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Telmisartan, 2400mg (40mg/capsule)
Telmisartan is a biphenyl-tetrazole small molecule and selective antagonist of the angiotensin II type 1 receptor (AT1R).
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Vedi i risultati di laboratorio →Telmisartan is a biphenyl-tetrazole small molecule and selective antagonist of the angiotensin II type 1 receptor (AT1R). In addition to its well-characterized AT1R antagonism, telmisartan exhibits partial agonist activity at peroxisome proliferator-activated receptor gamma (PPARγ), distinguishing it from many other compounds within the angiotensin receptor blocker (ARB) class.
This dual pharmacological profile enables investigation of both G protein-coupled receptor (GPCR) signaling and nuclear receptor-mediated transcriptional regulation within a single molecular framework.
Experimental studies have examined telmisartan's interactions with AT1R-associated signaling pathways, PPARγ-dependent transcriptional mechanisms, receptor-ligand binding dynamics, and downstream regulatory networks.
Research applications include AT1R pharmacology, angiotensin receptor signaling studies, PPARγ partial agonism research, receptor cross-talk investigation, structure-activity relationship analysis, and mechanistic evaluation of coordinated GPCR and nuclear receptor signaling systems. Supplied in capsule form.
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3D Molecular Structure
Drag to rotate · scroll to zoom| Chemical Formula | C33H30N4O2 |
|---|---|
| Synonyms | Micardis (trade name), BIBR 277 |
| Molar Mass | 514.617 g/mol |
| CAS Number | 144701-48-4 |
| PubChem CID | 65999 |
| Total Compound Content | 2,400 mg (40 mg per capsule) |
| Shelf Life | 36 months |
Telmisartan is a non-peptide angiotensin II type 1 receptor (AT1R) antagonist that selectively inhibits angiotensin II binding at the AT1 receptor with high specificity relative to related receptor subtypes. In addition to its well-characterized AT1R antagonism, telmisartan exhibits partial agonist activity at peroxisome proliferator-activated receptor gamma (PPARγ), distinguishing it from many other compounds within the angiotensin receptor blocker (ARB) class. This dual pharmacological profile enables investigation of both G protein-coupled receptor (GPCR) signaling and nuclear receptor-mediated transcriptional regulation within a single molecular framework.
Experimental studies have examined telmisartan's interactions with AT1R-associated signaling pathways, PPARγ-dependent transcriptional mechanisms, receptor-ligand binding dynamics, co-regulator recruitment processes, and downstream regulatory networks. Research applications include AT1R pharmacology, angiotensin receptor signaling studies, PPARγ partial agonism research, receptor cross-talk investigation, structure-activity relationship analysis, and mechanistic evaluation of coordinated GPCR and nuclear receptor signaling systems. Telmisartan is frequently utilized as a reference compound in AT1R binding investigations and comparative receptor pharmacology studies. Supplied in 40 mg capsules. Independently third-party HPLC-tested; COA available per batch.
Results refer to the tested sample. Check the batch and date in the report.
What makes telmisartan unique among angiotensin receptor blockers (ARBs) in research settings?
Telmisartan is distinguished by its dual pharmacological profile, functioning as both an angiotensin II type 1 receptor (AT1R) antagonist and a partial agonist of peroxisome proliferator-activated receptor gamma (PPARγ).
While many ARBs are characterized primarily by AT1R antagonism, telmisartan additionally enables investigation of PPARγ-associated transcriptional regulation within the same molecular framework. This combination makes it a valuable research tool for studies examining interactions between GPCR-mediated signaling and nuclear receptor-dependent regulatory mechanisms.
How does telmisartan's PPARγ activity differ from compounds with stronger PPARγ agonist properties?
Telmisartan is characterized as a partial PPARγ agonist, producing receptor activation that differs from compounds exhibiting higher intrinsic efficacy at the same receptor.
This property has made telmisartan useful for investigations of receptor activation dynamics, co-regulator recruitment processes, transcriptional regulation mechanisms, and the molecular distinctions between partial and higher-efficacy agonist profiles. Such studies contribute to broader understanding of PPARγ pharmacology and receptor-mediated signaling systems.
Why is telmisartan commonly used in receptor pharmacology research?
Telmisartan possesses a well-characterized interaction profile at both AT1R and PPARγ, making it a frequently utilized reference compound in receptor-binding investigations, ligand-receptor interaction studies, and comparative pharmacology research. Experimental applications include analysis of receptor selectivity, signaling pathway regulation, cofactor recruitment, structure-activity relationships, and mechanistic evaluation of coordinated GPCR and nuclear receptor signaling networks.
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