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Chloroquine Autophagy/Lysosome inhibitor

Name: Chloroquine
Brand: Selleck Chemicals
SKU: S6999
Rating: 5 (249 reviews)

Cat.No.S6999

Chloroquine is an antimalarial drug and Autophagy/lysosome inhibitor. Chloroquine also suppresses Toll-like receptor-9 (TLR9) protein expression. Chloroquine is highly effective against SARS-CoV-2 (COVID-19) infection with an EC50 of 1.13 μM in Vero E6 cells. Chloroquine has anti-HIV-1 activity.

Chemical Structure

Molecular Weight: 319.87

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Quality Control

Batch: Purity: 99.84%

99.84

Related Targets	CXCR Nrf2 Mitophagy LRRK2 ULK FKBP Heme Oxygenase cGAS LC3 Cell wall
Other Autophagy Inhibitors	Resveratrol (trans-Resveratrol) Spautin-1 PIK-III DC661 Lys05 Trihydrochloride Autophinib Spermidine SMER28 EN6 Flubendazole

Chemical Information, Storage & Stability

Molecular Weight	319.87	Formula	C₁₈H₂₆ClN₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	54-05-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	NSC-187208, CHQ, CQ			Smiles	CCN(CC)CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl

Solubility

In vitro
Batch:

DMSO : 64 mg/mL (200.08 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 64 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

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.
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.
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.	3.250mg/ml (10.16mM)	Taking the 1 mL working solution as an example, add 50 μL 65 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL ddH2O to adjust the volume to 1 mL. 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.

Mechanism of Action

Targets/IC₅₀/Ki	Autophagy lysosome TLR9 HIV-1 SARS-CoV-2 (Vero E6 cells based assay) 1.13 μM(EC50)
In vitro	Chloroquine is a widely used Autophagy inhibitor.
In vivo	The inhibition of Autophagy by Chloroquine potentiates the therapeutic effect of PI3K/AKT inhibitors in vitro and in vivo TNBC models, synergising with taxane-based chemotherapy.
References	[1] https://pubmed.ncbi.nlm.nih.gov/25385822/ [2] https://pubmed.ncbi.nlm.nih.gov/24273604/ [3] https://pubmed.ncbi.nlm.nih.gov/32145363/ [4] https://pubmed.ncbi.nlm.nih.gov/11166661/ [5] https://pubmed.ncbi.nlm.nih.gov/33638615/ [6] https://pubmed.ncbi.nlm.nih.gov/35761360/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05972551	Recruiting	Osteogenesis Imperfecta	Amgen	April 22 2024	Phase 3
NCT05890573	Recruiting	Pulmonary Fibrosis\|COVID-19 Pneumonia	Second Affiliated Hospital School of Medicine Zhejiang University	April 16 2024	Not Applicable
NCT05841758	Not yet recruiting	Sarcoidosis Pulmonary	Hospices Civils de Lyon	April 1 2024	Phase 4
NCT03994874	Not yet recruiting	Congestive Heart Failure	Iperboreal Pharma Srl	March 2024	Phase 1\|Phase 2
NCT06117722	Not yet recruiting	Chronic Heart Failure	Elpen Pharmaceutical Co. Inc.	March 1 2024	--

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