toxic to the parasites.
A 4-aminoquinoline compound with anti-inflammatory properties. |
| Molecular Formula |
C20H24CL3N3O
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|---|---|
| Molecular Weight |
428.7831
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| Exact Mass |
391.121
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| CAS # |
69-44-3
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| Related CAS # |
Amodiaquine dihydrochloride dihydrate;6398-98-7;Amodiaquine;86-42-0
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| PubChem CID |
6246
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| Appearance |
Light yellow to yellow solid powder
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| Boiling Point |
478ºC at 760 mmHg
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| LogP |
6.054
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
406
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ROEBJVHPINPMKL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H22ClN3O.2ClH/c1-3-24(4-2)13-14-11-16(6-8-20(14)25)23-18-9-10-22-19-12-15(21)5-7-17(18)19/h5-12,25H,3-4,13H2,1-2H3,(H,22,23)2*1H
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| Chemical Name |
4-[(7-chloroquinolin-4-yl)amino]-2-(diethylaminomethyl)phenol
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| Synonyms |
Amodiaquin dihydrochloride dihydrate
Amodiaquin dihydrochloride Amodiaquine hydrochloride dihydrate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~125 mg/mL (~291.52 mM)
H2O : ~50 mg/mL (~116.61 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.85 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.85 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00894660 | COMPLETED | Drug: Amodiaquine (Test) Drug: Amodiaquine (Comparator) |
Falciparum Malaria | Pfizer | 2009-06 | Phase 1 |
| NCT00238017 | UNKNOWN STATUS | Drug: amodiaquine-artesunate versus amodiaquine | Malaria | Charite University, Berlin, Germany | 2005-10 | Phase 4 |
| NCT00859807 | COMPLETED | Drug: Flavoquine®, Camoquin® Suspension | Falciparum Malaria | Pfizer | 2009-05 | Phase 4 |
| NCT01023399 | COMPLETED | Drug: Artesunate + Amodiaquine | Malaria | Sanofi | 2009-11 | Phase 4 |
| NCT04080895 | RECRUITING | Drug: Artemether-lumefantrine Drug: Amodiaquine Drug: Artemether-lumefantrine Drug: Artemether-lumefantrine + Amodiaquine |
Drug Combination Healthy Pharmacokinetic |
University of Oxford | 2022-11-01 | Phase 1 |
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