1. GPCR/G Protein
    Autophagy
  2. Angiotensin Receptor
    Autophagy
  3. Telmisartan

Telmisartan (Synonyms: BIBR 277)

Cat. No.: HY-13955 Purity: 99.96%
Handling Instructions

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.

For research use only. We do not sell to patients.

Telmisartan Chemical Structure

Telmisartan Chemical Structure

CAS No. : 144701-48-4

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10 mM * 1 mL in DMSO USD 79 In-stock
Estimated Time of Arrival: December 31
50 mg USD 72 In-stock
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100 mg USD 108 In-stock
Estimated Time of Arrival: December 31
500 mg USD 180 In-stock
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1 g USD 288 In-stock
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Customer Review

Top Publications Citing Use of Products

    Telmisartan purchased from MCE. Usage Cited in: Oncol Lett. 2018 Apr;15(4):5859-5864.

    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 MCE. 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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    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

    IC50: 9.2 nM (angiotensin II type 1 receptor)[1]

    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].

    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].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 6.67 mg/mL (12.96 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 0.67 mg/mL (1.30 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 0.67 mg/mL (1.30 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Cell Assay
    [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 has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [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 has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    514.62

    Formula

    C₃₃H₃₀N₄O₂

    CAS No.

    144701-48-4

    SMILES

    O=C(C1=CC=CC=C1C2=CC=C(CN3C4=CC(C5=NC6=CC=CC=C6N5C)=CC(C)=C4N=C3CCC)C=C2)O

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    Telmisartan
    Cat. No.:
    HY-13955
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    Telmisartan

    Cat. No.: HY-13955