Telmisartan
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.
Cited by 2 Publications
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Biological Activity
| Description | Telmisartan is an angiotensin II receptor antagonist (ARB) used in the management of hypertension. | |||||||||||||||||||||||||||||||||||||
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| Targets |
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| In vitro |
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. [1] 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. [2] 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. [3] |
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| Cell Data |
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| 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. [4] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 13 mg/mL (25.26 mM) |
|---|---|---|
| Water | Insoluble | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 514.62 |
|---|---|
| Formula | C33H30N4O2 |
| CAS No. | 144701-48-4 |
| Storage | powder |
| in solvent | |
| Synonyms | BIBR 277 |
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Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT03705533 | Completed | Drug: Telmisartan|Drug: Micardis | Bioequivalence | Pharmtechnology LLC|Algorithme Pharma An Altasciences Company | September 7 2018 | Phase 1 |
| NCT03461081 | Completed | Drug: telmisartan/amlodipine and atorvastatin | Hypertension With Hyperlipidemia | Jeil Pharmaceutical Co. Ltd. | May 7 2017 | Phase 1 |
| NCT03116516 | Completed | Drug: Temisartan/Amlodipine+Rosuvastatin|Drug: YHP1604 | Hypertension|Hyperlipidemia | Yuhan Corporation | April 21 2017 | Phase 1 |
| NCT02951962 | Completed | Drug: Twynsta 80/5mg|Drug: Crestor 20mg | Hypertension|Hyperlipidemia | Yuhan Corporation | August 2016 | Phase 1 |
| NCT02608242 | Terminated | Drug: YH22189|Drug: Twynsta 80/10mg|Drug: Crestor 20mg | Hypertension|Hyperlipidemia | Yuhan Corporation | November 2015 | Phase 1 |
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