Hydroxychloroquine (HCQ) Sulfate

別名:NSC 4375

Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.

Hydroxychloroquine (HCQ) Sulfate化学構造

CAS No. 747-36-4

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり
JPY 40500 国内在庫あり
JPY 70500 国内在庫あり
JPY 145500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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Hydroxychloroquine (HCQ) Sulfate関連製品

シグナル伝達経路

Autophagy阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
Antiproliferative assay A549 cells 25 ug/ml 20 hrs Antiproliferative activity in human A549 cells at 25 ug/ml up to 20 hrs by xCELLigence RTCA SP based cellular impedance analysis 28570977
Antiproliferative assay A549 cells 25 ug/ml 60 hrs Antiproliferative activity in human A549 cells at 25 ug/ml after 60 hrs by xCELLigence RTCA SP based cellular impedance analysis 28570977
Autophagy assay NCI-H3122 cells 25 to 50 uM 6 hrs Inhibition of autophagy in human NCI-H3122 cells assessed as increase in punctate LC3 expression at 25 to 50 uM after 6 hrs by fluorescence microscopic analysis 25699157
Apoptosis assay H460 cells 25 to 75 uM 24 hrs Induction of apoptosis in human H460 cells at 25 to 75 uM after 24 hrs by annexin-V staining-based flow cytometry 25699157
Antiviral assay Vero E6 cells 48 h IC50 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line at 48 h by immunofluorescence-based assay (detecting the viral NP protein in the nucleus of the Vero E6 cells)., IC50 = 0.67608 μM. 32353859
Antiproliferative assay BxPC3 cells 72 hrs Antiproliferative activity against human BxPC3 cells after 72 hrs by SRB method, IC50 = 33 μM. 25699157
Autophagy assay H460 cells 24 hrs Inhibition of autophagy in human H460 cells assessed as increase in LC3-2 level at IC50 after 24 hrs by immunoblot analysis 25699157
Antiviral assay Vero E6 cells 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC50 = 4.17 μM. ChEMBL
Antiviral assay Vero E6 cells 3 days IC50 determination at MOI 0.004 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells, IC50 = 9.21 μM. ChEMBL
Antiviral assay Vero E6 cells 3 days IC50 determination at MOI 0.01 using CellTiter- Glo (CTG) assay, performed 3 days post-infection in SARS-CoV-2 infected Vero E6 cells, IC50 = 11.17 μM. ChEMBL
Antiviral assay Vero E6 cells 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days, EC90 = 25.49 μM. ChEMBL
Function assay HEK-Blue cells Antagonist activity at human TLR9 expressed in HEK-Blue cells assessed as reduction in CpGB-induced NF-kappaB levels after 24 hrs by spectrophotometric analysis, IC50 = 0.11 μM. 30292896
Function assay HEK-Blue cells Antagonist activity at human TLR7 expressed in HEK-Blue cells assessed as reduction in CL264-induced NF-kappaB levels after 24 hrs by spectrophotometric analysis, IC50 = 0.8 μM. 30292896
Function assay HEK293 cells hERG binding assays: Displacement of [3H]-Dofetilide (5 nM final) from hERG membranes obtained from HEK293 cells, Ki = 2.51189 μM. 32353859
Antiviral assay Vero E6 cells IC90 for antiviral activity against SARS-CoV-2 in the Vero E6 cell line by measuring infectious viral titer of supernatent from compound-treated Vero E6 cells by Median Tissue Culture Infectious Dose (TCID)50 by the method of Reed and Muench, IC90 = 5.78 μM. 32353859
qHTS assay A673 cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
qHTS assay BT-37 cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
qHTS assay SK-N-MC cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
qHTS assay NB-EBc1 cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
qHTS assay LAN-5 cells qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
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生物活性

製品説明 Hydroxychloroquine (HCQ) Sulfate is an antimalarial agent used for the treatment of systemic lupus erythematosus, rheumatoid arthritis and other autoimmune, inflammatory and dermatologic conditions. Also acts as an inhibitor of autophagy and toll-like receptor (TLR) 7/9.
Targets
TLR9 [5] Autophagy [1]
In Vitro
In vitro

Hydroxychloroquine Sulfate is a potent inhibitor of autophagy. It prevents lysosomal acidification, thereby interfering with a key step in the autophagic process.HCQ treatment inhibits RCC (renal cell cancer) cell growth, promotes apoptosis, inhibits mitochondrial oxygen consumption, and increases rates of glycolysis[2].

Kinase Assay In vitro kinase assays
with purified proteins, recombinant S6 protein and recombinant active P70S6K are incubated in 1x kinase buffer with various amount of HCQ or RAD001 in the presence (25 μM) or absence of ATP for 30 minutes at 30°C. Total and phosphorylated S6 at ser235/236 and ser240/244 are detected by western analysis using phosphospecific antibodies. Note that recombinant GST-tagged S6 (53 kd) is distinguished from endogenous S6 (32 kd) on the western blot.
細胞実験 細胞株 Human RCC cell lines
濃度 75 or 100 μM
反応時間 48 h
実験の流れ

All cells are cultured in RPMI with 10% FBS, 1% glutamine, and 1% Pen/Strep. cells are seeded on the appropriated plates overnight and treated with HCQ (75 or 100 μM) for 48 hours.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot NOX2 / β-actin p-NF-κB / β-actin NLRP3 / β-actin p62 / LC3-I / LC3-II / GAPDH 32260307
IHC HE staining of spleen tissue 29456648
Immunofluorescence ZO-1 32260307
In Vivo
In Vivo

The treatment of Hydroxychloroquine Sulfate reduces the infarct size in an in vivo rat model of I/R injury and the cardioprotective effect of Hydroxychloroquine is ERK1/2 dependent[3].

In addition, Hydroxychloroquine Sulfate shows an early vascular protective effect. HCQ seems to prevent the occurrence of endothelial dysfunction(ED) in treated animals[4].

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05841758 Not yet recruiting
Extra Pulmonary Sarcoidosis
Hospices Civils de Lyon
September 1 2023 Phase 4
NCT04731051 Withdrawn
2019 Novel Coronavirus
King Hussein Cancer Center|Amman Pharmaceutical Industries (API)|Sana Pharmaceutical Industry|ACDIMA Biocenter
October 2022 Phase 1|Phase 2
NCT05733897 Recruiting
Nonalcoholic Steatohepatitis
National Taiwan University Hospital|National Taiwan University
June 10 2022 --
NCT05237843 Unknown status
Recurrent Pregnancy Loss
Ain Shams University
March 1 2022 Phase 1
NCT05113810 Recruiting
2019 Novel Coronavirus
Ministry of Health Jordan|King Hussein Cancer Center|ACDIMA Biocenter|Amman Pharmaceutical Industries|Sana Pharmaceutical Industry
March 20 2022 Phase 2
NCT04385264 Suspended
COVID-19
Center for Primary Care and Public Health (Unisante) University of Lausanne Switzerland
January 2022 Phase 2|Phase 3

化学情報

分子量 433.95 化学式

C18H28ClN3O5S

CAS No. 747-36-4 SDF Download Hydroxychloroquine (HCQ) Sulfate SDFをダウンロードする
Smiles CCN(CCCC(C)NC1=C2C=CC(=CC2=NC=C1)Cl)CCO.OS(=O)(=O)O
保管

In vitro
Batch:

Water : 87 mg/mL

DMSO : Insoluble ( 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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