Ro 46-2005_product_DataBase

Bioactivity

Ro 46-2005 is a novel synthetic non-peptide endothelin receptor antagonist, inhibits the specific binding of 125I-ET-1 to human vascular smooth muscle cells (ETA receptor) with IC50 of 220 nM.IC50 value: 220 nM (ETA) [2]Target: Endothelinin vitro: Ro 46-2005 proves to be equipotent (IC50 200-500 nM) for inhibition of [125I]ET-1 binding on the two known ET receptor subtypes (ETA and ETB). Ro 46-2005 also inhibits the functional consequences of ET-1 stimulation: the ET-l-induced release of arachidonic acid from rat mesangial cells was inhibited with an IC50 of 1.8 μM.[1]

Name

Ro 46-2005

CAS

150725-87-4

Formula

C23H27N3O6S

Molar Mass

473.54

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Breu V, et al. In vitro characterization of Ro 46-2005, a novel synthetic non-peptide endothelin antagonist of ETA and ETBreceptors. FEBS Lett. 1993 Nov 15;334(2):210-214. [2]. Clozel M, et al. Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature. 1993 Oct 21;365(6448):759-761. [3]. N.R. Sibson, et al. MRI Determination of the Mechanisms Underlying TNF-a-induced Changes in Cerebral Blood Volume, Tissue Water Diffusion and BBB Permeability. Proc. Intl. Soc. Mag. Reson. Med. 10 (2002)

PeptideDB

Ro 46-2005

CAS: 150725-87-4 F: C23H27N3O6S W: 473.54