SB-657510

SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The Ki values are 61, 17, 30, 65 and 56 nM for human, monkey, cat, rat and mouse receptors, respectively. SB-657510 exerts anti-inflammatory effects by inhibiting UII-induced upregulation of inflammatory mediators such as adhesion molecules, cytokines, and tissue factor in human vascular endothelial cells[1][2].

Product Specifications

CAS Number

[474960-44-6]

UNSPSC

12352005

Hazard Statement

H303, H315, H319, H335

Target

Urotensin Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

Neuroscience-Neuromodulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/sb-657510.html

Purity

99.84

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

ClC(C=C1)=C(O[C@H]2CN(C)CC2)C=C1NS(C3=CC(OC)=C(OC)C=C3Br)(=O)=O

Molecular Formula

C19H22BrClN2O5S

Molecular Weight

505.81

Precautions

H303, H315, H319, H335

References & Citations

[1]Park SL, et al. Inhibitory Effect of an Urotensin II Receptor Antagonist on Proinflammatory Activation Inducedby Urotensin II in Human Vascular Endothelial Cells. Biomol Ther (Seoul) . 2013 Jul 30;21 (4) :277-83.|[2]Behm DJ, et al. Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. Br J Pharmacol. 2008 Oct;155 (3) :374-86.|[3]Watson AM, et al. Urotensin II receptor antagonism confers vasoprotective effects in diabetes associated atherosclerosis: studies in humans and in a mouse model of diabetes. Diabetologia. 2013 May;56 (5) :1155-65.