Telmisartan; BIBR277;BIBR 277; BIBR-277; Kinzalmono; Micardis;
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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10g |
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Other Sizes |
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Purity: ≥98%
Telmisartan (formerly BIBR-277; BIBR 277; BIBR277; Kinzalmono; Micardis) is a long lasting angiotensin II receptor antagonist (ARB) approved for use in the management of hypertension. Telmisartan functions as a moderately potent (EC50=4.5 μM), selective PPARγ partial agonist, activating the receptor to 25% to 30% of the maximum level achieved by the full agonists pioglitazone and rosiglitazone. Telmisartan induces adipocyte differentiation of 3T3-L1 cells and causes a 60% decrease in the expression of ACC2 in murine muscle myotubes.
ln Vitro |
In intact RVSMC cell and membrane preparations, telmisartan inhibits 125I-AngII binding to the AT1 receptor in a concentration-dependent manner with an IC50 of 9.2 ± 0.8 nM. The IC50 value was 2.9 ± 0.5 nM when angiotensin II took the place of 125I-AngII under the same experimental circumstances. Unlabeled Telmisartan and cold AngII, with IC50 values of 7.7 ± 1.8 nM and 32.7 ± 5.7 nM, respectively, replaced the specific binding of [3H]Telmisartan to SMC membranes [1]. Treatment with telmisartan (100 μM) inhibits the growth of three EAC cell lines (OE19, OE33, and SKGT-4), causes cell cycle arrest in G0/G1 phase, controls proteins related to the cell cycle in EAC cells, and activates AMPK and mTOR pathway in cells. RTKs, downstream effectors, and cell cycle-related proteins are all inhibited by telmisartan [5].
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ln Vivo |
The specific binding of [3H]Telmisartan to the surface of live RVSMC was saturated and increased quickly to approach equilibrium within 1 hour in rats treated with Telmisartan (0.1, 0.3, and 1 mg/kg). With a dissociation half-life (t1/2) of 75 minutes, telmisartan dissociates from the receptor very slowly—nearly five times slower than angiotensin II (AngII) and comparable to candesartan. Telmisartan reduces the blood pressure response to exogenous AngII in vivo in a dose-dependent manner [1]. Regardless of whether therapy was started prior to or following aneurysm formation, or if it was continued for a brief or prolonged duration, telmisartan (10 mg/kg/day) was also successful in preventing aneurysm pathogenesis following PPE infusion. In aneurysmal aortas, telmisartan treatment was linked to lower messenger RNA levels of CCL5 and matrix metalloproteinases 2 and 9, but it had no discernible impact on the expression of genes controlled by PPARγ [2]. In 5XFAD animals, telmisartan (1 mg/kg/day) dramatically reduced neuron loss and spatial acquisition impairment, although NeuN expression in the hippocampus remained unchanged. 5XFAD mice's brains had less amyloid and microglia buildup when treated with telmisartan (1 mg/kg/day), which also causes microglia to polarize toward a neuroprotective phenotype. However, 5XFAD mice remain the same. NEP and IDE expression levels in particular brain areas [3]. Rats' immobility time is greatly reduced by telmisartan (0.05, 0.1, 1 mg/kg, po), which also adversely affects sadness and anxiety in addition to significantly lowering rats' blood cortisol, NO, IL-6, and IL-1β [4]. In mice bearing xenografts produced from OE19 cells, telmisartan (50 μg, ip) lowers tumor growth by 73.2%. Furthermore, the expression of miRNA was considerably changed in vivo by telmisartan [5].
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Animal Protocol |
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References |
[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 |
Molecular Formula |
C33H30N4O2
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Molecular Weight |
514.62
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CAS # |
144701-48-4
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Related CAS # |
Telmisartan-d3;1189889-44-8;Telmisartan-d7;1794754-60-1;Telmisartan-d4;Telmisartan-13C,d3;1261396-33-1
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O([H])C(C1=C([H])C([H])=C([H])C([H])=C1C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])N1C(C([H])([H])C([H])([H])C([H])([H])[H])=NC2C(C([H])([H])[H])=C([H])C(C3=NC4=C([H])C([H])=C([H])C([H])=C4N3C([H])([H])[H])=C([H])C1=2)=O
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Chemical Name |
4-((1,7-dimethyl-2-propyl-1H,3H-[2,5-bibenzo[d]imidazol]-3-yl)methyl)-[1,1-biphenyl]-2-carboxylic acid
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.67 mg/mL (1.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.67 mg/mL (1.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 6.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 3 mg/mL (5.83 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: 3.33 mg/mL (6.47 mM) in 17% Polyethylene glycol 12-hydroxystearate in Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.