Product Categories

Irbesartan (Avapro)

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

Catalog No.S1507

: Tel: +1-832-582-8158[email protected]

Irbesartan (Avapro) Chemical Structure
Molecular Weight: 428.53

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

Irbesartan (Avapro) is available in the following compound libraries:

Chemical Library (96-well) FDA Approved Drug Library (96-well) Inhibitor Library (96-well)

Product Information

Compare RAAS Inhibitors & Chemicals

Research Area
Research Area
Dr. Antonino Maria Sparta demonstrates a breakthrough in leukemia research by utilizing two inhibitors produced by Selleck Chemicals.

Cat.No.	Product Name	Solubility (25°C)
S2199	Aliskiren hemifumarate	122 mg/mL	122 mg/mL	122 mg/mL
S1359	Losartan potassium	92 mg/mL	92 mg/mL	92 mg/mL
S1657	Enalaprilat dihydrate	5 mg/mL	70 mg/mL	1 mg/mL
S2169	Rosuvastatin calcium (Crestor)	<1 mg/mL	100 mg/mL	<1 mg/mL
S1578	Candesartan (Atacand)	<1 mg/mL	88 mg/mL	1 mg/mL
S1738	Telmisartan (Micardis)	<1 mg/mL	13 mg/mL	<1 mg/mL
S2051	Captopril (Capoten)	2 mg/mL	43 mg/mL	43 mg/mL
S2076	Lisinopril (Zestril)	20 mg/mL	<1 mg/mL	<1 mg/mL
S2079	Moexipril HCl	<1 mg/mL	20 mg/mL	<1 mg/mL
S1284	Benazepril HCl	19 mg/mL	92 mg/mL	92 mg/mL
S1507	Irbesartan (Avapro)	<1 mg/mL	1 mg/mL	3 mg/mL
S1506	Perindopril Erbumine (Aceon)	88 mg/mL	<1 mg/mL	88 mg/mL
S1604	Olmesartan medoxomil (Benicar)	<1 mg/mL	89 mg/mL	<1 mg/mL
S1894	Valsartan (Diovan)	<1 mg/mL	87 mg/mL	87 mg/mL
S1793	Ramipril (Altace)	<1 mg/mL	83 mg/mL	83 mg/mL
S2037	Candesartan cilexetil (Atacand)	<1 mg/mL	122 mg/mL	4 mg/mL
S2664	Clinofibrate	<1 mg/mL	94 mg/mL	94 mg/mL
S2581	Quinapril HCl (Accupril)	95 mg/mL	18 mg/mL	95 mg/mL
S2081	Cilazapril monohydrate (Inhibace)	<1 mg/mL	87 mg/mL	87 mg/mL
S2095	Fosinopril sodium (Monopril)	117 mg/mL	<1 mg/mL	4 mg/mL
S2099	Temocapril HCl	<1 mg/mL	103 mg/mL	103 mg/mL
S3046	Azilsartan (TAK-536)	<1 mg/mL	91 mg/mL	<1 mg/mL
S3057	Azilsartan Medoxomil (TAK-491)	<1 mg/mL	114 mg/mL	<1 mg/mL

Product Description

Biological Activity Protocol Chemical Information Tech Support & FAQs

Biological Activity

Description	Irbesartan (Avapro, SR-47436, BMS-186295) is a highly potent and specific angiotensin II type 1 (AT1) receptor antagonist with IC50 of 1.3 nM.
Targets	AT1
IC50	1.3 nM ^[1]
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 α_v, 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]
Clinical Trials	A Phase I study to evaluate pharmacokinetics and safety after oral administration of Irbesartan and Atorvastatin in combination as HCP0912 in healthy male subjects has been completed.
Features	Irbesartan is a longer acting AT1 receptor antagonist than losartan and valsartan.

Protocol(Only for Reference)

Kinase Assay: ^[1]

Angiotensin II Binding Study on Rat Liver Membranes	The plasma membranes of livers are purified from male Sprague-Dawley rats, and diluted in the incubation buffer (20 mM Tris-HCI, 10 mM MgCI₂, 2 g/L RSA, 145 mg/L bacitracin, pH 7.5). Aliquots of membrane suspension (20-330 μg protein/assay) are incubated for 1 hour at 25 °C with [¹²⁵I]angiotensin II (AII) and various concentrations of Irbesartan in 200 μL of incubation buffer. The incubation is stopped by rapid filtration through a Whatman GF/B filter followed by three consecutive washing sin 5 mL of cold incubation buffer (the GF/B filters are preincubated for 1 hour in the incubation buffer). The radioactivity bound to the filter is counted in a γ counter. Specific binding is defined as the difference between total binding and the binding in the presence of 1 μM unlabeled angiotensin II (AII). The concentration of Irbesartan producing 50% inhibition (IC50) of radioligand binding is determined from competition curve.

Angiotensin II Binding Study on Rat Liver Membranes

The plasma membranes of livers are purified from male Sprague-Dawley rats, and diluted in the incubation buffer (20 mM Tris-HCI, 10 mM MgCI₂, 2 g/L RSA, 145 mg/L bacitracin, pH 7.5). Aliquots of membrane suspension (20-330 μg protein/assay) are incubated for 1 hour at 25 °C with [¹²⁵I]angiotensin II (AII) and various concentrations of Irbesartan in 200 μL of incubation buffer. The incubation is stopped by rapid filtration through a Whatman GF/B filter followed by three consecutive washing sin 5 mL of cold incubation buffer (the GF/B filters are preincubated for 1 hour in the incubation buffer). The radioactivity bound to the filter is counted in a γ counter. Specific binding is defined as the difference between total binding and the binding in the presence of 1 μM unlabeled angiotensin II (AII). The concentration of Irbesartan producing 50% inhibition (IC50) of radioligand binding is determined from competition curve.

Animal Study: ^[1]

Animal Models	Male Sprague-Dawley rats and female cynomolgus monkeys (Macaca fascicularis) injected (iv) with angiotensin II (AII)
Formulation	Dissolved in water by neutralization with a stoichiometric equivalent of KOH, or dissolved in saline by neutralization with a stoichiometric equivalent of L-arginine
Dosages	1 mg/kg
Administration	Oral gavage

References

Chemical Information

Download Irbesartan (Avapro) SDF

Molecular Weight (MW)	428.53
Formula	C₂₅H₂₈N₆O
CAS No.	138402-11-6
Synonyms	BMS-186295, SR-47436

Solubility (25°C) DMSO 1 mg/mL Water <1 mg/mL Ethanol 3 mg/mL
Storage	2 years -20°CPowder
	2 weeks4°Cin DMSO
	6 months-80°Cin DMSO

Chemical Name

Molarity Calculator Dilution Calculator Molecular Weight Calculator

Research Area

Tech Support & FAQs

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:3Monday–Friday 9:00 AM–5:00 PM (Central Time)

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related RAAS Inhibitors & Chemicals

Clinofibrate
Clinofibrate inhibits hydroxymethylglutaryl coenzyme A reductase (HMGCR) with IC50 of 0.47 mM.
Andarine (GTX-007)
Andarine (GTX-007) is a selective nonsteroidal androgen receptor (AR) agonist with K_i of 4 nM.
Ostarine(MK-2866)
Ostarine (GTx-024, MK-2866, Enobosarm, S-22) is a selective androgen receptor modulator (SARM) with K_i of 3.8 nM.
LY500307 (Erteberel)
LY500307 (SERBA-1) is a potent, selective estrogen receptor β agonist with EC50 of 0.66 nM.
GSK1292263
GSK-1292263 is a novel GPR119 agonist.
Equol
Equol is an isoflavandiol metabolized from daidzein by bacterial flora in the intestines.
Hexestrol(Bibenzyl)
Hexestrol binds to ERα and ERβ with EC50 of 0.07 nM and 0.175 nM, respectively.
TAK-875
TAK-875 is a selective GPR40 agonist with EC50 of 14 nM.
Galeterone (TOK-001)
Galeterone (TOK-001, VN/124-1) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively.
Epiandrosterone (3β-androsterone)
Epiandrosterone (3β-androsterone) is a steroid hormone with weak androgenic activity which acts as a L-type Ca²⁺ channel antagonist.

Choose Your Country or Region

Product Categories

Irbesartan (Avapro)