Astemizole是一种强效抗组胺化合物，可拮抗组胺H1受体，IC50值为4nM。
Cas No.:68844-77-9
Sample solution is provided at 25 µL, 10mM.
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Astemizole is a potent anti-histamine compound that antagonizes the histamine H1-receptor with an IC50 value of 4nM [1]. Astemizole can inhibit the KCa1.1 potassium ion channel in osteosarcoma cells, with an IC50 value of 0.135μM [2]. Astemizole has been widely used as an anti-cancer agent, inhibiting the growth of various tumor cells[3].
In vitro, Astemizole treatment for 6 days significantly inhibited cell death in BT-474 cells, with an IC50 value of 1.72μM[4]. 1µM of Astemizole was pre-treated for 12 hours, which significantly restored the viability of human umbilical vein endothelial cells (HUVECs) under oxidative stress and eliminated the intracellular reactive oxygen species (ROS) induced by H2O2[5]. Treatment with 5µM Astemizole for 96 hours can target the expression of Eag1 protein, induce apoptosis in HeLa cells, and inhibit cell proliferation[6].
In vivo, Astemizole treatment for 7 days (20mg/kg/day; p.o.) can effectively reverse the leakage of albumin across the blood-retinal barrier in experimental diabetes[7]. Oral administration of 50mg/kg of Astemizole daily for 12 weeks significantly inhibited the occurrence of hepatocellular carcinoma (HCC) in rats induced by diethylnitrosamine[8].
References:
[1] Laduron P M, Janssen P F, Gommeren W, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole[J]. Molecular Pharmacology, 1982, 21(2): 294-300.
[2] Mészáros B, Csoti A, Szanto T G, et al. The hEag1 K+ Channel Inhibitor Astemizole Stimulates Ca2+ Deposition in SaOS-2 and MG-63 Osteosarcoma Cultures[J]. International journal of molecular sciences, 2022, 23(18): 10533.
[3] Garcia-Quiroz J, Camacho J. Astemizole: an old anti-histamine as a new promising anti-cancer drug[J]. Anti-Cancer Agents in Medicinal Chemistry-Anti-Cancer Agents), 2011, 11(3): 307-314.
[4] García-Quiroz J, González-González M E, Díaz L, et al. Astemizole, an inhibitor of ether-à-go-go-1 potassium channel, increases the activity of the tyrosine kinase inhibitor gefitinib in breast cancer cells[J]. Revista de investigación clínica, 2019, 71(3): 186-194.
[5] Tian J N, Shi X D, Wang X K, et al. Astemizole protects against human umbilical vein endothelial cell injury induced by hydrogen peroxide via the p53 signaling pathway[J]. Molecular Medicine Reports, 2017, 15(6): 4286-4290.
[6] de Guadalupe Chávez-López M, Hernández-Gallegos E, Vázquez-Sánchez A Y, et al. Antiproliferative and proapoptotic effects of astemizole on cervical cancer cells[J]. International Journal of Gynecological Cancer, 2014, 24(5): 824-828.
[7] Hollis T M, Sill H W, Butler C, et al. Astemizole reduces blood-retinal barrier leakage in experimental diabetes[J]. Journal of diabetes and its complications, 1992, 6(4): 230-235.
[8] de Guadalupe Chavez-Lopez M, Pérez-Carreón J I, Zuñiga-García V, et al. Astemizole-based anticancer therapy for hepatocellular carcinoma (HCC), and Eag1 channels as potential early-stage markers of HCC[J]. Tumor Biology, 2015, 36(8): 6149-6158.
Astemizole是一种强效抗组胺化合物，可拮抗组胺H1受体，IC50值为4nM[1]。Astemizole能抑制骨肉瘤细胞中的KCa1.1钾离子通道，IC50值为0.135µM[2]。Astemizole已被广泛用作抗癌剂，抑制多种肿瘤细胞的生长[3]。
在体外，Astemizole处理6天显著抑制了BT-474细胞的死亡，IC50值为1.72µM[4]。预处理1µM的Astemizole 12小时，显著恢复了氧化应激下的人脐静脉内皮细胞（HUVECs）活力，并消除了由H2O2诱导的细胞内活性氧（ROS）[5]。使用5µM的Astemizole处理96小时，可靶向抑制Eag1蛋白的表达，诱导HeLa细胞凋亡，并抑制细胞增殖[6]。
在体内，口服给予20mg/kg/day剂量的Astemizole，持续7天，能有效逆转实验性糖尿病中白蛋白跨血-视网膜屏障的渗漏[7]。每日口服50mg/kg剂量的Astemizole，连续12周，显著抑制了diethylnitrosamine诱导的大鼠肝细胞癌（HCC）的发生[8]。
| Cell experiment [1]: | |
Cell lines | BT-474 cells |
Preparation Method | BT-474 cells were maintained in Hybri-Care medium supplemented with 1.5g/l sodium bicarbonate, 100units/ml penicillin plus 100µg/ml streptomycin, and heat-inactivated FBS to a final concentration of 10% in humidified atmosphere with 5% CO2 at 37°C. Cells were seeded in 96-well plates at a density of 1000 cells per well. After 24h, cells were incubated in the presence of different concentrations of Astemizole (0, 0.5, 1, 1.5, 2.0, 2.5μM), or the vehicle alone (DMSO) during 6 days. Cell proliferation was measured. |
Reaction Conditions | 0, 0.5, 1, 1.5, 2.0, 2.5μM; 6 days |
Applications | Astemizole treatment reduced the cell viability of BT-474 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | Male Wistar rats weighing 200g received intraperitoneal injections of Diethylnitrosamine (50mg/kg) once a week for 12 weeks. Oral administration of Astemizole (50mg/kg) was given daily for 12 weeks. The control group received PBS. Mice were weighed weekly. At the end of treatments, mice were sacrificed by decapitation. Livers were rapidly removed weighed, and photographed. |
Dosage form | 50mg/kg/day for 12 weeks; p.o. |
Applications | Astemizole treatment prevented diethylnitrosamine-induced rat HCC development in rats. |
References: | |
| Cas No. | 68844-77-9 | SDF | |
| 别名 | 阿司咪唑; R 43512 | ||
| 化学名 | 1-(4-fluorobenzyl)-N-(1-(4-methoxyphenethyl)piperidin-4-yl)-1H-benzo[d]imidazol-2-amine | ||
| Canonical SMILES | FC1=CC=C(C=C1)CN2C(NC3CCN(CCC(C=C4)=CC=C4OC)CC3)=NC5=CC=CC=C25 | ||
| 分子式 | C28H31FN4O | 分子量 | 458.57 |
| 溶解度 | ≥ 11.5mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1807 mL | 10.9035 mL | 21.8069 mL |
| 5 mM | 436.1 μL | 2.1807 mL | 4.3614 mL |
| 10 mM | 218.1 μL | 1.0903 mL | 2.1807 mL |
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