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 No. 138402-11-6

Purity & Quality Control

Irbesartan Related Products

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
NCT06256991 Not yet recruiting
Chronic Kidney Diseases|Hyperkalemia|Hypertension
University Medical Center Groningen|Amsterdam University Medical Center|Medical Centre Leeuwarden|Isala|Vifor Pharma Inc.|Dutch Kidney Foundation|Health Holland
 April 2024 Phase 4
NCT06208072 Recruiting
Primary Hypertension|Obesity
Hippocration General Hospital|National and Kapodistrian University of Athens
 September 1 2023 Not Applicable
NCT04983979 Terminated
CKD|Diabetes Mellitus Type 2|Hyperkalemia
Barts & The London NHS Trust
 June 17 2022 Phase 2

Chemical Information & 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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Irbesartan | Irbesartan ic50 | Irbesartan price | Irbesartan cost | Irbesartan solubility dmso | Irbesartan purchase | Irbesartan manufacturer | Irbesartan research buy | Irbesartan order | Irbesartan mouse | Irbesartan chemical structure | Irbesartan mw | Irbesartan molecular weight | Irbesartan datasheet | Irbesartan supplier | Irbesartan in vitro | Irbesartan cell line | Irbesartan concentration | Irbesartan nmr