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 Molecular Weight: 378.42 EC Number: 658-059-9

GRADE & PURITY 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

Overview

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%

Specifications

Synonyms

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

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

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).

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

Endothelin receptor, ET-A/ET-B antagonist

Product Properties

• ALogP: 3.8

Names and Identifiers

• Isomeric SMILES: CC1=CC(=NC(=N1)O[C@H](C(=O)O)C(C2=CC=CC=C2)(C3=CC=CC=C3)OC)C
• RTECS: UA2459660
• Molecular Weight: 378.42
• Reaxy-Rn: 7549073
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7549073&ln=

Associated Targets(Human)

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)

Chemical and Physical Properties

• Specific Rotation[α]: 173° (C=0.5,MeOH)
• Melt Point(°C): 178 °C(dec.)