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

Descripción general

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

Sinónimos

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-

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Grado

Moligand™

Tipo de acción

ANTAGONIST

Mecanismo de acción

Type-1 angiotensin II receptor antagonist

Propiedades del producto

• ALogP: 4.4

Nombres e identificadores

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

Objetivos asociados (humanos)

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)

Propiedades químicas y físicas

• Punto de fusión (°C): 188 °C(dec.)

Referencias

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]