Telmisartan (BIBR 277)

Alias:

Telmisartan; BIBR277;BIBR 277; BIBR-277; Kinzalmono; Micardis;

Cat No.:V1775 Purity: ≥98%
Telmisartan (formerly BIBR-277;BIBR 277; BIBR277;Kinzalmono; Micardis)is along lasting angiotensin II receptor antagonist (ARB) approved for use in the management of hypertension.
Telmisartan (BIBR 277) Chemical Structure CAS No.: 144701-48-4
Product category: RAAS
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
500mg
1g
10g
Other Sizes

Other Forms of Telmisartan (BIBR 277):

  • Telmisartan-d3 (Telmisartan d3)
  • Telmisartan-d7 (BIBR 277-d7)
  • Telmisartan-13C,d3
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
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].
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].
Animal Protocol

Rats
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
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C33H30N4O2
Molecular Weight
514.62
CAS #
144701-48-4
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
Chemical Name
4-((1,7-dimethyl-2-propyl-1H,3H-[2,5-bibenzo[d]imidazol]-3-yl)methyl)-[1,1-biphenyl]-2-carboxylic acid
Synonyms

Telmisartan; BIBR277;BIBR 277; BIBR-277; Kinzalmono; Micardis;

Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 13 mg/mL (25.3 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
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.

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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.

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