GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

TAK-491 | 1H-Benzimidazole-7-carboxylic acid, 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-, (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Azilsartan Medoxomil Azilsartan Medoxomil (TAK-491) is a potent angiotensin II type 1 (AT1) receptor antagonist, inhibits the RAAS , with an IC50 of 2.6 nM, exhibits >10,000-fold selectivity over AT2.
In vitro

Azilsartan medoxomil is a prodrug, which is rapidly converted to the active moiety, azilsartan (TAK-536), by ester hydrolysis in the gut and plasma during absorption after oral administration. Azilsartan selectively blocks the binding of angiotensin II to the AT1 (angiotensin II type 1) receptors found in the vascular smooth muscle and the adrenal gland, thereby promoting vasodilation and a decrease in the effects of aldosterone. Azilsartan is a highly selective antagonist to the AT1 receptor, with an IC50 of 2.6 nM, exhibiting a >10,000-fold affinity for the AT1 receptor compared with the AT2 receptor, and has not shown affinity for other cardiac receptors or ion channels. The inhibitory effect of Azilsartan persists after washout of the free compound (IC50 value of 7.4 nM). Azilsartan also inhibits the accumulation of angiotensin II -induced inositol 1-phosphate (IP1) in the cell-based assay with an IC50 value of 9.2 nM, and this effect is resistant to washout (IC50 value of 81.3 nM).

In vivo

Cell Data

cell lines：

Concentrations：~10 nM

Incubation Time：2 h

Powder Purity:≥97%

Specifications

Synonyms

TAK-491 | 1H-Benzimidazole-7-carboxylic acid, 1-[[2'-(2, 5-dihydro-5-oxo-1, 2, 4-oxadiazol-3-yl)[1, 1'-biphenyl]-4-yl]methyl]-2-ethoxy-, (5-methyl-2-oxo-1, 3-dioxol-4-yl)methyl ester

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Azilsartan Medoxomil (TAK-491) is a potent angiotensin II type 1 (AT1) receptor antagonist, inhibits the RAAS, with an IC50 of 2.6 nM, exhibits >10, 000-fold selectivity over AT2.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Names and Identifiers

• Isomeric SMILES: CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NOC(=O)N5)C(=O)OCC6=C(OC(=O)O6)C
• Molecular Weight: 568.55
• Reaxy-Rn: 12326818
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=12326818&ln=