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50mg |
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Purity: ≥98%
Amodiaquin (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 |
Treatment with amodiaquine (10–20 μM; 4 h) suppresses in a dose-dependent manner the expression of pro-inflammatory cytokines (IL-1β, interleukin-6, TNF-α, and iNOS) caused by lipopolysaccharide (PLS) [1]. TH+ neuron number and dopamine uptake analyses revealed that amodiaquine (5 μM; 24 h) effectively prevented neurotoxic (6-OHDA)-induced primary dopamine cell death. Additionally, amodiaquine was observed in rat PC12 cells. Modiquine's neuroprotective effects[1]
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ln Vivo |
Amodiaquine (40 mg/kg; intraperitoneal; daily; for 3 days) treatment decreased perihematoma activation of astrocytes and microglia/macrophages in male ICR mice. In addition to improving motor impairment in mice, amodiaquine also reduces 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: 10 µM, 15 µM, 20 µM Incubation Duration: 4 hrs (hours) Experimental Results: Inhibition of LPS-induced pro-inflammatory cytokines (IL-1β, interleukin-6, TNF-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. |
Molecular Formula |
C20H22CLN3O
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Molecular Weight |
355.86118
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CAS # |
86-42-0
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Related CAS # |
Amodiaquine dihydrochloride dihydrate;6398-98-7;Amodiaquine-d10;1189449-70-4;Amodiaquine dihydrochloride;69-44-3
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SMILES |
CCN(CC)CC1=C(C=CC(=C1)NC2=C3C=CC(=CC3=NC=C2)Cl)O
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InChi Key |
OVCDSSHSILBFBN-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H22ClN3O/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)
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Chemical Name |
4-[(7-chloroquinolin-4-yl)amino]-2-(diethylaminomethyl)phenol
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Synonyms |
Camochin Camoquin Camoquinal Camoquine Flavoquine Miaquin NSC 13453 SN-10751
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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 : ~66.67 mg/mL (~187.35 mM)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 | |
10 mM | 0.2810 mL | 1.4050 mL | 2.8101 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.