CAS 474960-44-6|SB 657510
| Common Name | SB 657510 | ||
|---|---|---|---|
| CAS Number | 474960-44-6 | Molecular Weight | 505.81000 |
| Density | / | Boiling Point | / |
| Molecular Formula | C19H22BrClN2O5S | Melting Point | / |
| MSDS | ChineseUSA | Flash Point | / |
| Symbol | GHS07 | Signal Word | Warning |
Names
| Name | 2-bromo-N-[4-chloro-3-[(3R)-1-methylpyrrolidin-3-yl]oxyphenyl]-4,5-dimethoxybenzenesulfonamide |
|---|---|
| Synonym | More Synonyms |
SB 657510 BiologicalActivity
| 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[1][2]. |
|---|---|
| Related Catalog | Signaling Pathways >>Others >>OthersResearch Areas >>Inflammation/Immunology |
| 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 [Ca2+]i mobilization elicited by 10 nM hU-II with an IC50 of 180 nM[2]. 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]. |
| 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. |
Chemical & Physical Properties
| Molecular Formula | C19H22BrClN2O5S |
|---|---|
| Molecular Weight | 505.81000 |
| Exact Mass | 504.01200 |
| PSA | 85.48000 |
| LogP | 5.09510 |
| InChIKey | KQCZCINJGIRLCD-CYBMUJFWSA-N |
| SMILES | COc1cc(Br)c(S(=O)(=O)Nc2ccc(Cl)c(OC3CCN(C)C3)c2)cc1OC |
Safety Information
| Symbol | GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H315-H319-H335 |
| Precautionary Statements | P261-P305 + P351 + P338 |
| Hazard Codes | Xi |
| RIDADR | NONH for all modes of transport |
Articles1
More Articles| Urotensin II receptor antagonism confers vasoprotective effects in diabetes associated atherosclerosis: studies in humans and in a mouse model of diabetes. Diabetologia 56(5) , 1155-65, (2013) The small, highly conserved vasoactive peptide urotensin II (UII) is upregulated in atherosclerosis. However, its effects in diabetes-associated atherosclerosis have not been assessed.Endothelial cell... |
Synonyms
| Benzenesulfonamide,2-bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxy |
| 2-Bromo-N-[4-chloro-3-[[(3R)-1-methyl-3-pyrrolidinyl]oxy]phenyl]-4,5-dimethoxy-benzenesulfonamide |
