Home GPCR & G Protein Angiotensin Receptor antagonist Telmisartan

Telmisartan

Catalog No.S1738 Synonyms: BIBR 277

For research use only.

Telmisartan (BIBR 277) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension.

Telmisartan Chemical Structure

CAS No. 144701-48-4

Selleck's Telmisartan has been cited by 6 Publications

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Biological Activity

Description Telmisartan (BIBR 277) is an angiotensin II receptor antagonist (ARB) used in the management of hypertension.
Targets
angiotensin II receptor [1]
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]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO cells NUTnfmNYTnWwY4Tpc44h[XO|YYm= M2rHWWFvfGGpb37pd5Qh[WO2aY\peJkh[XRiaIXtZY4hSVRzIILlZ4VxfG:{IHX4dJJme3OnZDDpckBEUE9iY3XscJMhdWWjc4Xy[YQh[W[2ZYKgc5Zmem6rZ3j0JIlv[3WkYYTpc44h[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUCuNFAzKM7:TR?= MmnaNlQ1PjJ4NkW=
HepG2 cells NIPPTmtHfW6ldHnvckBie3OjeR?= MlvITY5pcWKrdHnvckBw\iCuaY\ldkB{fGGpZTDQcIF{dW:maYXtJIJmemeqZXmgbY5n\WO2aX;uJIlvKEincFeyJINmdGy|LDDJR|UxRTBwMEK1JO69VQ>? NGDmZZMzOjV6NkGyOC=>
CV1 cells MnrrSpVv[3Srb36gZZN{[Xl? NEi5[nVC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHBRSVKpYX3tZUBmgHC{ZYPz[YQhcW5iYX\ybYNidiCpcnXlckBud26tZYmgR3YyKGOnbHzzJIJ6KEejbESgeJJidnOjY4TpeoF1cW:wIHHzd4F6NCCHQ{WwQVIvODJizszN MlzZNlAxPzl4M{[=
HEK293 cells NYrQUGxHTnWwY4Tpc44h[XO|YYm= NXfs[W45UW6qaXLpeIlwdiCxZjDoeY1idiCPQWTFNU1u\WSrYYTl[EBCW1BtIIXweIFs\SCneIDy[ZN{\WRiaX6gTGVMOjl|IHPlcIx{KGGodHXyJFEvPSCvaX7zJIJ6KG[udX;y[ZNk\W6lZTDhd5NigSxiSVO1NF0yPy57IN88US=> NGPKOpYzOzJ2MUCyPS=>
Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot p-eNOS / eNOS / p-AMPKα / AMPKα ; p-CREB / CREB / p-p38 MAPK / p38 MAPK ; Cyclin D1 / CDK4 / CDK6 / CDK2 / Cylcin E / E2F2 24827148 28052030
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 (from reference)

Solubility (25°C)

In vitro

 DMSO 13 mg/mL warmed
(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 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCC1=NC2=C(N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C=C(C=C2C)C5=NC6=CC=CC=C6N5C

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04736329 Recruiting Drug: Telmisartan Heart Failure With Reduced Ejection Fraction|Renal Insufficiency Cairo University February 1 2021 Not Applicable
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

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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