Home GPCR & G Protein Angiotensin Receptor antagonist Telmisartan For research use only.

Telmisartan

Synonyms: BIBR 277

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

Telmisartan Chemical Structure

Telmisartan Chemical Structure

CAS No. 144701-48-4

Purity & Quality Control

Telmisartan Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO cells Function assay Antagonist activity at human AT1 receptor expressed in CHO cells measured after overnight incubation by luciferase reporter gene assay, IC50=0.002 μM 24462665
HepG2 cells Function assay Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50=0.025 μM 22586124
CV1 cells Function assay Agonist activity at human PPARgamma expressed in african green monkey CV1 cells by Gal4 transactivation assay, EC50=2.02 μM 20079636
HEK293 cells Function assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay, IC50=17.9 μM 23241029
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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
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]
Experimental Result Images Methods Biomarkers Images 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
In Vivo
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06168487 Not yet recruiting
Prostate Cancer
Tyler J Curiel|Dartmouth-Hitchcock Medical Center
 January 1 2024 Early Phase 1
NCT05223101 Unknown status
Hypertension
HK inno.N Corporation
 January 19 2022 Phase 1
NCT05040880 Completed
Hypertension
HK inno.N Corporation
 July 8 2021 Phase 1
NCT04736329 Completed
Heart Failure With Reduced Ejection Fraction|Renal Insufficiency
Cairo University
 February 1 2021 Not Applicable
NCT05322889 Unknown status
Neuropathic Pain|Chemotherapy Effect
Dr. Frank Behrens|Johann Wolfgang Goethe University Hospital|Fraunhofer Institute for Molecular Biology and Applied Ecology
 April 9 2020 Phase 2

Chemical Information & Solubility

Molecular Weight 514.62 Formula

C33H30N4O2
CAS No. 144701-48-4 SDF Download Telmisartan SDF
Smiles CCCC1=NC2=C(N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C=C(C=C2C)C5=NC6=CC=CC=C6N5C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 13 mg/mL ( (25.26 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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