| CAS NO: | 6398-98-7 |
| 包装 | 价格(元) |
| 100mg | 电议 |
| 500mg | 电议 |
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 464.81 |
| Cas No. | 6398-98-7 |
| Formula | C20H28Cl3N3O3 |
| Solubility | ≥18.03 mg/mL in H2O with ultrasonic; ≥5.9 mg/mL in EtOH with ultrasonic; ≥70.4 mg/mL in DMSO |
| Chemical Name | 4-((7-chloroquinolin-4-yl)amino)-2-((diethylamino)methyl)phenol dihydrochloride dihydrate |
| Canonical SMILES | CCN(CC1=CC(NC2=C3C=CC(Cl)=CC3=NC=C2)=CC=C1O)CC.Cl.Cl.O.O |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 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。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
Amodiaquine dihydrochloride dihydrate is a potent inhibitor of histamineN-methyltransferase (HNMT), with estimatedKi of 18.6 nM [1].
HNMT occurs ubiquitously in vertebrate species, and is widely expressed in mammalian tissues with particularly high expression levels in kidney, liver, colon, prostate, ovary, and spinal cord cells. HNMT is a cytosolic protein that is responsible for the intracellular inactivation of histamine [1].
Over the concentration range 10-3 ~ 10-8 M, amodiaquine was a significantly more potent inhibitor than other compounds including chlorhexidine, producing 80% inhibition on rat kidney HNMT at 10-6 M whilst the next best inhibitor at this concentration, chlorhexidine, produced only 27% inhibition. [2].
In mice withPropionibacterium acnes-primed and lipopolysaccharide-induced hepatitis, the subcutaneous injection of amodiaquine at 2 and 5 mg/kg significantly increased the histamine levels in the liver. Pretreatment with amodiaquine also improved the survival rate of the hepatitis mice, which was partially associated with the decrease in serum levels of aspartate aminotransferase and alanine aminotransferase [3].
References:
[1]. Horton J R, Sawada K, Nishibori M, et al. Structural basis for inhibition of histamine N-methyltransferase by diverse drugs. Journal of Molecular Biology, 2005, 353(2): 334-344.
[2]. Harle D G, Baldo B A. Structural features of potent inhibitors of rat kidney histamine N-methyltransferase. Biochemical Pharmacology, 1988, 37(3): 385-388.
[3]. Yokoyama A, Mori S, Takahashi H K, et al. Effect of amodiaquine, a histamine N-methyltransferase inhibitor, on, Propionibacterium acnes and lipopolysaccharide-induced hepatitis in mice. European Journal of Pharmacology, 2007, 558(1-3): 179-184.
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