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Telmisartan

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Chemical Structure| 144701-48-4 同义名 : BIBR 277;Micardis;Kinzalmono;Pritor
CAS号 : 144701-48-4
货号 : A219723
分子式 : C33H30N4O2
纯度 : 98%
分子量 : 514.617
MDL号 : MFCD00918125
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 5 mg/mL(9.72 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • AT2 receptor
描述 In intact RVSMC cells and membrane preparations, telmisartan demonstrates concentration-dependent inhibition of 125I-AngII binding to AT1 receptors, exhibiting an IC50 of 9.2 ± 0.8 nM. Under the same conditions, angiotensin II displaces 125I-AngII with an IC50 value of 2.9 ± 0.5 nM. The specific binding of [3H]telmisartan to SMC membranes is competitively displaced by unlabeled telmisartan with an IC50 of 7.7 ± 1.8 nM and by cold AngII with an IC50 of 32.7 ± 5.7 nM [1]. Telmisartan (100 μM) decreases the proliferation of three EAC cell lines (OE19, OE33, and SKGT-4), induces cell cycle arrest in G0/G1 phase, regulates cell cycle-related proteins, promotes AMPK phosphorylation, and modulates cell cycle-related proteins through the AMPK/mTOR pathway in EAC cells. Telmisartan also inhibits the activation of RTKs, downstream effectors, and cell cycle-related proteins [5].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CHO cells Function assay Antagonist activity at human AT1 receptor expressed in CHO cells measured after overnight incubation by luciferase reporter gene assay, IC50=0.002 μM 24462665
CV1 cells Function assay Agonist activity at human PPARgamma expressed in african green monkey CV1 cells by Gal4 transactivation assay, EC50=2.02 μM 20079636
HEK293 cells Function assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50=17.9 μM 23241029
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01392534 - Completed - Poland ... 展开 >> Many Locations, Poland 收起 <<
NCT02177500 Hypertension Phase 3 Completed - -
NCT02129192 Healthy Phase 1 Completed - Japan ... 展开 >> Boehringer Ingelheim Investigational Site Tokyo, Hachioji, Japan 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.72mL

1.94mL

0.97mL

19.43mL

3.89mL

1.94mL
参考文献

[1]Maillard MP, et al. In vitro and in vivo characterization of the activity of telmisartan: an insurmountable angiotensin II receptor antagonist. J Pharmacol Exp Ther. 2002 Sep;302(3):1089-95.

[2]Xuan H, et al. Inhibition or deletion of angiotensin II type 1 receptor suppresses elastase-induced experimental abdominal aortic aneurysms. J Vasc Surg. 2017 Apr 20. pii: S0741-5214(17)30100-3.

[3]Torika N, et al. Intranasal telmisartan ameliorates brain pathology in five familial Alzheimer's disease mice. Brain Behav Immun. 2017 Apr 3.

[4]Aswar U, et al. Telmisartan attenuates diabetes induced depression in rats. Pharmacol Rep. 2017 Apr;69(2):358-364.

[5]Fujihara S, et al. The angiotensin II type 1 receptor antagonist telmisartan inhibits cell proliferation and tumor growth of esophageal adenocarcinoma via the AMPKα/mTOR pathway in vitro and in vivo. Oncotarget. 2017 Jan 31;8(5):8536-8549.