Hydroxychloroquine (HCQ) Sulfate

別名：NSC 4375

製品コード：S4430 純度：99.99%

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.

CAS No. 747-36-4

サイズ	価格(税別)	在庫状況
10mg	JPY 22000	国内在庫あり
50mg	JPY 40500	国内在庫あり
200mg	JPY 70500	国内在庫あり
1g	JPY 145500	国内在庫あり

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（107）

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Hydroxychloroquine (HCQ) Sulfate関連製品

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関連化合物ライブラリー	Kinase Inhibitor Library FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Highly Selective Inhibitor Library	もっと見る

シグナル伝達経路

Autophagy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

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
Kinase Assay	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].

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
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06408298	Not yet recruiting	Resectable Localized Prostate Cancer	Lionel.D.Lewis MD\|Dartmouth Cancer Center\|Dartmouth-Hitchcock Medical Center	June 2024	Early Phase 1
NCT05841758	Not yet recruiting	Sarcoidosis Pulmonary	Hospices Civils de Lyon	April 1 2024	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

参考
[1] Ramser B, et al.J Invest Dermatol, 2009,129(10):2419-26. [2] Lee HO, et al. PLoS One. 2015, 10(7): e0131464. [3] Bourke L, et al. PLoS One. 2015, 10(12):e0143771. [4] Marta Mosca, et al. 2013 ACR/ARHP Annual Meeting. [5] Lamphier M, et al. Mol Pharmacol. 2014, 85(3):429-440. + 展開

参考

+ 展開

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	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

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
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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