SB-657510
Based on 1 Customer Validation
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.84%
- CAS 番号: 474960-44-6
- 分子式: C19H22BrClN2O5S
- 分子量:505.81
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
43 nM
Compound: 4
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Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
Antagonist activity at recombinant human urotensin2 receptor expressed in CHO cells assessed as inhibition of urotensin2-stimulated Ca2+ mobilization after 1 hr by FLIPR assay
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[PMID: 23453841] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EA.hy926 cells (UII-induced)
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Concentration:1 μM
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Incubation Time:0.5, 1, 2, 4, 8 hours
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Result:Remarkably decreased the UII-induced protein expression of tissue factor.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 474960-44-6
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性状 Solid
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分子量 505.81
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分子式 C19H22BrClN2O5S
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Color White to off-white
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SMILES
ClC(C=C1)=C(O[C@H]2CN(C)CC2)C=C1NS(C3=CC(OC)=C(OC)C=C3Br)(=O)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (197.70 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (280 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9770 mL | 9.8851 mL | 19.7703 mL | 49.4257 mL |
| 5 mM | 0.3954 mL | 1.9770 mL | 3.9541 mL | 9.8851 mL | |
| 10 mM | 0.1977 mL | 0.9885 mL | 1.9770 mL | 4.9426 mL | |
| 15 mM | 0.1318 mL | 0.6590 mL | 1.3180 mL | 3.2950 mL | |
| 20 mM | 0.0989 mL | 0.4943 mL | 0.9885 mL | 2.4713 mL | |
| 25 mM | 0.0791 mL | 0.3954 mL | 0.7908 mL | 1.9770 mL | |
| 30 mM | 0.0659 mL | 0.3295 mL | 0.6590 mL | 1.6475 mL | |
| 40 mM | 0.0494 mL | 0.2471 mL | 0.4943 mL | 1.2356 mL | |
| 50 mM | 0.0395 mL | 0.1977 mL | 0.3954 mL | 0.9885 mL | |
| 60 mM | 0.0330 mL | 0.1648 mL | 0.3295 mL | 0.8238 mL | |
| 80 mM | 0.0247 mL | 0.1236 mL | 0.2471 mL | 0.6178 mL | |
| 100 mM | 0.0198 mL | 0.0989 mL | 0.1977 mL | 0.4943 mL |
SB-657510 関連分類
HY-10656 関連分類
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