生物活性
|
产品描述 |
SUN 1334H is a potent, orally active, highly selective antagonist of H1 receptor(Ki of 9.7 nM). |
|
靶点活性 |
H1 receptor(ki),ki： 9.7 nM |
|
体外活性 |
In CHO-K1/hERG cells,SUN-1334H causes potent inhibition of histamine induced contractions of isolated guinea-pig ileum(IC50 : 0.198 μM)[2]. |
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体内活性 |
In beagle dogs and ovalbumin-induced rhinitis in guinea pigs, SUN-1334H potently inhibits histamine-induced bronchospasm over 24 hours following oral administration and completely suppresses histamine-induced skin wheal [1]. SUN-1334H shows potent reduction of passive and active cutaneous anaphylactic reactions in skin allergy models. In central nervous system side effects models, SUN-1334H, desloratadine and fexofenadine are devoid of any significant effects[2]. |
化学信息
|
分子量 |
489.38 |
|
分子式 |
C23H28Cl2F2N2O3 |
|
CAS |
607736-84-5 |
|
溶解度 |
（ < 1 mg/ml refers to the product slightly soluble or insoluble ) |
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储存条件 |
store at -80°C |
|
备注 |
For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
配制溶液
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.043 ml | 10.217 ml | 20.434 ml |
| 5 mM | 0.409 ml | 2.043 ml | 4.087 ml |
| 10 mM | 0.204 ml | 1.022 ml | 2.043 ml |
| 50 mM | 0.041 ml | 0.204 ml | 0.409 ml |
参考文献
- 1. Mandhane SN, et al. Preclinical efficacy and safety pharmacology of SUN-1334H, a potent orally active antihistamine agent. Drugs R D. 2008;9(2):93-112.
- 2. Mandhane SN, et al. Characterization of anti-inflammatory properties and evidence for no sedation liability for the novel antihistamine SUN-1334H. Int Arch Allergy Immunol. 2010;151(1):56-69.
产品操作手册
