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Irbesartan

Catalog No. T1615   CAS 138402-11-6
Synonyms: SR-47436, BMS-186295

Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker. The mechanism of action of irbesartan is as an Angiotensin 2 Receptor Antagonist.

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Irbesartan Chemical Structure
Irbesartan, CAS 138402-11-6
Pack Size Availability Price/USD Quantity
10 mg In stock $ 48.00
25 mg In stock $ 58.00
50 mg In stock $ 90.00
100 mg In stock $ 150.00
200 mg In stock $ 189.00
500 mg In stock $ 217.00
1 mL * 10 mM (in DMSO) In stock $ 47.00
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Purity: 99.92%
Purity: 99.81%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Irbesartan (SR-47436) is an Angiotensin 2 Receptor Blocker. The mechanism of action of irbesartan is as an Angiotensin 2 Receptor Antagonist.
Targets&IC50 AT1 receptor:1.3 nM
In vitro Administering 7 mg/kg of Irbesartan daily to rats with congestive heart failure induced by lily alkaloid significantly inhibited skeletal muscle cell apoptosis and intramuscular atrophy. This effect is associated with a decrease in TNFα levels and is attributed to AT1 receptor blockade. Oral administration of 1 mg/kg Irbesartan in conscious rats with normal blood pressure reduced angiotensin II-induced hypertension, exhibiting effects similar to losartan treatment. However, its efficacy in normotensive monkeys was significantly higher than that of 10 mg/kg losartan.
In vivo At a concentration of 10 μM, Irbesartan inhibits the increase in mRNA and protein levels of integrins αv, β1, β3, and β5, osteopontin, and α-actinin in rat cardiac fibroblasts induced by angiotensin II, resulting in reduced cell adhesion to the extracellular matrix (ECM) proteins. Additionally, Irbesartan significantly induces the expression of the adipogenic marker gene, fatty acid-binding protein 2 (aP2), in 3T3-L1 cells in a concentration-dependent manner, with an EC50 of 3.5 μM and inducing effects being 3.3 times stronger at 10 μM. Also, 10 μM Irbesartan substantially induces peroxisome proliferator-activated receptor-γ transcriptional activity by 3.4 times, independent of its AT1 receptor antagonist action. Pre-treatment with 10 μM Irbesartan in rat vascular smooth muscle cells reduces angiotensin II-induced apoptosis by inhibiting angiotensin II internalization, demonstrating concentration dependency. Irbesartan competes with angiotensin II for binding to the AT1 receptor subtype with an IC50 of 1.3 nM and exhibits 10 times higher efficacy than Losartan in antagonizing AII-induced spasms in rabbit aortic rings, with IC50 values of 4 nM compared to Losartan's 14 nM and 25 nM, respectively.
Synonyms SR-47436, BMS-186295
Molecular Weight 428.53
Formula C25H28N6O
CAS No. 138402-11-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 25 mg/mL (58.34 mM)

TargetMolReferences and Literature

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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Anti-Cancer Drug Library EMA Approved Drug Library Inhibitor Library Bioactive Compound Library Anti-Metabolism Disease Compound Library FDA-Approved & Pharmacopeia Drug Library Human Metabolite Library

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Keywords

Irbesartan 138402-11-6 Apoptosis Endocrinology/Hormones RAAS inhibit BMS 186295 hypertensive renal injury Angiotensin Receptor blood vessels Ang II type 1 (AT1) receptor blocker (ARB) Inhibitor SR47436 SR 47436 blood heart failure Th22 cells SR-47436 diabetic kidney disease BMS-186295 BMS186295 chemotaxis inhibitor

 

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