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

Irbesartan

Synonyms: BMS-186295, SR-47436

Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.

Irbesartan Chemical Structure

Irbesartan Chemical Structure

CAS: 138402-11-6

Selleck's Irbesartan has been cited by 5 Publications

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Purity & Quality Control

Batch: Purity: 99.92%
99.92

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Biological Activity

Description Irbesartan is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.
Features Irbesartan is a longer acting AT1 receptor antagonist relative to losartan and valsartan.
Targets
AT1 receptor [1]
1.3 nM
In vitro
In vitro

Irbesartan competes with angiotensin II (AII) for binding at the AT1 receptor subtype and antagonizes AII-induced contraction in rabbit aorta ring with IC50 of 4 nM. Irbesartan has no affinity for AT2 receptors. [1] Irbesartan (10 μM) blocks angiotensin II induced increase in αv, β1, β3, and β5 integrins, osteopontin, and α-actinin mRNA and protein levels in rat cardiac fibroblasts, leading to the decrease of cell attachment to extracellular matrix (ECM) proteins. [2] Irbesartan treatment markedly induces the expression of the adipogenic marker gene adipose protein 2 (aP2) in 3T3-L1 cells in a concentration-dependent manner with EC50 of 3.5 μM and 3.3-fold induction at the concentration of 10 μM. Irbesartan (10 μM) markedly induces transcriptional activity of the peroxisome proliferator–activated receptor-γ (PPARγ) by 3.4-fold independent of its AT1 receptor blocking action. [3] Pretreatment with Irbesartan (~10 μM) decreases angiotensin II-induced apoptosis in rat vascular smooth muscle cells by blocking angiotensin II internalization in a concentrationdependent manner. [4]
In Vivo
In vivo

Oral administration of Irbesartan (1 mg/kg) reduces angiotensin II (AII)-induced hypertension, equipotent with losartan in conscious normotensive rats, markedly more active than losartan (10 mg/kg) in normotensive cynomolgus monkeys. [1] Administration of Irbesartan (7 mg/kg/day) significantly prevents skeletal muscle apoptosis and muscle atrophy in rats with monocrotaline-induced congestive heart failure (CHF), which is involved with the decrease of TNFα level and attributed to AT1 receptor blocking. [5]
Animal Research Animal Models Male Sprague-Dawley rats and female cynomolgus monkeys (Macaca fascicularis) injected (iv) with angiotensin II (AII)
Dosages 1 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04983979 Terminated CKD|Diabetes Mellitus Type 2|Hyperkalemia Barts & The London NHS Trust June 17 2022 Phase 2
NCT03627715 Completed Diabetic Kidney Disease Dimerix Bioscience Pty Ltd|Iqvia Pty Ltd November 6 2018 Phase 2
NCT03649152 Completed Focal Segmental Glomerulosclerosis Dimerix Bioscience Pty Ltd|Iqvia Pty Ltd November 8 2018 Phase 2

Chemical lnformation & Solubility

Molecular Weight 428.53 Formula

C25H28N6O
CAS No. 138402-11-6 SDF Download Irbesartan SDF
Smiles CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 1 mg/mL ( (2.33 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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