Amodiaquine是一种4-氨基喹啉类化合物，主要用于疟疾的治疗，还具有抗炎、抗病毒作用。Amodiaquine是一种核受体Nurr1激动剂，EC50值约为20μM。
Cas No.:86-42-0
Sample solution is provided at 25 µL, 10mM.
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Amodiaquine is a 4-aminoquinoline compound primarily used for the treatment of malaria, and also possesses anti-inflammatory and antiviral effects[1]. Amodiaquine is a nuclear receptor Nurr1 agonist with an EC50 value of approximately 20μM[2]. Amodiaquine is a histamine N-methyltransferase inhibitor[3].
In vitro, treatment of primary CD4+ T cells isolated from mouse lymph nodes and spleen with Amodiaquine (10µM) for 24h and 48h inhibited the proliferation of Th1, Th2, Th17, and Treg cells induced by different exogenous cytokines and promoted T cell apoptosis[4]. Pretreatment of HKC-8 cells with Amodiaquine (10µM) for 1h improved the functional mitochondrial quality and the balance of mitochondrial fusion/fission protein expression[5].
In vivo, Amodiaquine (20mg/kg) administered intraperitoneally every other day for 14 weeks to diabetic mice effectively reduced proteinuria and histopathological changes in the kidneys of diabetic mice and increased the activity of 5′AMP-activated protein kinase (AMPK) in the kidneys[5]. Amodiaquine (40mg/kg) administered intraperitoneally three times in total (at 3h after induction of ICH and then daily at a 24-h interval) to mice with intracerebral hemorrhage (ICH), effectively reduced the activation of microglia/macrophages and astrocytes around the hematoma, inhibited the mRNA expression of ICH-induced IL-1β, CCL2 and CXCL2, and improved motor dysfunction in mice[6].
References:
[1] Romero A H, Delgado F. 4-Aminoquinoline as a privileged scaffold for the design of leishmanicidal agents: structure–property relationships and key biological targets[J]. Frontiers in Chemistry, 2025, 12: 1527946.
[2] Sai M, Hank E C, Tai H M, et al. Development of Nurr1 agonists from amodiaquine by scaffold hopping and fragment growing[J]. Communications Chemistry, 2024, 7(1): 149.
[3] Horton J R, Sawada K, Nishibori M, et al. Structural basis for inhibition of histamine N-methyltransferase by diverse drugs[J]. Journal of molecular biology, 2005, 353(2): 334-344.
[4] Oh S, Shin J H, Jang E J, et al. Anti-inflammatory activity of chloroquine and amodiaquine through p21-mediated suppression of T cell proliferation and Th1 cell differentiation[J]. Biochemical and biophysical research communications, 2016, 474(2): 345-350.
[5] Jeong H Y, Kang J M, Jun H H, et al. Chloroquine and amodiaquine enhance AMPK phosphorylation and improve mitochondrial fragmentation in diabetic tubulopathy[J]. Scientific Reports, 2018, 8(1): 8774.
[6] Kinoshita K, Matsumoto K, Kurauchi Y, et al. A Nurr1 agonist amodiaquine attenuates inflammatory events and neurological deficits in a mouse model of intracerebral hemorrhage[J]. Journal of Neuroimmunology, 2019, 330: 48-54.
Amodiaquine是一种4-氨基喹啉类化合物，主要用于疟疾的治疗，还具有抗炎、抗病毒作用[1]。Amodiaquine是一种核受体Nurr1激动剂，EC50值约为20μM[2]。Amodiaquine是一种组胺N-甲基转移酶抑制剂[3]。
在体外，Amodiaquine（10µM）处理从小鼠淋巴结和脾脏中分离的原代CD4+ T 细胞24h和48h，抑制了不同外源性细胞因子诱导的Th1、Th2、Th17和Treg细胞的增殖，促进了T细胞凋亡[4]。Amodiaquine（10µM）预处理HKC-8细胞1h，改善了细胞的功能性线粒体质量和线粒体融合/分裂蛋白表达的平衡[5]。
在体内，Amodiaquine（20mg/kg）每隔一天通过腹腔注射给药治疗糖尿病小鼠14周，有效减轻了糖尿病小鼠肾脏的蛋白尿和组织病理学改变，增加了肾脏中5′AMP激活蛋白激酶（AMPK）的活性[5]。Amodiaquine（40mg/kg，3次，首次给药是在诱导脑出血后3小时，之后每隔24小时给药一次）通过腹腔注射给药治疗脑内出血（ICH）小鼠，减少了小胶质细胞/巨噬细胞和星形胶质细胞的血肿周围活化，抑制了ICH诱导的IL-1β、趋化因子2（CCL2）和C-X-C基序趋化因子配体2（CXCL2）的mRNA表达，并改善了小鼠的运动功能障碍[6]。
| Cell experiment [1]: | |
Cell lines | Primary CD4+ T cells isolated from mouse lymph nodes and spleen |
Preparation Method | CD4+ T cells were isolated from lymph node and spleen using CD4 mini MACS beads and stimulated with plate-bound anti-CD3/anti-CD28 Ab (2μg/mL) in the presence of recombinant human IL-2 (rhIL-2, 10U/mL) for 24h. Cells were additionally treated with either 10µM Chloroquine (CQ) or Amodiaquine (AQ) for an additional 24h and 48h. IL-12 (2ng/mL), IL-4 (10ng/mL), TGF-β (5ng/mL) and IL-6 (10ng/mL), or TGF-β (5ng/mL) was added to the activated cells. Cell proliferation was detected by CFSE staining combined with flow cytometry. |
Reaction Conditions | 10µM; 24, 48h |
Applications | The addition of IL-12 and IL-4 induced highly proliferative Th1 and Th2 cell development respectively. TGF-β with IL-6 or TGF-β alone promoted activated CD4+ T cells to differentiate into Th17 or Treg cells. Amodiaquine can inhibit the proliferation of Th1, Th2, Th17 and Treg cells, and its effect is stronger than that of chloroquine. |
| Animal experiment [2]: | |
Animal models | C57/BL6J mice |
Preparation Method | Diabetes was induced in eight-week-old male C57/BL6J mice by the intraperitoneal injection of streptozotocin (STZ) at a dose of 50mg/kg for 5 consecutive days. In the intervention study, the following four groups of mice (n=5 in each group) were used for three separate experiments: (1) a normal control group, (2) a diabetic control group, (3) a diabetes+chloroquine (50mg/kg) group, and (4) a diabetes+Amodiaquine (20mg/kg) group. Chloroquine and Amodiaquine were dissolved in saline and administered to the mice at the indicated doses via intraperitoneal injections at 48-h intervals for 14 weeks beginning 2 weeks after STZ administration. All the mice were sacrificed 16 weeks after STZ administration, and their kidney tissues were collected for analysis. |
Dosage form | 20mg/kg; 14 weeks; i.p. |
Applications | Amodiaquine treatment effectively mitigated albuminuria and renal histopathologic changes and increased 5′ AMP-activated protein kinase (AMPK) activity in the kidneys of diabetic mice. |
References: | |
| Cas No. | 86-42-0 | SDF | |
| 别名 | 阿莫地喹,Amodiaquin | ||
| Canonical SMILES | OC(C=C1)=C(CN(CC)CC)C=C1NC2=CC=NC3=C2C=CC(Cl)=C3 | ||
| 分子式 | C20H22ClN3O | 分子量 | 355.9 |
| 溶解度 | DMF: 2.5 mg/ml,DMSO: 5 mg/ml,Ethanol: 2 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8098 mL | 14.0489 mL | 28.0978 mL |
| 5 mM | 562 μL | 2.8098 mL | 5.6196 mL |
| 10 mM | 281 μL | 1.4049 mL | 2.8098 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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