产品描述: | 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 |
靶点: |
EC50: ~20 μM (Nurr1-LBD (ligand binding domain)) Histamine N-methyltransferase;HistoneMethyltransferase; Parasite; HistamineReceptor |
体内研究: |
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 |
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 Parkinson's disease. Proc Natl Acad Sci U S A. 2015 Jul 14;112(28):8756-61. 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. 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. 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. |
溶解性: |
DMSO : 100 mg/mL (215.14 mM; Need ultrasonic) H2O : 20 mg/mL (43.03 mM; Need ultrasonic) |
保存条件: |
RT |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.151 ml |
10.757 ml |
21.514 ml |
5 mM |
0.43 ml |
2.151 ml |
4.303 ml |
10 mM |
0.215 ml |
1.076 ml |
2.151 ml |
50 mM |
0.043 ml |
0.215 ml |
0.43 ml |
|
注意: |
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