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Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
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Telmisartan Chemical Structure
CAS No. : 144701-48-4
This product is a controlled substance and not for sale in your territory.
Based on 15 publication(s) in Google Scholar
Other Forms of Telmisartan:
Telmisartan-d3
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Telmisartan-d4
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Telmisartan-13C,d3
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Telmisartan-d7
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Telmisartan (Standard)
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Telmisartan purchased from MedChemExpress. Usage Cited in:
Oncol Lett. 2018 Apr;15(4):5859-5864.
[Abstract]
Western blot analysis of A549 cells treated with Telmisartan for 24 h. The band intensities are quantified. The results are normalized to the GAPDH loading control.
Telmisartan purchased from MedChemExpress. Usage Cited in:
Open Life Sci. 2018 Jul;13(1):242-249.
Expression of the apoptosis-related proteins including Bax, Bcl-2 and Cleaved Caspase-3 treated with Telmisartan in OS cells are determined by western blot analysis.
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AT1 Receptor AT2 Receptor
Description
Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
IC50 & Target
AT1 Receptor
In Vitro
In intact RVSMC cells and in membrane preparations, telmisartan inhibits the binding of 125I-AngII to AT1 receptors in a concentration-dependent manner, with an IC50 of 9.2 ± 0.8 nM. In the same experimental 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 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 treatment (100 μM) reduces the proliferation of three EAC cell lines (OE19, OE33, and SKGT-4), induces cell cycle arrest in G0/G1 phase and regulates cell cycle-related proteins in EAC cells, and induces the phosphorylation of AMPK and regulates cell cycle-related proteins via the AMPK/mTOR pathway in EAC cells. Telmisartan inhibits the activation of RTKs, downstream effectors and cell cycle-related proteins[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Telmisartan Related Antibodies
In Vivo
In the telmisartan (0.1, 0.3, and 1 mg/kg)-treated rats, the specific binding of [3H]telmisartan to the surface of living RVSMC is saturable and increases quickly to reach equilibrium within 1 h. Telmisartan dissociates very slowly from the receptor with a dissociation half-life (t1/2) of 75 min, which is comparable with candesartan and almost 5 times slower than angiotensin II (AngII). In vivo, telmisartan blunts the blood pressure response to exogenous AngII dose dependently[1]. Telmisartan (10 mg/kg/d) administration effectively suppresses aneurysm pathogenesis after PPE infusion as well, regardless of whether treatment is initiated before or after aneurysm creation or continues for a limited or extended time. Telmisartan treatment is associated with reduced messenger RNA levels for CCL5 and matrix metalloproteinases 2 and 9 in aneurysmal aortae, with no apparent effect on PPARγ-regulated gene expression[2]. Telmisartan (1 mg/kg/day) significantly ameliorates neuronal loss and the spatial acquisition impairment in 5XFAD mice, but without any changes of NeuN expression in the hippocampus layer. Telmisartan (1 mg/kg/day) treatment reduces amyloid burden and microglial accumulation in 5XFAD mice brain, induces microglial polarization towards neuroprotective phenotype, but does not alter the expression levels of NEP and IDE in 5XFAD mice specific brain areas[3]. Telmisartan (0.05, 0.1, 1 mg/kg, p.o.) shows significant reduction in immobility time, antagonizes depression and anxiety, and also significantly 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, miRNA expression is significantly altered by telmisartan in vivo[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Room temperature in continental US; may vary elsewhere.
Stockage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Solvant et solubilité
In Vitro:
DMSO : 6.67 mg/mL (12.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
1.9432 mL
9.7159 mL
19.4318 mL
5 mM
0.3886 mL
1.9432 mL
3.8864 mL
10 mM
0.1943 mL
0.9716 mL
1.9432 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (6.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% Corn Oil
This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (6.7 mg/mL) to 900 μLCorn oil, and mix evenly.
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution.
If precipitation or phase separation occurs during preparation,
heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 0.5% CMC-Na/saline water
Solubility: 3 mg/mL (5.83 mM); Suspended solution; Need ultrasonic
Protocol 2
Add each solvent one by one: 17% Solutol HS-15 in Saline
Solubility: 3.33 mg/mL (6.47 mM); Suspended solution; Need ultrasonic and warming
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[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.
[Content Brief]
[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.
[Content Brief]
[3]. Torika N, et al. Intranasal telmisartan ameliorates brain pathology in five familial Alzheimer's disease mice. Brain Behav Immun. 2017 Apr 3.
[Content Brief]
[4]. Aswar U, et al. Telmisartan attenuates diabetes induced depression in rats. Pharmacol Rep. 2017 Apr;69(2):358-364.
[Content Brief]
[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.
[Content Brief]
Test cellulaire
[5]
Cell proliferation is assayed using the CCK-8 cell counting kit. Briefly, 5×103 cells are seeded into each well of a 96-well plate and cultured in 100 μL of RPMI-1640 supplemented with 10% FBS. After 24 h, ARBs (telmisartan, irbesartan, losartan, and valsartan at 0, 1, 10, or 100 μM) or vehicle is added to each well, and cells are cultured for an additional 48 h. CCK-8 reagent (10 μL) is added to each well, and the plates are incubated at 37°C for 3 h. The absorbance is measured at 450 nm using a microplate reader.
MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Administration animale
[5]
Male athymic mice (BALB/c-nu/nu; 6 weeks old; 20-25 g) are maintained under specific pathogen-free conditions using a laminar airflow rack. The mice have continuous free access to sterilized (γ-irradiated) food and autoclaved water. Each mouse is subcutaneously inoculated with OE19 cells (5×106 cells per animal) in the flank. One week later, the xenografts are identifiable as masses with a maximal diameter > 4 mm. The animals are randomly assigned to treatment with telmisartan (50 μg per day) or diluent only (control). The telmisartan group is intraperitoneally (i.p.) injected five times per week with 2 mg/kg telmisartan for four weeks; the control group is administered 5% DMSO alone for four weeks. Tumor growth is monitored daily by the same investigators, and tumor size is measured weekly. The tumor volume (mm3) is calculated as the tumor length (mm) × tumor width (mm)2/2. All animals are sacrificed on day 22 after treatment, and all animals survive during this period. Between-group differences in tumor growth are analyzed by two-way ANOVA.
MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.
Références
[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.
[Content Brief]
[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.
[Content Brief]
[3]. Torika N, et al. Intranasal telmisartan ameliorates brain pathology in five familial Alzheimer's disease mice. Brain Behav Immun. 2017 Apr 3.
[Content Brief]
[4]. Aswar U, et al. Telmisartan attenuates diabetes induced depression in rats. Pharmacol Rep. 2017 Apr;69(2):358-364.
[Content Brief]
[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.
[Content Brief]
[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.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
1.9432 mL
9.7159 mL
19.4318 mL
48.5795 mL
5 mM
0.3886 mL
1.9432 mL
3.8864 mL
9.7159 mL
10 mM
0.1943 mL
0.9716 mL
1.9432 mL
4.8580 mL
Telmisartan Related Classifications
GPCR/G ProteinAutophagy
Angiotensin ReceptorAutophagy
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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