Catalog No.S1738 Synonyms: BIBR 277
Molecular Weight(MW): 514.62
Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension.
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|Description||Telmisartan is an angiotensin II receptor antagonist (ARB) used 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. Telmisartan causes a 60% to 70% decrease in the expression of ACC2 in murine muscle myotubes.  Telmisartan, but not candesartan, another ARB, downregulates RAGE mRNA levels in a dose-dependent manner. Telmisartan decreases basal as well as AGE-induced RAGE protein expression in Hep3B cells. Telmisartan dose-dependently inhibits AGE-induced ROS generation and subsequent CRP gene and protein induction in Hep3B cells.  Telmisartan effectively facilitates differentiation of 3T3-L1 preadipocytes. Telmisartan causes a dose-dependent increase in mRNA levels for PPARgamma target genes such as aP2 and adiponectin in both differentiating adipocytes and fully differentiated adipocytes. Telmisartan attenuates 11beta-hydroxysteroid dehydrogenase type 1 mRNA level in differentiated adipocytes. 
|In vivo||Telmisartan promotes increases in caloric expenditure and protects against dietary-induced weight gain in rats fed with a high-fat, high-carbohydrate diet. Telmisartan reduces the accumulation of visceral fat and decreases adipocyte size to a much greater extent than valsartan and is also associated with a significant reduction in hepatic triglyceride levels in rats fed with a high-fat, high-carbohydrate diet. |
|In vitro||DMSO||13 mg/mL (25.26 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02699645||Not yet recruiting||Acute Intracerebral Haemorrhage (ICH)||The George Institute||May 2017||Phase 4|
|NCT02968160||Recruiting||Metabolic Syndrome||Yuhan Corporation|Linical Korea||October 2016||Phase 4|
|NCT02768948||Not yet recruiting||Diabetic Nephropathy||Centre Hospitalier Universitaire de Nice||July 2016||--|
|NCT02620163||Completed||Hypertension||Yuhan Corporation||December 2015||Phase 3|
|NCT02734355||Completed||Atrial Fibrillation||Research Institute for Complex Problems of Cardiovascular Diseases, Russia||November 2015||Phase 4|
|NCT02933658||Completed||Hypertension and Dyslipidemia||Daewon Pharmaceutical Co., Ltd.||November 2015||Phase 1|
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