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Telmisartan Angiotensin Receptor antagonist

Cat.No.S1738

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

Batch: Purity: 99.97%
99.97

Cell Culture, Treatment & Working Concentration

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
HepG2 cells Function assay Inhibition of liver stage Plasmodium berghei infection in HepG2 cells, IC50=0.025 μM
CV1 cells Function assay Agonist activity at human PPARgamma expressed in african green monkey CV1 cells by Gal4 transactivation assay, EC50=2.02 μM
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
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Solubility

In vitro
Batch:

DMSO : 15 mg/mL (29.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
Batch:

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Working concentration: mg/ml;

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

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Chemical Information, Storage & Stability

Molecular Weight 514.62 Formula

C33H30N4O2

Storage (From the date of receipt)
CAS No. 144701-48-4 Download SDF Storage of Stock Solutions

Synonyms BIBR 277 SMILES CCCC1=NC2=C(N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C=C(C=C2C)C5=NC6=CC=CC=C6N5C

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
angiotensin II receptor
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. This compound induces adipocyte differentiation of 3T3-L1 cells. It causes a 60% to 70% decrease in the expression of ACC2 in murine muscle myotubes. This chemical, but not candesartan, another ARB, downregulates RAGE mRNA levels in a dose-dependent manner. It decreases basal as well as AGE-induced RAGE protein expression in Hep3B cells. This compound dose-dependently inhibits AGE-induced ROS generation and subsequent CRP gene and protein induction in Hep3B cells. It effectively facilitates differentiation of 3T3-L1 preadipocytes. This chemical 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. It 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. This compound 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.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16567593/

Applications

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
S1738-WB1
24827148

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-10-03)

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Ovarian Cancer
Tyler J Curiel
2026-01-21 PHASE2
NCT06168487 RECRUITING
Prostate Cancer
Tyler J Curiel
2024-04-22 PHASE1
NCT07784608 NOT_YET_RECRUITING
Drug-drug Interactions
Huons Co., Ltd.
2026-09 PHASE1

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