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Irbesartan Angiotensin Receptor antagonist

Cat.No.S1507

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

Batch: Purity: 99.92%
99.92

Solubility

In vitro
Batch:

DMSO : 1 mg/mL (2.33 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 428.53 Formula

C25H28N6O

Storage (From the date of receipt)
CAS No. 138402-11-6 Download SDF Storage of Stock Solutions

Synonyms BMS-186295, SR-47436 SMILES CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5

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Mechanism of Action

Features
Irbesartan is a longer acting AT1 receptor antagonist relative to losartan and valsartan.
Targets/IC50/Ki
AT1 receptor
1.3 nM
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. This compound has no affinity for AT2 receptors. It (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. This chemical 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. It (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. Pretreatment with this compound (~10 μM) decreases angiotensin II-induced apoptosis in rat vascular smooth muscle cells by blocking angiotensin II internalization in a concentrationdependent manner.

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. Administration of this compound (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.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/17509562/
  • [5] https://pubmed.ncbi.nlm.nih.gov/11331262/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-04-28)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07555054 NOT_YET_RECRUITING
Chronic Kidney Disease
Jiangsu Hansoh Pharmaceutical Co., Ltd.
2026-05-21 PHASE2
NCT06660940 NOT_YET_RECRUITING
Diabetic Kidney Disease; Diabetic Retinopathy
Chinese PLA General Hospital
2024-10 PHASE4
NCT06635772 NOT_YET_RECRUITING
Immunoglobulin a Nephropathy
Hansoh BioMedical R&D Company
2024-11 PHASE2
NCT03476616 COMPLETED
Hypertension; Obesity
Hippocration General Hospital
2018-09-01 PHASE4
NCT05272878 ACTIVE_NOT_RECRUITING
Acute Kidney Injury
Assistance Publique - Hôpitaux de Paris
2022-11-22 PHASE3
NCT06208072 UNKNOWN
Primary Hypertension; Obesity
Hippocration General Hospital
2023-09-01

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