Irbesartan

Catalog No.S1507 Synonyms: BMS-186295, SR-47436

For research use only.

Irbesartan (BMS-186295, SR-47436) is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.

Irbesartan Chemical Structure

CAS No. 138402-11-6

Selleck's Irbesartan has been cited by 5 Publications

2 Customer Reviews

Purity & Quality Control

Choose Selective Angiotensin Receptor Inhibitors

Biological Activity

Description Irbesartan (BMS-186295, SR-47436) 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

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 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]

Protocol (from reference)

Animal Research:[1]
  • 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

Solubility (25°C)

In vitro

DMSO 4 mg/mL warmed
(9.33 mM)
Ethanol 3 mg/mL
(7.0 mM)
Water Insoluble

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
30% PEG400+0.5% Tween80+5% propylene glycol
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 428.53
Formula

C25H28N6O

CAS No. 138402-11-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCCCC1=NC2(CCCC2)C(=O)N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NNN=N5

In vivo Formulation Calculator (Clear solution)

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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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04983979 Not yet recruiting Drug: Sodium Zirconium Cyclosilicate|Drug: Placebo CKD|Diabetes Mellitus Type 2|Hyperkalemia Barts & The London NHS Trust August 15 2021 Phase 2
NCT03627715 Active not recruiting Drug: Propagermanium|Drug: Placebo Diabetic Kidney Disease Dimerix Bioscience Pty Ltd|Iqvia Pty Ltd November 6 2018 Phase 2
NCT03649152 Active not recruiting Drug: Propagermanium|Drug: Placebo Focal Segmental Glomerulosclerosis Dimerix Bioscience Pty Ltd|Iqvia Pty Ltd November 8 2018 Phase 2
NCT03476603 Recruiting Drug: Irbesartan Obesity Morbid Norwegian University of Science and Technology|St. Olavs Hospital|Volvat Medisinsk Senter Stokkan|Namsos Hospital|Alesund Hospital November 2 2016 --
NCT02597361 Completed Drug: Irbesartan|Drug: Placebo Ehlers-Danlos Syndrome Vascular Type Assistance Publique - Hôpitaux de Paris|Ministry of Health France January 2016 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

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