Cat. No. Name Size Price Add Cart
KI1355Telmisartan50 mg$112
Telmisartan100 mg$192

Chemical Characteristic

Product NameTelmisartan
SynonymsMicardis
CAS No.144701-48-4
Molecular Weight 514.62
FormulaC33H30N4O2
Chemical Name2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid
Smilesc1(c(cccc1)C(=O)O)c1ccc(cc1)Cn1c(nc2c1cc(c1nc3c(n1C)cccc3)cc2C)CCC
Chemical Structure

Biological activities

Telmisartan is an angiotensin II receptor antagonist (angiotensin receptor blocker, ARB) used in the treatment of hypertension. Telmisartan is an angiotensin II receptor blocker that shows high affinity for the angiotensin II receptor type 1 (AT1), with a binding affinity 3000 times greater for AT1 than AT2. In addition to blocking the Renin-Angiotensin system (RAs), telmisartan also is a selective modulator of peroxisome proliferator-activated receptor gamma (PPAR-γ), a central regulator of insulin and glucose metabolism. Furthermore, telmisartan has the longest half life (24 hours) of all angiotensin II type 1 receptor antagonists so far.[1] In vitro, the specific binding of telmisartan to the surface of living rat vascular smooth muscle cells (RVSMC) is saturable and increases quickly to reach equilibrium within 60 minutes. Telmisartan dissociates very slowly from the angiotensin II receptor with a dissociation half-life (t1/2) of 75 minutes. In vivo, telmisartan at doses > 0.1 mg/kg has a long lasting blockade of the blood pressure response to exogenous angiotensin II and the blockade remains significant at 24 hours.[2]

Protocols

In vivo: Telmisartan is dissolved in 0.5% carboxymethylcellulose sodium.[2]

References

[1] Benson SC, et al. Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity. Hypertension. 2004, 43(5): 993-1002.
[2] 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, 302(3): 1089-1095.

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