Ambrisentan - Moligand™, 10mM in DMSO , Endothelin receptor, ET-A/ET-B antagonist, CAS No.177036-94-1, Endothelin receptor, ET-A/ET-B antagonist

CAS: 177036-94-1 Cat. No.: A408058 Fórmula: C₂₂H₂₂N₂O₄ Peso molecular: 378.42 Número EC: 658-059-9

CALIDAD & PUREZA Moligand™, 10mM in DMSO

Synonyms

LU-208075, BSF-208075 | (αS)​-α-​[(4,​6-​dimethyl-​2-​pyrimidinyl)​oxy]​-​β-​methoxy-​β-​phenyl-benzenepropanoic acid

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

Ambrisentan Ambrisentan (LU-208075, BSF-208075) is a highly selective antagonist of the endothelin-1 type A receptor , used in the treatment of pulmonary arterial hypertension (PAH).
In vitro

Ambrisentan only increases intracellular calcein fluorescence in P388/dx cells at concentrations above 100 μM and in L-MDR1 cells not at all indicating negligible P-gp inhibition. Ambrisentan inhibits specific [(125)I]ET-1 binding in these tissues in a concentration-dependent manner. Ambrisentan undergoes oxidative metabolism mainly by cytochrome P450 (CYP) 3A4 and to a lesser extent by CYP3A5 and CYP2C19. Ambrisentan is not only a strong inducer of CYP3A4, but also of ABCB1 and ABCG2. Ambrisentan also has a concentration-dependent effect on PXR activity, but because plateau effects are not reached, an EC50-value could not be calculated. Ambrisentan inhibits specific [(125)I]ET-1 binding in a concentration-dependent manner at nanomolar ranges of IC50. Ambrisentan significantly increases the dissociation constant for bladder [(125)I]ET-1 binding without affecting maximal number of binding sites (Bmax). Ambrisentan seem to bind to bladder ET-1 receptor in a competitive and reversible manner. Ambrisentan is an effective and safe treatment which is a valuable addition to the armamentarium against PAH. Ambrisentan offers a relative lack of drug interactions, once daily dosing and reassuring liver safety, offering safety and convenience advantages over bosentan.

In vivo

Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Especificaciones

Sinónimos

LU-208075, BSF-208075 | (αS)​-α-​[(4,​6-​dimethyl-​2-​pyrimidinyl)​oxy]​-​β-​methoxy-​β-​phenyl-benzenepropanoic acid

Especificaciones y pureza

Moligand™, 10mM in DMSO

Mecanismos bioquímicos y fisiológicos

Ambrisentan (LU-208075, BSF-208075) is a highly selective antagonist of the endothelin-1 type A receptor, used in the treatment of pulmonary arterial hypertension (PAH).

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

Endothelin receptor, ET-A/ET-B antagonist

Propiedades del producto

ALogP

3.8

Nombres e identificadores

Isómeros SMILES

CC1=CC(=NC(=N1)O[C@H](C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)C

RTECS

UA2459660

Peso molecular

378.42

Reaxy-Rn

7549073

Reaxys-RN_link_address

https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7549073&ln=

Objetivos asociados (humanos)

EDNRA Tclin Endothelin-1 receptor (4 Activities)

Discover Target: EDNRA

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

EDNRB Tclin Endothelin receptor type B (1 Activities)

Discover Target: EDNRB

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

Propiedades químicas y físicas

• Rotación específica [α]: 173° (C=0.5,MeOH)
• Punto de fusión (°C): 178 °C(dec.)

Preguntas frecuentes

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 177036-94-1, the molecular formula is C22H22N2O4, and the molecular weight is 378.42 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.