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/ Telmisartan/替米沙坦

Telmisartan/替米沙坦 {[allProObj[0].p_purity_real_show]}

货号：A219723 同义名： BIBR 277; Micardis

Telmisartan is an angiotensin II receptor antagonist with Ki value of 3.7nM, used in the management of hypertension with elimination half-life‎ of ‎24 hours.

Telmisartan/替米沙坦 化学结构 CAS号：144701-48-4
Telmisartan/替米沙坦 化学结构
CAS号：144701-48-4
Telmisartan/替米沙坦 3D分子结构
CAS号：144701-48-4
Telmisartan/替米沙坦 化学结构 CAS号：144701-48-4
Telmisartan/替米沙坦 3D分子结构 CAS号：144701-48-4
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Telmisartan/替米沙坦 纯度/质量文件 产品仅供科研

货号：A219723 标准纯度： {[allProObj[0].p_purity_real_show]}
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Telmisartan/替米沙坦 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].

Telmisartan/替米沙坦 细胞研究

细胞系 浓度 检测类型 检测时间 活性说明 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
HepG2 cells Function assay Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50=0.025 μM 22586124

Telmisartan/替米沙坦 动物研究

Animal study In rats treated with telmisartan (0.1, 0.3, and 1 mg/kg), the specific binding of [3H]telmisartan to the surface of living RVSMC saturates rapidly and reaches equilibrium within 1 hour. Telmisartan exhibits slow dissociation from the receptor, with a dissociation half-life (t1/2) of 75 minutes, comparable to candesartan and nearly 5 times slower than angiotensin II (AngII).in vivo, telmisartan dose-dependently attenuates the blood pressure response to exogenous AngII [1].Telmisartan (10 mg/kg/day) effectively inhibits aneurysm pathogenesis following PPE infusion, irrespective of whether treatment commences before or after aneurysm induction or is maintained for a short or prolonged duration. Telmisartan therapy is linked to decreased mRNA levels of CCL5 and matrix metalloproteinases 2 and 9 in aneurysmal aortae, without observable impact on PPARγ-regulated gene expression [2].Telmisartan (1 mg/kg/day) significantly ameliorates neuronal loss and spatial acquisition impairment in 5XFAD mice, without altering NeuN expression in the hippocampus layer. Telmisartan treatment also reduces amyloid burden and microglial accumulation in the brain of 5XFAD mice, induces microglial polarization towards a neuroprotective phenotype, but does not alter the expression levels of NEP and IDE in specific brain areas of 5XFAD mice [3].Telmisartan (0.05, 0.1, 1 mg/kg, pO.) significantly reduces immobility time, antagonizes depression and anxiety, and attenuates serum cortisol, NO, IL-6, and IL-1β in rats [4].Telmisartan (50 μg, i.p.) leads to a 73.2% reduction in tumor growth in mice bearing xenografts derived from OE19 cells. Furthermore, telmisartan significantly alters miRNA expressionin vivo[5].

Telmisartan/替米沙坦 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 <<

Telmisartan/替米沙坦 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.

Telmisartan/替米沙坦 实验方案

计算器
存储液制备 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

Telmisartan/替米沙坦 技术信息

CAS号144701-48-4
分子式C33H30N4O2
分子量 514.62
SMILES Code O=C(C1=CC=CC=C1C2=CC=C(CN3C4=CC(C5=NC6=CC=CC=C6N5C)=CC(C)=C4N=C3CCC)C=C2)O
MDL No. MFCD00918125
别名 BIBR 277; Micardis; Kinzalmono; Pritor
运输蓝冰
InChI Key RMMXLENWKUUMAY-UHFFFAOYSA-N
Pubchem ID 65999
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, room temperature
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案一
方案二

Tags: Telmisartan | 144701-48-4 | BIBR 277 | BIBR277 | BIBR-277 | GPCR/G Protein | Autophagy | Angiotensin Receptor | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Telmisartan/替米沙坦 纯度/质量文件 | Telmisartan/替米沙坦 生物活性 | Telmisartan/替米沙坦 细胞研究 | Telmisartan/替米沙坦 临床数据 | Telmisartan/替米沙坦 参考文献 | Telmisartan/替米沙坦 实验方案 | Telmisartan/替米沙坦 技术信息

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