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CAS No.: 69-44-3

Amodiaquine 2HCl Catalog No. CSN23394

Synonyms: Amodiaquin dihydrochloride;Amodiaquine hydrochloride

Amodiaquine 2HCl is a 4-aminoquinoline similar to chloroquine with both anti-malarial and anti-inflammatory effect used to treat malaria.

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技术信息

生物活性

描述Amodiaquine 2HCl, a 4-aminoquinoline class of antimalarial agent, is a potent and orally active histamine N-methyltransferase inhibitor with a Ki of 18.6 nM. Amodiaquine 2HCl is also a Nurr1 agonist and specifically binds to Nurr1-LBD (ligand binding domain) with an EC50 of ~20 μM. Anti-inflammatory effect^[1]. The subcutaneous injection of amodiaquine (2 and 5 mg/kg) significantly increased the histamine levels in the liver in comparison to saline treated mice. Pretreatment with amodiaquine also improved the survival rate of the hepatitis mice. Amodiaquine partially suppressed increases of tumor necrosis factor (TNF)-alpha in the serum and TNF-alpha mRNA expression in the liver, whereas the expression of interleukin (IL)-18, interferon (IFN)-gamma and IL-12 in the liver was not changed by amodiaquine treatment^[2]. Daily administration of a Nurr1 agonist amodiaquine (40 mg/kg, i.p.) from 3 h after ICH (intracerebral hemorrhage) induction diminished perihematomal activation of microglia/macrophages and astrocytes. Amodiaquine also suppressed ICH-induced mRNA expression of IL-1β, CCL2 and CXCL2, and ameliorated motor dysfunction of mice^[3].
参考文献

[1] HOEKENGA MT. 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
[2] Yokoyama A, Mori S, Takahashi HK, Kanke T, Wake H, Nishibori M. 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
[3] Kinoshita K, Matsumoto K, Kurauchi Y, Hisatsune A, Seki T, Katsuki H. 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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3322 mL
- 11.6610 mL
- 23.3220 mL
- 5 mM
- 0.4664 mL
- 2.3322 mL
- 4.6644 mL
- 10 mM
- 0.2332 mL
- 1.1661 mL
- 2.3322 mL

技术信息

CAS号

69-44-3

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H24Cl3N3O

运输

蓝冰

分子量

428.78

别名

Amodiaquin dihydrochloride;Amodiaquine hydrochloride

溶解度

DMSO	56.0 mg/mL (130.6 mM)

动物实验配方

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