Telmisartan
Telmisartan is a long-acting antagonist at angiotensin II type 1 (AT II) receptors that is clinically used to treat hypertension. Telmisartan exhibits antihypertensive, anti-diabetic, anti-obesity, anti-inflammatory, and anti-hyperlipidemic activities. Telmisartan decreases levels of total cholesterol and LDL in vivo. Telmisartan also decreases weight gain and increases activity endurance and oxygen consumption in other animal models. This compound is also a selective modulator of PPARγ/δ, decreasing insulin, glucose, and triglyceride levels in high fat diet-fed rats. In endothelial cells, telmisartan decreases expression of MCP-1 and VCAM-1 and prevents activation of NF-κB.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/1897520
| Cas No. |
144701-48-4 |
|---|---|
| Purity |
≥98% |
| Formula |
C33H30N4O2 |
| Formula Wt. |
514.63 |
| Chemical Name |
4-[(1,4-Dimethyl-2-propyl[2,6-bi-1H-benzimidazol]-1-yl)methyl][1,1-biphenyl]-2-carboxylic acid |
| IUPAC Name |
2-[4-[[4-methyl-6-(1-methylbenzimidazol-2-yl)-2-propylbenzimidazol-1-yl]methyl]phenyl]benzoic acid |
| Synonym |
BIBR 277; Micardis; Pritor |
| Melting Point |
261-263°C |
| Solubility |
Soluble in DMSO (1.2mg/mL). Insoluble in water. Chloroform. |
| Appearance |
White to Off-White Crystalline Powder |
Xu S, Song H, Huang M, et al. Telmisartan inhibits the proinflammatory effects of homocysteine on human endothelial cells through activation of the peroxisome proliferator-activated receptor-δ pathway. Int J Mol Med. 2014 Sep;34(3):828-34. PMID: 24994548.
Sueta D, Koibuchi N, Hasegawa Y, et al. Telmisartan Exerts Sustained Blood Pressure Control and Reduces Blood Pressure Variability in Metabolic Syndrome by Inhibiting Sympathetic Activity. Am J Hypertens. 2014 May 28. [Epub ahead of print]. PMID: 24871627.
Feng X, Luo Z, Ma L, et al. Angiotensin II receptor blocker telmisartan enhances running endurance of skeletal muscle through activation of the PPAR-δ/AMPK pathway. J Cell Mol Med. 2011 Jul;15(7):1572-81. PMID: 20477906.
Inoue T, Taguchi I, Abe S, et al. Inhibition of intestinal cholesterol absorption might explain cholesterol-lowering effect of telmisartan. J Clin Pharm Ther. 2011 Feb;36(1):103-10. PMID: 21198725.
Benson SC, Pershadsingh HA, Ho CI, et al. Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating activity. Hypertension. 2004 May;43(5):993-1002. PMID: 15007034.
Okada M, Kosaka N, Hoshino Y, et al. Effects of captopril and telmisartan on matrix metalloproteinase-2 and -9 expressions and development of left ventricular fibrosis induced by isoprenaline in rats. Biol Pharm Bull. 2010;33(9):1517-1521. PMID: 20823567.
