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Ro 46-2005

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Chemical Structure| 150725-87-4 同义名 : -
CAS号 : 150725-87-4
货号 : A757918
分子式 : C23H27N3O6S
纯度 : 99%+
分子量 : 473.542
MDL号 : MFCD00918670
存储条件：

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

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(221.73 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.56mL

2.11mL

1.06mL

21.12mL

4.22mL

2.11mL
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.