| Name | SB-657510 |
| 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. SB-657510 plays an anti-inflammatory role by inhibiting UII-induced inflammatory mediators, such as adhesion molecules, in human vascular endothelial cells and upregulation of cytokines and tissue factors. SB 657510 has a therapeutic effect on diabetes-related atherosclerotic disease in diabetic mouse models. |
| In vitro | The UII-induced increase in adhesion between U937 and EA.hy926 cells was blocked by SB-657510 dramatically. 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(IC50 of 180 nM).[2] |
| In vivo | The progression of high-fat diet-induced atherosclerosis and diabetes-associated atherosclerosis inhibited by SB-657510.[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] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 27 mg/mL (53.38 mM), Sonication is recommended.
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| Keywords | urotensin-II (UT) | SB-657510 | SB657510 | SB 657510 | NeurotensinReceptor | Neurotensin Receptor |
| Inhibitors Related | Monomethyl fumarate | Pamoic acid disodium | Azathioprine | CRTh2 antagonist 2 | Fezagepras sodium | Benzyl nicotinate | 1-methoxycyclopropanecarboxylic acid | TUG-1375 | CAY10595 | TUG-424 | Timapiprant | Tricosanoic acid |
| Related Compound Libraries | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Anti-Diabetic Compound Library | Inhibitor Library | Anti-Cardiovascular Disease Compound Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library |