[CAS NO. 138402-11-6] Irbesartan

Name: Irbesartan
Brand: Arctom Scientific
SKU: SLK-S1507

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PRODUCTS SPECIFICATIONS [138402-11-6]

Store

Catalog

SLK-S1507

Brand

Selleck

CAS

138402-11-6

DESCRIPTION [138402-11-6]

Overview

MDL	MFCD00864464
Molecular Weight	428.53
Molecular Formula	C25H28N6O
SMILES	O=C1C2(N=C(CCCC)N1CC3=CC=C(C=C3)C4=C(C=CC=C4)C=5NN=NN5)CCCC2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3336 mL	11.6678 mL	23.3356 mL
5 mM	-	-	-
10 mM	-	-	-
50 mM	-	-	-

Description

Irbesartan (BMS-186295, SR-47436,APROVEL) is a highly potent and specific receptor antagonist with 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. Irbesartan (10 μM) blocks angiotensin II induced increase in α, β, β, and β 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. 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. 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.

References

[1] Bernhart CA, et al. J Med Chem, 1993, 36(22), 3371-3380.
[2] Kawano H, et al. Hypertension, 2000, 35, 273-279.
[3] Schupp M, et al. Circulation, 2004, 109(17), 2054-2057.
[4] Ruiz E, et al. Eur J Pharmacol, 2007, 567(3), 231-239.
[5] Dalla Libera L, et al. Circulation, 2001, 103(17), 2195-2200.

Synonyms

1,3-Diazaspiro[4.4]non-1-en-4-one, 2-butyl-3-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-

1,3-Diazaspiro[4.4]non-1-en-4-one, 2-butyl-3-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-

2-Butyl-3-[[2′-(2H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one

SR 47436

2-Butyl-3-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]-1,3-diazaspiro[4.4]non-1-en-4-one

Irbesartan

BMS 186295

Avapro

Aprovel

Karvea

2-Butyl-3-[[2′-(tetrazol-5-yl)biphenyl-4-yl]-methyl]-1,3-diazaspiro[4.4]non-1-en-4-one

Irbetan

Irbest

Kansartan

X-Tension

3-Butyl-2-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-2,4-diazaspiro[4.4]non-3-en-1-one

2-Butyl-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one

2-Butyl-3-[2′-(2H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-1,3-diaza-spiro[4.4]non-1-en-4-one

Sabervel