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SB-657510
🥰Excellent
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.
SB-657510
🥰Excellent
Purity: 98.03%
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.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $45 | In Stock | |
| 5 mg | $136 | In Stock | |
| 10 mg | $203 | In Stock | |
| 25 mg | $328 | In Stock | |
| 50 mg | $443 | In Stock | |
| 100 mg | $592 | In Stock | |
| 200 mg | $798 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $152 | In Stock |
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Purity:98.03%
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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.Product Introduction
Bioactivity
Chemical Properties
| 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. |
| Targets&IC50 | UTII receptor (mouse):56 nM, UTII receptor (rat):65 nM, UTII receptor (cat):30 nM, UTII receptor (monkey):17 nM, UTII receptor (human):61 nM |
| 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 |
| Smiles | COc1cc(Br)c(cc1OC)S(=O)(=O)Nc1ccc(Cl)c(O[C@@H]2CCN(C)C2)c1 |
| Relative Density. | 1.512 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 27.0 mg/mL (53.4 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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