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

Amodiaquine dihydrochloride dihydrate  (Synonyms: Amodiaquin dihydrochloride dihydrate)

Cat. No.: HY-B1322 Purity: 99.89%
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Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate 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.

Amodiaquine dihydrochloride dihydrate Chemical Structure

Amodiaquine dihydrochloride dihydrate Chemical Structure

CAS No. : 6398-98-7

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Based on 9 publication(s) in Google Scholar

Other Forms of Amodiaquine dihydrochloride dihydrate:

Amodiaquine dihydrochloride dihydrate Related Antibodies

Top Publications Citing Use of Products

View All Nuclear Hormone Receptor 4A/NR4A Isoform Specific Products:

View All Isoforms
Nurr1/NR4A2 Nur77/NR4A1

View All Parasite Isoform Specific Products:

View All Isoforms
Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

View All Histone Methyltransferase Isoform Specific Products:

View All Isoforms
EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate 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
Vero C1008 CC50
> 38.63 μM
Compound: Amodiaquine Hydrochloride
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 CC50
> 38.63 μM
Compound: Amodiaquine Hydrochloride
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 IC50
2.36 μM
Compound: Amodiaquine Hydrochloride
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 IC50
2.59 μM
Compound: Amodiaquine Dihydrochloride Dihydrate
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 CC50
34.42 μM
Compound: Amodiaquine Dihydrochloride Dihydrate
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 CC50
34.42 μM
Compound: Amodiaquine Dihydrochloride Dihydrate
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
CC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 IC50
4.94 μM
Compound: Amodiaquine Dihydrochloride Dihydrate
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
10.1101/2020.03.25.008482
Vero C1008 IC50
5.64 μM
Compound: Amodiaquine Hydrochloride
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells
10.1101/2020.03.25.008482
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 dihydrochloride dihydrate 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.
Clinical Trial
Molecular Weight

464.81

Formula

C20H22ClN3O.2H2O.2HCl
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

OC1=CC=C(NC2=CC=NC3=CC(Cl)=CC=C23)C=C1CN(CC)CC.Cl.Cl.O.O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (215.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 20 mg/mL (43.03 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1514 mL 10.7571 mL 21.5142 mL
5 mM 0.4303 mL 2.1514 mL 4.3028 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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:

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.38 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.38 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.89%

SDS (393 KB)

COA (254 KB) LCMS (92 KB)

Handling Instructions (2659 KB)
References

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 (sealed storage, away from moisture and light). 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
H2O / DMSO 1 mM 2.1514 mL 10.7571 mL 21.5142 mL 53.7854 mL
5 mM 0.4303 mL 2.1514 mL 4.3028 mL 10.7571 mL
10 mM 0.2151 mL 1.0757 mL 2.1514 mL 5.3785 mL
15 mM 0.1434 mL 0.7171 mL 1.4343 mL 3.5857 mL
20 mM 0.1076 mL 0.5379 mL 1.0757 mL 2.6893 mL
25 mM 0.0861 mL 0.4303 mL 0.8606 mL 2.1514 mL
30 mM 0.0717 mL 0.3586 mL 0.7171 mL 1.7928 mL
40 mM 0.0538 mL 0.2689 mL 0.5379 mL 1.3446 mL
DMSO 50 mM 0.0430 mL 0.2151 mL 0.4303 mL 1.0757 mL
60 mM 0.0359 mL 0.1793 mL 0.3586 mL 0.8964 mL
80 mM 0.0269 mL 0.1345 mL 0.2689 mL 0.6723 mL
100 mM 0.0215 mL 0.1076 mL 0.2151 mL 0.5379 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Amodiaquine dihydrochloride dihydrate 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:

Amodiaquine dihydrochloride dihydrate6398-98-7Amodiaquin dihydrochloride dihydrateNuclear Hormone Receptor 4A/NR4AParasiteHistone MethyltransferaseNerve Growth Factor IB-like ReceptorNurr1antimalarialneuroprotectiveIL-1βCCL2CXCL2anti-inflammatoryN-methyltransferaseInhibitorinhibitorinhibit

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