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SB-657510
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SB-657510
Catalog No. T12848Cas 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. 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.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $75 | In Stock | |
| 5 mg | $226 | In Stock | |
| 10 mg | $340 | In Stock | |
| 25 mg | $547 | In Stock | |
| 50 mg | $738 | In Stock | |
| 100 mg | $987 | In Stock | |
| 500 mg | $1,970 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $253 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| 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] |
| Molecular Weight | 505.81 |
| Formula | C19H22BrClN2O5S |
| Cas No. | 474960-44-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 27.0 mg/mL (53.4 mM) | ||||||||||||||||||||||||||||||
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