B4874-1ml | Hydroxychloroquine Sulfate [747-36-4] Clinisciences

Background

Hydroxychloroquine Sulfate is a synthetic quinine derivative commonly used as an antimalarial drug [1]. It is also useful in managing systemic lupus erythematosus, rheumatoid arthritis, and other diseases. Also acts as an inhibitor of autophagy and toll-like receptor 7/9(TLR7/9) [1-3].

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 [4].

Hydroxychloroquine sulfate is prescribed for the treatment of lupus, and both Hydroxychloroquine sulfate and its analog chloroquine inhibit TLR7 and 9 signaling [4].

References:

[1] Ben-Zvi I, Kivity S, Langevitz P, et al. Hydroxychloroquine: From Malaria to Autoimmunity. Clin. Rev. Allergy Immunol, 2012, 42 (2): 145-153.

[2] Yildirim-Toruner C, Diamond B. Current and novel therapeutics in the treatment of systemic lupus erythematosus. Journal of Allergy and Clinical Immunology, 2011, 127 (2): 303-312.

[3] Swierkot J, and Szechinski J. Methotrexate in rheumatoid arthritis. Pharmacol. Rep, 2006, 58 (4): 473-492.

[4] Lamphier M, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Mol Pharmacol, 2014, 85 (3): 429-40.

Product Citation

1. Xiaofei Zhang, Tiebo Mao, et al. "Synergistic blocking of RAS downstream signaling and epigenetic pathway in KRAS mutant pancreatic cancer." Aging (Albany NY). 2022 Apr 25;14(8):3597-3606. PMID: 35468095
2. Renjie Dou, Jinjun Qian, et al. "Suppression of steroid 5α-reductase type I promotes cellular apoptosis and autophagy via PI3K/Akt/mTOR pathway in multiple myeloma." Cell Death Dis. 2021 Feb 24;12(2):206. PMID: 33627630
3. Zhuo Sun, Yidan Cao, et al. "Antiangiogenic effect of arsenic trioxide in HUVECs by FoxO3a‐regulated autophagy." J Biochem Mol Toxicol. 2021 Feb 16;e22728. PMID: 33592126

Chemical Properties

Storage	Store at -20°C
M.Wt	433.95
Cas No.	747-36-4
Formula	C₁₈H₂₈ClN₃O₅S
Solubility	insoluble in DMSO; insoluble in EtOH; ≥17.6 mg/mL in H2O
Chemical Name	2-[4-[(7-chloroquinolin-4-yl)amino]pentyl-ethylamino]ethanol; sulfuric acid
SDF	Download SDF
Canonical SMILES	CCN(CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl)CCO.OS(=O)(=O)O
Shipping Condition	Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips	We do not recommend long-term storage for the solution, please use it up soon.

Protocol

Cell experiment:[1]
Cell lines	Human renal cell cancer (RCC) cell lines, ACHN, Caki-1 and 769-P
Reaction Conditions	0 ~ 125 μM hydroxychloroquine for 48 h incubation
Applications	Hydroxychloroquine treatment inhibited growth of all three lines in a dose dependent manner. At the highest concentration of hydroxychloroquine, cell growth inhibition was similar between all three lines, ranging between 43 and 56%.
Animal experiment:[2]
Animal models	MRL/lpr mice
Dosage form	60 mg/kg Administered orally five times a week
Applications	Hydroxychloroquine was used as a control, exhibiting no impact on anti-dsDNA antibodies, whereas cytoxan caused a statistically significant suppression in anti-nuclear antibody titers. Hydroxychloroquine, as an inhibitor of toll-like receptor 7/9 (TLR7/9), could be a useful tool to study the mechanism and efficacy of other TLR7/9 inhibitors in vivo.
Note	The technical data provided above is for reference only.
	References: 1. Lee HO, Mustafa A, Hudes GR, et al. Hydroxychloroquine destabilizes phospho-S6 in human renal carcinoma cells. PLoS One, 2015, 10(7): e0131464. 2. Lamphier M, Zheng W, Latz E, et al. Novel small molecule inhibitors of TLR7 and TLR9: mechanism of action and efficacy in vivo. Molecular Pharmacology, 2014, 85(3): 429-440.

Quality Control

Purity = 99.84%

Chemical structure

Hydroxychloroquine Sulfate [747-36-4]

Référence B4874-1ml

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