Ro 46-2005

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: Endothelin in 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]

Product Specifications

CAS Number

[150725-87-4]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Endothelin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Cardiovascular Disease; Endocrinology

Assay Protocol

https://www.medchemexpress.com/Ro-46-2005.html

Purity

98.32

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=S(C1=CC=C(C(C)(C)C)C=C1)(NC2=NC=NC(OCCO)=C2OC3=CC=CC(OC)=C3)=O

Molecular Formula

C23H27N3O6S

Molecular Weight

473.54

Precautions

H302, H315, H319, H335

References & Citations

[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)