货号	规格	价格	上海	北京	珠海	重庆	武汉
S87909-5mg促销	99.50%	￥180.00 ￥144.00 S87909-5mg ￥144.00 现货	6 6	-	-	-	-
S87909-10mg促销	99.50%	￥280.00 ￥224.00 S87909-10mg ￥224.00 现货	4 4	-	-	-	-
S87909-25mg促销	99.50%	￥500.00 ￥400.00 S87909-25mg ￥400.00 现货	7 7	-	-	-	-
S87909-50mg促销	99.50%	￥750.00 ￥600.00 S87909-50mg ￥600.00 现货	4 4	-	-	-	-
S87909-100mg促销	≥98%	￥1200.00 ￥960.00 S87909-100mg ￥960.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Astemizole (R 43512), a second-generation antihistamine drug to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects

靶点：

Histamine Receptor;Potassium Channel;PotassiumChannel; HistamineReceptor

体内研究：

Astemizole (p.o., 10 and 30 mg/kg) and (i.v., 1 and 3 mg/kg) has no effect on respiratory rate, heart rate and blood pressure, and even at high doses of 30 mg/kg and 3 mg/kg, also has no effect on body temperature and exercise capacity in male common marmosets. But Astemizole can prolong the QT interval and induce premature ventricular contractions at 30 mg/kg (po) and 1 mg/kg (iv). Astemizole (p.o., 3 and 30 mg/kg) shows that the pre-drug control values (C) of the idioventricular rate, QT interval and QTcF are 31 beats/min, 319 ms and 256 at dose of 3 mg/kg, while those are 31 beats/min, 331 ms and 270 at dose of 30 mg/kg, respectively in mice. Moreover, Astemizole at a dose of 30 mg/kg (po) may cause tip-twisting ventricular tachycardia by inhibiting hERG K+ channels

参考文献：

1. Laduron PM, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol Pharmacol. 1982 Mar;21(2):294-300. 2. Richards DM, et al. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28(1):38-61. 3. Ikuo Horii, et al. Development of telemetry system in the common marmoset--cardiovascular effects of astemizole and nicardipine. J Toxicol Sci. 2002 May;27(2):123-30. 4. Hiroko Izumi-Nakaseko, et al. Possibility as an anti-cancer drug of astemizole: Evaluation of arrhythmogenicity by the chronic atrioventricular block canine model. J Pharmacol Sci. 2016 Jun;131(2):150-3.

溶解性：

Soluble in DMSO

保存条件：

RT,避光

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.181 ml	10.903 ml	21.807 ml
5 mM	0.436 ml	2.181 ml	4.361 ml
10 mM	0.218 ml	1.09 ml	2.181 ml
50 mM	0.044 ml	0.218 ml	0.436 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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