Chloroquine diphosphate salt

powder or crystals, 98.5-101.0% (EP)

N4-(7-Chloro-4-quinolinyl)-N1,N1-dimethyl-1,4-pentanediamine diphosphate salt, N4-(7-chloroquinolin-4-yl)-N1,N1-diethylpentane-1,4-diamine diphosphate
Empirical Formula (Hill Notation):
C18H26ClN3 · 2H3PO4
CAS Number:
Molecular Weight:
Beilstein/REAXYS Number:
EC Number:
MDL number:
PubChem Substance ID:

Quality Level


98.5-101.0% (EP)


powder or crystals


193-198 °C
200 °C (dec.) (lit.)

Mode of action

enzyme | inhibits

antibiotic activity spectrum


SMILES string




InChI key


Gene Information

human ... ABCC1(4363)

Looking for similar products? Visit Product Comparison Guide

General description

Chloroquine is a member of quinolone family and is a weak intercalating agent. Chloroquine is used for treating amebiasis, rheumatoid arthritis, discoid and systemic lupus erythematosus.


DNA intercalator. Also used to increase transfection efficiency.
Chloroquine diphosphate salt has been used :
  • in in vitro antiplasmodial assays
  • in transfection and infection assays
  • in autophagy inhibition
  • in differentiation of induced pluripotent stem (iPS) cells into cardiomyocytes
  • in flow treatment of infected blood


25, 50, 100, 250 g in glass bottle

Biochem/physiol Actions

Standard anti-malarial drug. Substrate for MRP in multidrug resistant cell line and inhibits photoaffinity labeling of MRP by quinoline-based photoactive drug IAAQ (N-[4-[1-hydroxy-2-(dibutylamino)ethyl]quinolin-8-yl]-4-azidosalicylamide).

Features and Benefits

This compound is also offered as part of Sigma′s Library of Pharmacologically Active Compounds (LOPAC®1280), a biologically annotated collection of high-quality, ready-to-screen compounds. Click here to learn more.
This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

Legal Information

LOPAC is a registered trademark of Sigma-Aldrich Co. LLC


Exclamation mark

Signal Word


Hazard Statements


Acute Tox. 4 Oral


13 - Non Combustible Solids

WGK Germany


Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Personal Protective Equipment

dust mask type N95 (US),Eyeshields,Gloves

Certificate of Analysis

Certificate of Origin

Ecotoxicological evaluation of the antimalarial drug chloroquine
Zurita JL, et al.
Aquatic Toxicology (Amsterdam, Netherlands), 75(2), 97-107 (2005)
Mechanism of inhibition of DNA gyrase by analogues of nalidixic acid: the target of the drugs is DNA
Shen LL and Pernet AG
Proceedings of the National Academy of Sciences of the USA, 82(2), 307-311 (1985)
Ototoxicity of chloroquine
Matz GJ and Naunton RF
Archives of Otolaryngology, 88(4), 370-372 (1968)
Screening of medicinal plants from Reunion Island for antimalarial and cytotoxic activity
Jonville MC, et al.
Journal of Ethnopharmacology, 120(3), 382-386 (2008)
E2F1 modulates p38 MAPK phosphorylation via transcriptional regulation of ASK1 and Wip1
Hershko T, et al.
The Journal of Biological Chemistry, 281(42), 31309-31316 (2006)
We presents an article on Autophagy in Cancer Promotes Therapeutic Resistance
Read More
Protein-based drug transporters are found in most tissues including liver, kidney, intestine, and brain. These transporters are particularly important in cancer treatment and multi-drug resistance research. Understanding the specific mechanisms of tumor cell transporters is becoming an essential aspect of chemotherapeutic drug design.
Read More
Related Content
Discover Bioactive Small Molecules for ADME/Tox
Read More

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service