Astemizole

立即咨询

Astemizole

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

68844-77-9

包装与价格：

包装	价格(元)
10mM (in 1mL DMSO)	电议
50mg	电议
100mg	电议

产品介绍

化学性质

Physical Appearance	A solid
Storage	Store at -20°C
M.Wt	458.57
Cas No.	68844-77-9
Formula	C₂₈H₃₁FN₄O
Solubility	insoluble in H2O; ≥11.46 mg/mL in DMSO with gentle warming; ≥12.46 mg/mL in EtOH
Chemical Name	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
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。

资料参考

Astemizole是有效的抗组胺化合物，拮抗组胺H1受体，其IC50值为4 nM。其对毒蕈碱乙酰胆碱受体的抑制作用较低，其Ki值为2.4 M。

组胺H1受体是视紫红质样G蛋白偶联受体的一员，由生物胺组胺激活，并于全身表达，尤其是平滑肌、血管内皮细胞、中枢神经系统以及心脏。

Astemizole靶向肿瘤迁移所必须的蛋白，对Ether à go-go 1（Eag1）和Eag-related quality（Erg）钾离子通道具有特异性。此外，Eag1被认为是几种肿瘤的必要标记物。Astemizole抑制Eag1和Erg通道的作用，并在细胞内作用于Eag1通道，从而抑制肿瘤细胞在体内外的扩增。值得注意的是，几个罕见案例报道，Astemizole具有一些心血管反应。然而，Astemizole具有抗增殖活性并曾经用于临床，至今仍是一个非常有前景的抗恶性肿瘤药物。此外，基于Astemizole可以合成多种新型抗癌药物[1]。

参考文献：
1. Astemizole: an old anti-histamine as a new promising anti-cancer drug. Anticancer Agents Med Chem. 2011 Mar;11(3):307-14.

试验操作

Animal experiment:[1]
Animal models	Mice xenografted with the human breast cancer cell line T-47D and a primary breast cancer-derived cell culture (MBCDF)
Dosage form	50 mg/kg/day Administered by oral route for 3 weeks
Applications	Compared to untreated controls, astemizole and calcitriol significantly reduced, while the coadministration of both drugs further suppressed, tumor growth. In addition, the combined therapy significantly downregulated tumoral EAG1 and Ki-67 expression. Hence, in vivo dual targeting of the oncogenic EAG1 potassium channel by astemizole and calcitriol was able to enhance antineoplastic effects in breast tumors.
Note	The technical data provided above is for reference only.
	References: 1. García-Quiroz J, García-Becerra R, Santos-Martínez N, et al. In vivo dual targeting of the oncogenic Ether-à-go-go-1 potassium channel by calcitriol and astemizole results in enhanced antineoplastic effects in breast tumors. BMC Cancer, 2014, 14: 745.