Valsartan (CGP-48933) - Moligand™, 10mM in DMSO , Antagonist of AT 1 receptor, CAS No.137862-53-4, Antagonist of AT 1 receptor

CAS: 137862-53-4 Cat. No.: V408202 Peso molecular: 435.52 Número EC: 604-045-2

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

N-​(1-​oxopentyl)​-​N-​[[2'-​(2H-​tetrazol-​5-​yl)​[1,​1'-​biphenyl]​-​4-​yl]​methyl]​-L-​valine

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Valsartan (CGP-48933) Valsartan (CGP-48933) is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure.
In vitro

Valsartan dose-dependently inhibits the vasoconstriction induced by angiotensin II and lowers blood pressure in renin-dependent models of hypertension. Valsartan is at least as effective as ACE inhibitors, diuretics, beta-blockers and calcium antagonists.

In vivo

Valsartan results in improved glucose tolerance, reduced fasting blood glucose levels, and reduced serum insulin levels in mice fed a Western diet. Valsartan treatment also blocks Western diet-induced increases in serum levels of the proinflammatory cytokines interferon-gamma and monocyte chemotactic protein 1. Valsartan enhances mitochondrial function and prevents Western diet-induced decreases in glucose-stimulated insulin secretion in the pancreatic islets of mice. Valsartan treatment blocks or attenuates Western diet-induced changes in expression of several key inflammatory signals: interleukin 12p40, interleukin 12p35, tumor necrosis factor-alpha, interferon-gamma, adiponectin, platelet 12-lipoxygenase, collagen 6, inducible NO synthase, and AT1R in isolated adipocytes. Valsartan significantly increases insulin-mediated 2-[3H]deoxy-d-glucose (2-[3H]DG) uptake into skeletal muscle and attenuates the increase in plasma glucose concentration after a glucose load and plasma concentrations of glucose and insulin. Valsartan treatment exaggerates the insulin-induced phosphorylation of IRS-1, the association of IRS-1 with the p85 regulatory subunit of phosphoinositide 3 kinase (PI 3-K), PI 3-K activity, and translocation of GLUT4 to the plasma membrane. Valsartan also reduces tumor necrosis factor-alpha (TNF-alpha) expression and superoxide production in skeletal muscle of KK-Ay mice.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥98%

Specifications

Sinónimos

N-​(1-​oxopentyl)​-​N-​[[2'-​(2H-​tetrazol-​5-​yl)​[1, ​1'-​biphenyl]​-​4-​yl]​methyl]​-L-​valine

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Valsartan (CGP-48933) is a selective angiotensin II receptor antagonist, used to treat high blood pressure and congestive heart failure.

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

Antagonist of AT 1 receptor

Propiedades del producto

• ALogP: 4.4

Nombres e identificadores

• Isómeros SMILES: CCCCC(=O)N(CC1=CC=C(C=C1)C2=CC=CC=C2C3=NNN=N3)[C@@H](C(C)C)C(=O)O
• WGK Alemania: 3
• CAS alternativo: 137862-53-4
• Número NSC: 758927
• Términos de entrada MeSH: 48933, CGP;CGP 48933;Diovan;Kalpress;Miten;N-valeryl-N-((2'-(1H-tetrazol-5-yl)biphenyl-4-yl)methyl)valine;Nisis;Provas;Tareg;Vals;valsartan
• Peso molecular: 435.52
• Reaxy-Rn: 24721853
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=24721853&ln=

Objetivos asociados (humanos)

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

Discover Target: AGTR1

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

Propiedades químicas y físicas

• Rotación específica [α]: -65°C
• Punto de fusión (°C): 117°C

Referencias

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