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CAS No.: 150725-87-4

Ro 46-2005 Catalog No. CSN17902

Synonyms: RO-462005

Ro 46-2005 is an antagonist of endothelin receptor.

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生物活性

实验方案

技术信息

生物活性

描述Endothelin (ET), a 21 amino acid peptide, containing two disulfide bridges, is the most potent vasoconstrictor known to date. Two G-protein-coupled ET receptors with seven transmembrane spanning domains have been described, cloned from human tissue and defined as ETA and ETB receptors. Whereas ETA receptors are selective for ET-1 and ET-2 over ET-3, ET receptors bind all three isopeptides with similar potency. Ro 46-2005 is a new synthetic non-peptide endothelin (ET) receptor antagonist with IC50 220 nM for ETA. It binds to natural ETA receptors containing tissue, i.e. human smooth muscle cells and rat mesangial cells, and also to recombinant human ETA receptors with similar potencies^[3]. In a binding assay study, human smooth muscle cells, rat endothelial cells on membranes were performed in 250 μl 50 mM Tris buffer (pH 7.4, 25 mM MnC12, 1 mM EDTA, 0.5% (w/v) BSA) containing 5 - 35 μg protein, 32 pM 125I-labelled ET and increasing amounts of unlabelled ligands. In binding assays with [125I]ET-3 on ETA receptor a tracer concentration of 213 pM was used. Ro 46-2005 competed for the binding of ET-1 on cells carrying ETA receptor, i.e. human smooth muscle cells and rat endothelial cells, with IC50 values of 220 ± 60 nM and 430 ± 140 nM, respectively. Its potency for binding to ETB receptors was similar on membranes of human placenta (IC50 160 ± 77 nM) and porcine cerebellum (IC50 227 ± 92 nM)^[4].
参考文献

[1] Breu V, Loffler BM, et al. In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETB receptors. FEBS Lett. 1993 Nov 15;334(2):210-4.
[2] Clozel M, Breu V, et al. Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature. 1993 Oct 21;365(6448):759-61.
[3] Breu V, Löffler BM, Clozel M. In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETB receptors. FEBS Lett. 1993 Nov 15;334(2):210-4.
[4] Sakamoto S, Obayashi S, Aso T, Sato J, Hamasaki H, Azuma H. The mechanism of myometrial contractions induced by endothelin-1 in rat. Mol Hum Reprod. 1997 Dec;3(12):1029-35.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.1117 mL
- 10.5587 mL
- 21.1175 mL
- 5 mM
- 0.4223 mL
- 2.1117 mL
- 4.2235 mL
- 10 mM
- 0.2112 mL
- 1.0559 mL
- 2.1117 mL

技术信息

CAS号

150725-87-4

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H27N3O6S

运输

蓝冰

分子量

473.54

别名

RO-462005

溶解度

DMSO	320.0 mg/mL (675.8 mM)
Water	insoluble

动物实验配方

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Ro 46-2005 Catalog No. CSN17902

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