SB-657510( —— )

Catalog No. M33117 CAS No. 474960-44-6

SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively.

Purity : >98% (HPLC)

COA

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Biological Information

Product Name

SB-657510
Note

Research use only, not for human use.
Brief Description

SB-657510 is a urotensin II (UII) receptor (UT) antagonist. The Ki values of UT for human, monkey, cat, rat and mouse were 61, 17, 30, 65 and 56 nM, respectively.
Description

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.
In Vitro

SB-657510 dramatically blocks the UII-induced increase in adhesion between U937 and EA.hy926 cell. SB-657510 (1 μM; 0.5-8 hours) blocks the expression of tissue factor induced by UII in endothelial cells.SB-706375 (1-10000 nM) inhibits [Ca2+]i mobilization elicited by 10?nM hU-II with an IC50 of 180?nM.Western Blot Analysis Cell Line:EA.hy926 cells (UII-induced)Concentration:1 μM Incubation Time:0.5, 1, 2, 4, 8 hours Result:Remarkably decreased the UII-induced protein expression of tissue factor.
In Vivo

SB-657510 inhibits the progression of high-fat diet induced atherosclerosis and diabetes-associated atherosclerosis.Levels of phosphorylated ERK are significantly attenuated in the aorta of SB-657510-treated (30 mg/kg/day) diabetic mice (Male Apoe KO mice).
Synonyms

——
Pathway

GPCR/G Protein
Target

Neurotensin Receptor
Recptor

Neurotensin Receptor
Research Area

——
Indication

——

Chemical Information

CAS Number

474960-44-6
Formula Weight

505.81
Molecular Formula

C19H22BrClN2O5S
Purity

>98% (HPLC)
Solubility

In Vitro:?DMSO : 100 mg/mL (197.70 mM; Ultrasonic )
SMILES

COc1cc(Br)c(cc1OC)S(=O)(=O)Nc1ccc(Cl)c(O[C@@H]2CCN(C)C2)c1
Chemical Name

——

Shipping & Storage Information

Storage

(-20℃)
Shipping

With Ice Pack
Stability

≥ 2 years

Reference

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.?

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