Shanghai Jizhi Biochemical Technology Co., Ltd
China
Product Name: Hydroxychloroquine sulfate
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DC Chemicals Limited
China
Product Name: Hydroxychloroquine Sulphate
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Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Hydroxychloroquine sulfate
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Zhejiang Hangyu API Co., Ltd
China
Product Name: Hydroxychloroquine sulfate
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Purity: 99.5%
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Henan Tianfu Chemical Co., Ltd.
China
Product Name: Hydroxychloroquine sulfate
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747-36-4

747-36-4 structure

747-36-4 structure

Name: Hydroxychloroquine sulfate
Chemical Name: Hydroxychloroquine sulfate
CAS Number: 747-36-4
Molecular Formula: C₁₈H₂₈ClN₃O₅S
Molecular Weight: 433.950
Catalog: API Antiparasitic drug Antimalarial
Create Date: 2018-04-24 08:00:00
Modify Date: 2024-01-03 09:49:38
Hydroxychloroquine sulfate is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling.

Name	Hydroxychloroquine sulfate
Synonyms	2-[{4-[(7-Chloro-4-quinolinyl)amino]pentyl}(ethyl)amino]ethanol sulfate (1:1) 2-[{4-[(7-Chlorchinolin-4-yl)amino]pentyl}(ethyl)amino]ethanolsulfat(salt) EINECS 212-019-3 Hydroxychloroquine Sulfate Plaquenil Ethanol, 2-[[4-[(7-chloro-4-quinolinyl)amino]pentyl]ethylamino]-, sulfate (1:1) (salt) 2-[4-[(7-chloroquinolin-4-yl)amino]pentyl-ethylamino]ethanol,sulfuric acid TCMDC-123987 Hydroxychloroquine Sulphate 2-[{4-[(7-Chloroquinolin-4-yl)amino]pentyl}(ethyl)amino]ethanol sulfate (1:1) 2-[{4-[(7-chloroquinolin-4-yl)amino]pentyl}(ethyl)amino]ethanol sulfate (salt) MFCD00078203 Ercoquin Quensyl

Description	Hydroxychloroquine sulfate is a synthetic antimalarial drug which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling.
Related Catalog	Signaling Pathways >> Anti-infection >> Parasite Signaling Pathways >> Immunology/Inflammation >> Toll-like Receptor (TLR) Research Areas >> Infection Research Areas >> Cancer
Target	Antimalarial[1], TLR7/9[2]
In Vitro	Hydroxychloroquine sulfate is a synthetic antimalarial drug derived from 4-aminoquinoline; it has been used for several decades for the treatment of some rheumatic diseases such as rheumatoid arthritis (RA)[1]. Five micromolar Hydroxychloroquine sulfate or chloroquine also has no measurable effect on intracellular pH, although these concentrations can inhibit TLR9 or 7 signaling induced by DNA or RNA ligands[2].
In Vivo	Hydroxychloroquine sulfate is prescribed for the treatment of lupus, and both Hydroxychloroquine sulfate and its analog chloroquine inhibit TLR7 and 9 signaling[2].
Kinase Assay	Five microliters of a solution of 2% L-α-phosphatidylcholine in dodecane is deposited per well on membranes of a 96-well plate. AT791 (10 µM), E6446 (10 µM), Hydroxychloroquine sulfate (40 µM), or chloroquine (40 µM) are added to one of the two compartments in pH 5.5 buffer (50 mM NaAce, 15 mM NaCl) or pH 7.4 buffer (50 mM KPO4, 150 mM NaCl), and the plate is incubated at 37°C. The next day, compound concentrations in both chambers are quantitated. In one variation of this experiment, 5 µM AT791 or E6446 is added to both chambers, one of which contains pH 5.5 buffer and the other pH 7.4 buffer. The redistribution of compound between the two chambers is monitored for 8 hours[2].
Animal Admin	MRL/lpr mice are dosed orally five times a week with 20 or 60 mg/kg E6446 or 60 mg/kg Hydroxychloroquine sulfate beginning at 5 weeks of age. Cytoxan is administered at 50 mg/kg i.p. every 10 days. A serum sample is taken immediately before the beginning of treatment to monitor changes in autoreactive antibodies. Subsequently, serum samples are collected approximately monthly and analyzed for anti-dsDNA by ELISA after 1:500 dilution. Body weights and urine samples are taken at the same interval, and proteinuria is assessed. Anti-nuclear antibodies (ANA) are assessed using commercially available HEp2 slide kits, with serum diluted to 1:100 in kit buffer. ANA scores are read blinded[2].
References	[1]. Manzo C, et al. Psychomotor Agitation Following Treatment with Hydroxychloroquine. Drug Saf Case Rep. 2017 Dec;4(1):6. [2]. Lamphier M, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol Pharmacol. 2014 Mar;85(3):429-40.

Boiling Point	516.7ºC at 760 mmHg
Melting Point	240 °C
Molecular Formula	C₁₈H₂₈ClN₃O₅S
Molecular Weight	433.950
Flash Point	266.3ºC
Exact Mass	433.143829
PSA	131.37000
LogP	4.28400
Storage condition	Refrigerator

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KK3342500

CAS REGISTRY NUMBER :: 747-36-4

LAST UPDATED :: 199806

DATA ITEMS CITED :: 1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 600 mg/kg

TOXIC EFFECTS :: Brain and Coverings - other degenerative changes Cardiac - other changes Lungs, Thorax, or Respiration - acute pulmonary edema

REFERENCE :: JATOD3 Journal of Analytical Toxicology. (Preston Pub. Inc., POB 48312, Niles, IL 60648) V.1- 1977- Volume(issue)/page/year: 14,186,1990

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302-H319
Precautionary Statements	P280-P301 + P312 + P330-P305 + P351 + P338-P337 + P313
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes	Xi: Irritant;
Risk Phrases	R36/37/38
Safety Phrases	37/39-26
RIDADR	3276
WGK Germany	3
RTECS	KK3342500
Packaging Group	III
Hazard Class	6.1
HS Code	2933499090

HS Code	2933499090
Summary	2933499090. other compounds containing in the structure a quinoline or isoquinoline ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%