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Chloroquine diphosphate. (Synonyms: 磷酸氯喹)

目录号: PC16221 纯度: ≥98%

CAS No. :50-63-5

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中文名称	Chloroquine diphosphate.
中文别名	磷酸氯喹;7-氯-4-(4-二乙氨基-1-甲基丁氨基)喹啉二磷酸盐;磷酸氯化喹啉;二磷酸氯喹;氯喹二磷酸盐;氯喹啉二磷酸盐;氯喹宁二磷酸盐;磷酸氯喹 GMP;磷酸氯喹 USP标准品;磷酸氯喹标准品;磷酸氯喹啉;磷酸氯喹原药;磷酸氯盐标准品;氯喹磷酸盐标准品;氯酸氯喹;酮康唑;1-十六醇;1-十六醇.1-十六烷醇;磷酸氯喹,certified 标准品;N4-(7-氯-4-喹啉基)-N1,N1-二甲基-1,4-戊二胺二磷酸盐;磷酸氯喹，医药级,纯度:>99%;氯化喹啉磷酸盐;氯喹磷酸盐
英文名称	Chloroquine diphosphate
英文别名	chloroquine bis(phosphate);7-chlor-4-(4-(diaethylamino)-1-methylbutylamino)-chinolindiphosphat;7-chloro-4-((4’-diethylamino-1-methylbutyl)amino)quinolinediphosphate;7-chloro-4-(4-diethylamino-1-methyl-butylamino)-quinolindiphosphate;alermine;aralendiphosphate;chingaminphosphate;chloroquindiphosphate;Chloroquine diphosphate salt;Chloroquine (diphosphate);Chloroquine diphosphate;Chloroquine Phosphate;7-Chloro-4-[4-(diethylamino)-1-methylbutylamino]quinoline Diphosphate;N4-(7-Chloro-4-quinolyl)-N1,N1-diethyl-1,4-pentanediamine Diphosphate;N4-(7-chloroquinolin-4-yl)-N1,N1-diethylpentane-1,4-diamine diphosphate;N-(7-Chloro-4-quinolinyl)-N,N-dimethyl-1,4-pentanediamine diphosphate salt;Aralen phosphate;Delagil;Arechin;Chingaminum;Chingamin phosphate;H-Stadur;Aralen diphosphate;Tanakan;Khingamin;Miniquine;Tanakene;Chlorochin diphosphate;Chloroquin diphosphate;Tanakan (antimalarial);Gontochin phosphate;dl-Chloroquine diphosphate;Ipsen 225;3377 RP;WR 1522;Chloroquine dihydrogen phosphate (1:2);SN 7,6
Cas No.	50-63-5
分子式	C₁₈H₃₂ClN₃O₈P₂
分子量	515.86
包装储存	4°C, sealed storage, away from moisture and light *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

生物活性

Chloroquine phosphate is an antimalarial and anti-inflammatory agent widely used to treat malaria and rheumatoid arthritis. Chloroquine phosphate is an autophagy and toll-like receptors (TLRs) inhibitor. Chloroquine phosphate is highly effective in the control of SARS-CoV-2 (COVID-19) infection 体外研究 (EC₅₀=1.13 μM).

性状

Solid

IC50 & Target[1][2]

Plasmodium

Malaria

TLRs

SARS-COV-2

HIV-1

体外研究(In Vitro)

Chloroquine (CHQ, 20 μM) inhibits IL-12p70 release and reduces Th1-priming capacity of activated human monocyte-derived Langerhans-like cells (MoLC). Chloroquine (CHQ, 20 μM) enhances IL-1–induced IL-23 secretion in MoLC and subsequently increases IL-17A release by primed CD4 T cells. Chloroquine (25 μM) suppresses MMP-9 mRNA expression in normoxia and hypoxia in parental MDA-MB-231 cells. Chloroquine has cell-, dose- and hypoxia-dependent effects on MMP-2, MMP-9 and MMP-13 mRNA expression. TLR7 and TLR9 inhibition using IRS-954 or chloroquine significantly reduces HuH7 cell proliferation 体外研究.
Chloroquine (0.01-100 μM; 48?hours) potently blocks virus infection (vero E6 cells infected with SARS-CoV-2) at low-micromolar concentration (EC₅₀=?1.13?μM). Chloroquine blocks virus infection by increasing endosomal pH required for virus/cell fusion, as well as interfering with the glycosylation of cellular receptors of SARS-CoV.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Chloroquine (80 mg/kg, i.p.) does not prevent the growth of the triple-negative MDA-MB-231 cells with high or low TLR9 expression levels in the orthotopic mouse model. TLR7 and TLR9 inhibition using IRS-954 or chloroquine significantly inhibits tumour growth in the mouse xenograft model. HCC development in the DEN/NMOR rat model is also significantly inhibited by chloroquine.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

ClinicalTrial

参考文献

[1]. Said A, et al. Chloroquine promotes IL-17 production by CD4+ T cells via p38-dependent IL-23 release by monocyte-derived Langerhans-like cells. J Immunol. 2014 Dec 15;193(12):6135-43. [Information]

[2]. Tuomela J, et al. Chloroquine has tumor-inhibitory and tumor-promoting effects in triple-negative breast cancer. Oncol Lett. 2013 Dec;6(6):1665-1672. [Information]

[3]. Mohamed FE, et al. Effect of toll-like receptor 7 and 9 targeted therapy to prevent the development of hepatocellular carcinoma. Liver Int. 2014 Jul 2. doi: 10.1111/liv.12626. [Information]

[4]. Colson P, et al. Chloroquine and hydroxychloroquine as available weapons to fight COVID-19. Int J Antimicrob Agents. 2020;55(4):105932. [Information]

[5]. Wang M, et al. Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) 体外研究. Cell Res. 2020 Mar;30(3):269-271. [Information]

[6]. Savarino A, et al. The anti-HIV-1 activity of chloroquine. J Clin Virol. 2001;20(3):131-135. [Information]

溶解度数据

体外研究:

H₂O : ≥ 33 mg/mL (63.97 mM)

DMSO : < 1 mg/mL (ultrasonic) (insoluble or slightly soluble)

* "≥" means soluble, but saturation unknown.

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9385 mL	9.6926 mL	19.3851 mL
5 mM	0.3877 mL	1.9385 mL	3.8770 mL
10 mM	0.1939 mL	0.9693 mL	1.9385 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制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

1.

建议依照次序添加每种溶剂： PBS
Solubility: 100 mg/mL (193.85 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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