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Amodiaquine dihydrochloride dihydrate Histone Methyltransferase inhibitor

Name: Amodiaquine dihydrochloride dihydrate
Brand: Selleck Chemicals
SKU: S4589
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S4589

Amodiaquine is a potent, non-competitive inhibitor of histamine N-methyl transferase with estimated Ki of 18.6 nM. It is also used as an antimalarial and anti-inflammatory agent.

Amodiaquine dihydrochloride dihydrate Histone Methyltransferase inhibitor Chemical Structure

Quality Control

Batch: Purity: 99.80%

99.80

Related Targets	HDAC JAK BET PKC PARP HIF PRMT EZH2 AMPK Histone Acetyltransferase
Other Histone Methyltransferase Inhibitors	Pinometostat (EPZ5676) 3-Deazaneplanocin A (DZNep) Hydrochloride BIX-01294 Trihydrochloride EPZ015666 (GSK3235025) UNC1999 EPZ004777 MM-102 (HMTase Inhibitor IX) Chaetocin SGC 0946 EPZ005687

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (197.93 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 29 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.6mg/ml (9.90mM)	Taking the 1 mL working solution as an example, add 50 μL of 92 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.66mg/ml (1.42mM)	Taking the 1 mL working solution as an example, add 50 μL of 13.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	464.81	Formula	C₂₀H₂₂ClN₃O.2HCl.2H₂O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	6398-98-7	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			SMILES	CCN(CC)CC1=C(C=CC(=C1)NC2=C3C=CC(=CC3=NC=C2)Cl)O.O.O.Cl.Cl

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC₅₀/Ki	histamine N-methyl transferase (Cell-free assay) 18.6 nM(Ki)
In vivo	In vivo administration of a small dose amodiaquine dramatically enhanced the effect of histamine on the gastric secretion in dogs. Amodiaquine prevents severe hepatic injury and high lethality in P. acnes-primed and LPS-induced hepatitis mice. Its treatment enhances the elevation of histamine in the liver of P. acnes-primed and LPS-induced hepatitis mice without accompanying tele-methyl histamine elevation.
References	[1] https://pubmed.ncbi.nlm.nih.gov/17222819/ [2] https://pubmed.ncbi.nlm.nih.gov/16168438/ [3] https://pubmed.ncbi.nlm.nih.gov/1203620/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-01-07)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT07322068	NOT_YET_RECRUITING	Malaria, Falciparum	Stanford University	2026-09	PHASE4
NCT06967519	RECRUITING	Malaria; Hiv	Yale University	2025-12-18	PHASE4
NCT05951595	RECRUITING	Uncomplicated Plasmodium Falciparum Malaria	University of Oxford	2025-09-11	PHASE3
NCT06083688	COMPLETED	Malaria,Falciparum; Anemia in Children	Liverpool School of Tropical Medicine	2024-10-14	PHASE4
NCT04080895	TERMINATED	Pharmacokinetic; Healthy; Drug Combination	University of Oxford	2022-11-01	PHASE1
NCT05764746	COMPLETED	Uncomplicated Plasmodium Falciparum Malaria	Muhimbili University of Health and Allied Sciences	2023-05-01	PHASE2; PHASE3

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