Azilsartan - Moligand™, 10mM in DMSO , Type-1 angiotensin II receptor antagonist, CAS No.147403-03-0, Type-1 angiotensin II receptor antagonist

CAS: 147403-03-0 Cat. No.: A408730 Formula: C₂₅H₂₀N₄O₅ Molecular Weight: 456.45 EC Number: 808-058-6

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

TAK-536 | 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-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Azilsartan Azilsartan (TAK-536) is an angiotensin II type 1 (AT1) receptor antagonist with IC50 of 2.6 nM.
In vitro

Azilsartan inhibits the specific binding of ¹²⁵I-Sar¹-Ile⁸-AII to human angiotensin type 1 receptors. Azilsartan also inhibits the accumulation of AII-induced inositol 1-phosphate (IP1) in the cell-based assay with an IC50 value of 9.2 nM. In isolated rabbit aortic strips, Azilsartan reduces the maximal contractile response to AII with a pD\'2 value of 9.9. The inhibitory effects of Azilsartan on contractile responses induced by AII persists after the strips are washed. Azilsartan suppresses the increase in plasma glucose level in the oral glucose tolerance test (OGTT) without significant change in insulin concentration and improved insulin sensitivity. In skeletal muscle, Azilsartan decreases the expression of TNF-α at doses of 0.001%. In adipose tissue, Azilsartan reduces TNF-α expression but increases the expression of adiponectin, PPARγ, C/EBα, and aP2. In cultured 3T3-L1 preadipocytes, Azilsartan enhances adipogenesis and exertes greater effects than valsartan on expression of genes encoding peroxisome proliferator-activated receptor-α (PPARα), PPARδ, leptin, adipsin, and adiponectin. Azilsartan also potently inhibits vascular cell proliferation in the absence of exogenously supplemented angiotensin II.

In vivo

In Koletsky rats, Azilsartan treatment lowers blood pressure, basal plasma insulin concentration and the homeostasis model assessment of insulin resistance index, and inhibited over-increase of plasma glucose and insulin concentrations during oral glucose tolerance test. Azilsartan downregulates 11β-hydroxysteroid dehydrogenase type 1 expression.
Cell Data

cell lines：BCSC

Concentrations：0 μM -1 μM

Incubation Time：2 hours

Powder Purity:≥99%

Specifications

Synonyms

TAK-536 | 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-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Azilsartan (TAK-536) is an angiotensin II type 1 (AT1) receptor antagonist with IC50 of 2.6 nM.

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

Mechanism of action

Type-1 angiotensin II receptor antagonist

Product Properties

• ALogP: 4.4

Names and Identifiers

• Isomeric SMILES: CCOC1=NC2=CC=CC(=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C5=NOC(=O)N5)C(=O)O
• WGK Germany: 3
• Molecular Weight: 456.45
• Reaxy-Rn: 7673311
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7673311&ln=

Associated Targets(Human)

AGTR1 Tclin Type-1 angiotensin II receptor (0 Activities)

Discover Target: AGTR1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Melt Point(°C): 188 °C(dec.)

References

1. Yunong Li, Haixia Zhu, Jingbo Yang, Kehui Ke, Yanmei Zhu, Li Chen, Youyang Qu, Rui Suo, Xiujie Chen, Yulan Zhu.  (2018)  Discovering Proangiogenic Drugs in Ischemic Stroke Based on the Relationship between Protein Domain and Drug Substructure.  ACS Chemical Neuroscience,      [PMID:30346717] [10.1021/acschemneuro.8b00381]

2. Qi Liang, Xiaoying Fu, Jianfeng Zhang, Jiaxue Hao, Gangjun Feng, Jing Wang, Qian Li, Faizan Ahmad, Xinfeng Zhao.  (2020)  Immobilized angiotensin II type I receptor: A powerful method of high throughput screening for antihypertensive compound identification through binding interaction analysis.  JOURNAL OF CHROMATOGRAPHY A,      [PMID:32156458] [10.1016/j.chroma.2020.461003]

Frequently Asked Questions

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 147403-03-0, the molecular formula is C25H20N4O5, and the molecular weight is 456.45 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.