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/ Hydroxychloroquine sulfate/硫酸羟基氯喹

Hydroxychloroquine sulfate/硫酸羟基氯喹 {[allProObj[0].p_purity_real_show]}

货号：A105779 同义名： 硫酸羟氯喹 / HCQ sulfate; Hydroxychloroquine(sulfate)(CRM)

Hydroxychloroquine sulfate (HCQ sulfate) 是一种合成的抗疟疾化合物，可抑制 Toll 样受体 7/9 (TLR7/9) 信号传导，并对 SARS-CoV-2 感染具有抑制作用。

Hydroxychloroquine sulfate/硫酸羟基氯喹 化学结构 CAS号：747-36-4
Hydroxychloroquine sulfate/硫酸羟基氯喹 化学结构
CAS号：747-36-4
Hydroxychloroquine sulfate/硫酸羟基氯喹 3D分子结构
CAS号：747-36-4
Hydroxychloroquine sulfate/硫酸羟基氯喹 化学结构 CAS号：747-36-4
Hydroxychloroquine sulfate/硫酸羟基氯喹 3D分子结构 CAS号：747-36-4
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Hydroxychloroquine sulfate/硫酸羟基氯喹 纯度/质量文件 产品仅供科研

货号：A105779 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 Autophagy ↓ 其他靶点 纯度
SBI-0206965 +++

ULK2, IC50: 711 nM

ULK1, IC50: 108 nM

 		95%
Hydroxychloroquine sulfate ✔ 99%
Valproic acid sodium ✔ HDAC 97%
PFK-015 ++

PFKFB3, IC50: 207 nM

 		99%+
MRT68921 HCl ++++

ULK2, IC50: 1.1 nM

ULK1, IC50: 2.9 nM

 		99%+
ROC-325 ✔ 99%+
Autophinib +++

Autophagy, IC50: 40 nM

 		99%
Lys05 ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Hydroxychloroquine sulfate/硫酸羟基氯喹 生物活性

靶点

  • Autophagy
描述 Hydroxychloroquine sulfate (HCQ sulfate) is a synthetic antimalarial agent that also inhibits Toll-like receptor 7/9 (TLR7/9) signaling. It is effective at inhibiting SARS-CoV-2 infection in vitro[1].[2].[3].
体内研究

Hydroxychloroquine sulfate is also prescribed for lupus treatment, and together with its analog chloroquine, it inhibits TLR7 and TLR9 signaling[2].
体外研究

Originally derived from 4-aminoquinoline, it has been used for several decades to treat rheumatic diseases such as rheumatoid arthritis (RA)[1].

At a concentration of five micromolar, Hydroxychloroquine sulfate or chloroquine does not affect intracellular pH, though it can inhibit TLR9 or 7 signaling triggered by DNA or RNA ligands[2].

Hydroxychloroquine sulfate/硫酸羟基氯喹 细胞实验

Cell Line
Concentration Treated Time Description References
ZR-75-1 ICI-R cells 1 μM 6 days To evaluate the effect of hydroxychloroquine on antiestrogen sensitivity, results showed that HCQ enhanced antiestrogen-mediated cell death. Clin Cancer Res. 2014 Jun 15;20(12):3222-32.
MCF7-RR cells 1 μM 6 days To evaluate the effect of hydroxychloroquine on antiestrogen sensitivity, results showed that HCQ enhanced antiestrogen-mediated cell death. Clin Cancer Res. 2014 Jun 15;20(12):3222-32.
LCC9 cells 1 μM 6 days To evaluate the effect of hydroxychloroquine on antiestrogen sensitivity, results showed that HCQ enhanced antiestrogen-mediated cell death. Clin Cancer Res. 2014 Jun 15;20(12):3222-32.
MCF7 cells 1 μM 6 days To evaluate the effect of hydroxychloroquine on antiestrogen sensitivity, results showed that HCQ enhanced antiestrogen-mediated cell death. Clin Cancer Res. 2014 Jun 15;20(12):3222-32.
Patient-derived organoids 1uM 7 days To evaluate the effect of hydroxychloroquine on patient-derived organoids from gastric cancer peritoneal metastasis, results showed that hydroxychloroquine significantly induced organoid apoptosis. Nat Commun. 2023 Feb 14;14(1):822.
3T3-L1 adipocytes 50 μM 24 h To evaluate the effect of hydroxychloroquine on inflammatory and metabolic gene expression in adipocytes activated by serum from RA patients. Results showed that hydroxychloroquine significantly reduced mRNA expression of TNF-α and IL-1β and modulated the expression of genes related to lipid and glucose metabolism. Front Immunol. 2021 Oct 13;12:744022.
H1975 cells 10 μM 16 h To investigate the effect of hydroxychloroquine in combination with erlotinib or paclitaxel on EGFR TKI-resistant cells. Results showed that hydroxychloroquine combined with erlotinib or paclitaxel reduced EGFR activation and AKT activity. Theranostics. 2020 Feb 3;10(6):2727-2743.
Peripheral blood mononuclear cells (PBMCs) 100 μM 24 h To investigate the inhibitory effect of hydroxychloroquine on trained immunity. Results showed hydroxychloroquine inhibited HKCA-induced trained immune responses, including responses to virus-like stimuli and interferons. Cell Rep Med. 2020 Nov 10;1(9):100146.
hFob1.19 cells 10 µM 12 h Inhibited autophagy, reduced HG-induced lipid peroxide and ROS accumulation Mol Med. 2023 Sep 14;29(1):125.

Hydroxychloroquine sulfate/硫酸羟基氯喹 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Athymic nude mice LCC9 and MCF7-RR cells mammary fat pad xenograft model HCQ: drinking water; TAM: diet; ICI: subcutaneous injection 0.29 mg/ml (drinking water) 5 weeks To evaluate the effect of hydroxychloroquine combined with antiestrogen therapy on resensitizing resistant breast tumors. Results showed that HCQ combined with TAM significantly reduced tumor size and weight, while the ICI+HCQ combination was less effective. Clin Cancer Res. 2014 Jun 15;20(12):3222-32.
NOD/SCID mice Gastric cancer peritoneal metastasis model Intraperitoneal injection 30 μg/g Every 3 days for 3 weeks To evaluate the effect of hydroxychloroquine on gastric cancer peritoneal metastasis in mice, results showed that hydroxychloroquine significantly inhibited peritoneal metastasis. Nat Commun. 2023 Feb 14;14(1):822.
Nude mice H292 lung cancer xenograft model Intraperitoneal injection 60 mg/kg Once daily until tumor volume reached 1500 mm3 or 10% weight loss To evaluate the effect of hydroxychloroquine on the growth of H292 wild-type and ATG7 knockout tumors. Results showed that HCQ inhibited the growth of WT tumors but had no significant effect on ATG7 knockout tumors. Dev Cell. 2019 Sep 23;50(6):690-703.e6
C57BL/6 mice Obese collagen-induced arthritis (CIA) model Oral 60 mg/kg Once daily for 15 days To evaluate the effect of hydroxychloroquine on body weight, insulin resistance, and adipose tissue inflammation in obese CIA mice. Results showed that hydroxychloroquine significantly reduced body weight and insulin resistance and improved metabolic and inflammatory status in adipose tissue. Front Immunol. 2021 Oct 13;12:744022.
Nude mice HCCLM3 xenograft model Intraperitoneal injection 50 mg/kg Combination therapy with lenvatinib and hydroxychloroquine significantly inhibited HCC growth and metastasis, prolonging survival. J Hematol Oncol. 2021 Jan 14;14(1):16.
Mice CCSP-rtTA-EGFR L858R-T790M transgenic mice Oral 180 mg/kg Daily administration for 30 days To evaluate the effect of hydroxychloroquine in combination with gefitinib or paclitaxel on EGFR TKI-resistant tumors. Results showed that hydroxychloroquine combined with gefitinib or paclitaxel significantly reduced tumor volume and cell proliferation. Theranostics. 2020 Feb 3;10(6):2727-2743.
Mice IMQ-induced psoriasis-like skin lesion model Gavage 20 mg/kg Once daily for 7 days To investigate the effect of TLR7 inhibitor (hydroxychloroquine) on IMQ-induced psoriasis-like skin lesions, results showed that hydroxychloroquine reduced the severity of skin lesions and inflammatory responses. Cell Death Dis. 2023 May 9;14(5):315
Mice Polytrauma model and DVT model Intraperitoneal injection 50mg/kg Single dose, lasting 30 minutes To assess the effect of HCQ on PEV release and thrombus formation, results showed HCQ significantly reduced PEV release and decreased thrombus burden J Thromb Haemost. 2019 Oct;17(10):1733-1745
Mice IGF1Rtg mice and dnPI3K mice Intraperitoneal injection 60 mg/kg Daily for 4 weeks To evaluate the effect of autophagy inhibition on cardiac function in dnPI3K mice. Results showed that HCQ treatment abolished the differences in cardiac function between dnPI3K and WT mice. Circulation. 2022 Jun 21;145(25):1853-1866

Hydroxychloroquine sulfate/硫酸羟基氯喹 动物研究

Dose Mice: 3 mg/kg - 100 mg/kg[3] (p.o.) Dog: 7.5 mg/kg - 12.5 mg/kg[4] (p.o.)
Administration p.o.

Hydroxychloroquine sulfate/硫酸羟基氯喹 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02603146 Healthy Participants ... 展开 >> Rheumatoid Arthritis (RA) Prevention 收起 << Phase 2 Recruiting March 2020 -
NCT01897116 Melanoma Phase 1 Completed - United States, Pennsylvania ... 展开 >> Abramson Cancer Center of the University of Pennsylvania Philadelphia, Pennsylvania, United States, 19104 收起 <<
NCT00430807 Giant Cell Arteritis Phase 3 Completed - France ... 展开 >> Hospital Agen, France, 47923 Hospital Albi, France, 81000 Hospital Auch Auch, France, 32008 Hospital Avignon Avignon, France, 84902 University Hospital Besançon Besançon, France, 25030 Hospital Béziers Beziers, France, 34525 University Hospital Côte de Nacre Caen, France, 14033 University Hospital Dijon Dijon, France, 21035 Hospital Foix, France, 09017 Hospital Lavaur, France, 81500 University Hospital Dupuytren Limoges, France, 87042 Hospital Lisieux, France, 14100 Hospital Lourdes, France, 65107 Hospital Mazamet, France, 81200 Hospital Montauban, France, 82013 University Hospital Nantes, France, 44035 Saint Louis Hospital Paris, France, 75010 University Hospital Saint Antoine Paris, France, 75012 University Hospital Bichat Paris, France, 75018 Hospital Suresnes Suresnes, France, 92151 University Hospital Toulouse Toulouse, France, 31059 University Hospital Toulouse, France, 31059 University Hospital Bretonneau Tours, France, 37044 收起 <<

Hydroxychloroquine sulfate/硫酸羟基氯喹 参考文献

[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.

[3]Yao X, et al. In Vitro Antiviral Activity and Projection of Optimized Dosing Design of Hydroxychloroquine for the Treatment of Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2). Clin Infect Dis. 2020 Mar 9. pii: ciaa237.

Hydroxychloroquine sulfate/硫酸羟基氯喹 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.30mL

0.46mL

0.23mL

11.52mL

2.30mL

1.15mL

23.04mL

4.61mL

2.30mL

Hydroxychloroquine sulfate/硫酸羟基氯喹 技术信息

CAS号747-36-4
分子式C18H28ClN3O5S
分子量 433.95
SMILES Code CCN(CCO)CCCC(NC1=CC=NC2=CC(Cl)=CC=C12)C.O=S(O)(O)=O
MDL No. MFCD00078203
别名 硫酸羟氯喹 ;HCQ sulfate; Hydroxychloroquine(sulfate)(CRM); HCQ; NSC 4375; Hydroxychloroquine(sulfate); HCQ(sulfate)
运输蓝冰
InChI Key JCBIVZZPXRZKTI-UHFFFAOYSA-N
Pubchem ID 12947
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, room temperature
溶解方案

DMSO: 105 mg/mL(241.96 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(230.44 mM)

配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Hydroxychloroquine sulfate | HCQ sulfate;Hydroxychloroquine (sulfate) (CRM);HCQ;NSC 4375 | 硫酸羟氯喹 | Insect Repellent | Autophagy | TLR | AmBeed-信号通路专用抑制剂 | Hydroxychloroquine sulfate/硫酸羟基氯喹 纯度/质量文件 | Hydroxychloroquine sulfate/硫酸羟基氯喹 亚型比较 | Hydroxychloroquine sulfate/硫酸羟基氯喹 生物活性 | Hydroxychloroquine sulfate/硫酸羟基氯喹 动物研究 | Hydroxychloroquine sulfate/硫酸羟基氯喹 临床数据 | Hydroxychloroquine sulfate/硫酸羟基氯喹 参考文献 | Hydroxychloroquine sulfate/硫酸羟基氯喹 实验方案 | Hydroxychloroquine sulfate/硫酸羟基氯喹 技术信息

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