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Amodiaquine dihydrochloride dihydrate

组胺N-甲基转移酶抑制剂，Amodiaquine二盐酸盐二水合物是组胺N-甲基转移酶抑制剂，用作抗疟和抗炎剂。

目录号: PC12622 纯度: ≥98%

CAS No. :6398-98-7

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中文名称	Amodiaquine dihydrochloride dihydrate
中文别名	阿莫地喹盐酸盐;阿莫地喹二盐酸盐二水合物;阿莫地喹盐酸盐 USP标准品;阿莫地喹盐酸盐标准品;阿莫地喹盐酸盐(盐酸阿莫地喹);阿莫地喹盐酸盐水合物标准品;盐酸阿莫地喹;盐酸氨酚喹;盐酸卡莫喹;盐酸氯酚喹啉;4-(7-氯-4-喹啉氨基)-2-([二乙胺基]甲基)苯酚;4-[(7-氯代喹啉-4-基)氨基]-2-[(二乙氨基)甲基]苯酚二盐酸盐二水合物
英文名称	Amodiaquine dihydrochloride dihydrate
英文别名	Amodiaquine HCL;AmodiaquineHydrochloride;Amodiaquine dihydrochloride dihydrate;Amodiaquin Dihydrochloride Dihydrate;4-((7-Chloroquinolin-4-yl)amino)-2-((diethylamino)methyl)phenol dihydrochloride dihydrate;AMODIAQUIN;Amodiaquin (dihydrochloride dihydrate);AModiaquine Dihydrochloride;AMODIAQUIN DIHYDROCHLORIDE;AMODIAQUIN DIHYDROCHLORIDE DIHYDATE;AMODIAQUIN HYDROCHLORIDE;Amodiaquin hydrochloride dihydrate;AMODIAQUINE 2HCL DIHYDRATE;Amodiaquine hydrochloride USP24;4-[(7-Chloroquinolin-4-yl)amino]-2-[(diethylamino)methyl]phenol Dihydrochloride Dihydrate;4-([7-Chloro-4-quinolinyl]amino)-2-([diethylamino]methyl)phenol dihydrochloride dihydrate;Amodiaquine hydrochloride;K6PW2S574L;Amodiaquine hydrochloride [USP];AK164307;Amodiaquine hydrochloride (USP);4-(7-Chloro-4-quinolinylamino)-2-(diethylaminomethyl)phenol dihydrochloride dihydrate;CAM-AQ 1;4-[(7-c
Cas No.	6398-98-7
分子式	C₂₀H₂₈Cl₃N₃O₃
分子量	464.81
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

Amodiaquine dihydrochloride dihydrate (Amodiaquin dihydrochloride dihydrate), a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor. Amodiaquine dihydrochloride dihydrate is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC₅₀ of ~20 μM. Anti-inflammatory effect.

性状

Solid

IC50 & Target[1][2]

EC50: ~20 μM (Nurr1-LBD (ligand binding domain))
Histamine N-methyltransferase

体外研究(In Vitro)

Amodiaquine (10-20 μM; 4 hours) treatment suppresses LPS-induced expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α and iNOS) in a dose-dependent manner.
Amodiaquine (5 μM; 24 hours) significantly inhibits neurotoxin (6-OHDA-induced cell death in primary dopamine cells as examined by the number of TH neurons and dopamine uptake. The neuroprotective effect of Amodiaquine is also observed in rat PC12 cells.

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

RT-PCR

Cell Line:	Primary microglia
Concentration:	10 μM, 15 μM, 20 μM
Incubation Time:	4 hours
Result:	Suppressed LPS-induced expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α and iNOS) in a dose-dependent manner.

体内研究(In Vivo)

Amodiaquine (40 mg/kg; intraperitoneal injection; daily; for 3 days; male ICR mice) treatment diminishes perihematomal activation of microglia/macrophages and astrocytes. Amodiaquine also suppresses ICH-induced mRNA expression of IL-1β, CCL2 and CXCL2, and ameliorated motor dysfunction of mice.

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

Animal Model:	Male ICR mice (8-10?weeks of age) induced ntracerebral hemorrhage (ICH)
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection; daily; for 3 days
Result:	Diminished perihematomal activation of microglia/macrophages and astrocytes.

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]. Chun-Hyung Kim, et al. Nuclear receptor Nurr1 agonists enhance its dual functions and improve behavioral deficits in an animal model of Parkinsons disease. Proc Natl Acad Sci U S A. 2015 Jul 14;112(28):8756-61. [Information]

[2]. Keita Kinoshita, et al. A Nurr1 agonist amodiaquine attenuates inflammatory events and neurological deficits in a mouse model of intracerebral hemorrhage. J Neuroimmunol. 2019 May 15;330:48-54. [Information]

[3]. Akira Yokoyama, et al. Effect of amodiaquine, a histamine N-methyltransferase inhibitor, on, Propionibacterium acnes and lipopolysaccharide-induced hepatitis in mice. Eur J Pharmacol. 2007 Mar 8;558(1-3):179-84. [Information]

[4]. M T HOEKENGA. The treatment of acute malaria with single oral doses of amodiaquin, chloroquine, hydroxychloroquine and pyrimethamine. Am J Trop Med Hyg. 1954 Sep;3(5):833-8. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (215.14 mM; Need ultrasonic)

H₂O : 20 mg/mL (43.03 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1514 mL	10.7571 mL	21.5142 mL
5 mM	0.4303 mL	2.1514 mL	4.3028 mL
10 mM	0.2151 mL	1.0757 mL	2.1514 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： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.38 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.38 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

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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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