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 分子式: C₂₂H₂₂N₂O₄ 分子量: 378.42 EC番号: 658-059-9

グレード＆純度 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

概要

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%

仕様

同義語

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

仕様と純度

Moligand™, 10mM in DMSO

生化学的・生理学的メカニズム

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).

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

等級

Moligand™

アクションタイプ

ANTAGONIST

作用メカニズム

Endothelin receptor, ET-A/ET-B antagonist

製品の性質

ALogP

3.8

名前と識別子

異性体SMILES

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

RTECS

UA2459660

分子量

378.42

Reaxy-Rn

7549073

Reaxys-RN_link_address

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

関連ターゲット（人間）

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)

化学的性質と物理的性質

• 比旋光度［α］: 173° (C=0.5,MeOH)
• 融点（°C）: 178 °C(dec.)

よくある質問

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.