[CAS NO. 474960-44-6] SB-657510
PRODUCTS SPECIFICATIONS [474960-44-6]
DESCRIPTION [474960-44-6]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 505.81 |
| Molecular Formula | C19H22BrClN2O5S |
| SMILES | ClC(C=C1)=C(O[C@H]2CN(C)CC2)C=C1NS(C3=CC(OC)=C(OC)C=C3Br)(=O)=O |
Summary
SB-657510 is a selective urotensin II (UII) receptor (UT) antagonist. The K i 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] .
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
[1]
.
SB-706375 (1-10000 nM) inhibits [Ca
2+
]
i
mobilization elicited by 10 nM hU-II with an IC
50
of 180 nM
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| 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
[1]
.
Levels of phosphorylated ERK are significantly attenuated in the aorta of SB-657510-treated (30 mg/kg/day) diabetic mice (Male Apoe KO mice)
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
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 |
References
- [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.